TW202333666A - 抗芳香酶er﹢癌症之拉索昔芬(lasofoxifene)治療 - Google Patents
抗芳香酶er﹢癌症之拉索昔芬(lasofoxifene)治療 Download PDFInfo
- Publication number
- TW202333666A TW202333666A TW111143872A TW111143872A TW202333666A TW 202333666 A TW202333666 A TW 202333666A TW 111143872 A TW111143872 A TW 111143872A TW 111143872 A TW111143872 A TW 111143872A TW 202333666 A TW202333666 A TW 202333666A
- Authority
- TW
- Taiwan
- Prior art keywords
- lasoxifene
- cancer
- patient
- administered
- inhibitor
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims abstract description 120
- 201000011510 cancer Diseases 0.000 title claims abstract description 79
- GXESHMAMLJKROZ-IAPPQJPRSA-N lasofoxifene Chemical compound C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 GXESHMAMLJKROZ-IAPPQJPRSA-N 0.000 title claims abstract 3
- 229960002367 lasofoxifene Drugs 0.000 title claims abstract 3
- 238000011282 treatment Methods 0.000 title description 40
- 108010078554 Aromatase Proteins 0.000 title description 3
- 102000014654 Aromatase Human genes 0.000 title 1
- 239000003886 aromatase inhibitor Substances 0.000 claims abstract description 99
- 229940122815 Aromatase inhibitor Drugs 0.000 claims abstract description 83
- 238000000034 method Methods 0.000 claims abstract description 82
- 108010007005 Estrogen Receptor alpha Proteins 0.000 claims abstract description 70
- 102100038595 Estrogen receptor Human genes 0.000 claims abstract description 60
- 230000035772 mutation Effects 0.000 claims abstract description 54
- 229940002612 prodrug Drugs 0.000 claims abstract description 40
- 239000000651 prodrug Substances 0.000 claims abstract description 40
- 150000003839 salts Chemical class 0.000 claims abstract description 40
- 108020001756 ligand binding domains Proteins 0.000 claims abstract description 38
- 108090000623 proteins and genes Proteins 0.000 claims abstract description 26
- 108010038795 estrogen receptors Proteins 0.000 claims abstract description 15
- 229960004390 palbociclib Drugs 0.000 claims description 69
- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical group N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims description 69
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 46
- 229960003881 letrozole Drugs 0.000 claims description 40
- 206010006187 Breast cancer Diseases 0.000 claims description 38
- 238000009261 endocrine therapy Methods 0.000 claims description 29
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 claims description 27
- 239000003112 inhibitor Substances 0.000 claims description 18
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 claims description 14
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 claims description 13
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims description 12
- 101000715943 Caenorhabditis elegans Cyclin-dependent kinase 4 homolog Proteins 0.000 claims description 10
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 claims description 10
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims description 10
- 239000003197 protein kinase B inhibitor Substances 0.000 claims description 8
- 229940126638 Akt inhibitor Drugs 0.000 claims description 7
- 229960000255 exemestane Drugs 0.000 claims description 7
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims description 6
- 229960002932 anastrozole Drugs 0.000 claims description 6
- 229940078010 arimidex Drugs 0.000 claims description 6
- 229940087620 aromasin Drugs 0.000 claims description 6
- 229940087476 femara Drugs 0.000 claims description 6
- 229950003687 ribociclib Drugs 0.000 claims description 6
- 230000000699 topical effect Effects 0.000 claims description 6
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 5
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims description 5
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims description 5
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 5
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 5
- 239000006213 vaginal ring Substances 0.000 claims description 5
- 229940044953 vaginal ring Drugs 0.000 claims description 5
- 206010055113 Breast cancer metastatic Diseases 0.000 claims description 4
- 238000001990 intravenous administration Methods 0.000 claims description 4
- 229940095064 tartrate Drugs 0.000 claims description 4
- 229950001573 abemaciclib Drugs 0.000 claims description 3
- UZWDCWONPYILKI-UHFFFAOYSA-N n-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical compound C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims description 3
- 102000015694 estrogen receptors Human genes 0.000 claims description 2
- 102000013701 Cyclin-Dependent Kinase 4 Human genes 0.000 claims 1
- 102000013698 Cyclin-Dependent Kinase 6 Human genes 0.000 claims 1
- 101000882584 Homo sapiens Estrogen receptor Proteins 0.000 abstract description 2
- 210000004027 cell Anatomy 0.000 description 53
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 description 46
- 229960002258 fulvestrant Drugs 0.000 description 45
- 208000026310 Breast neoplasm Diseases 0.000 description 33
- 125000005647 linker group Chemical group 0.000 description 26
- 102000007594 Estrogen Receptor alpha Human genes 0.000 description 25
- 206010027476 Metastases Diseases 0.000 description 20
- 230000009401 metastasis Effects 0.000 description 20
- 238000011374 additional therapy Methods 0.000 description 18
- 238000011360 adjunctive therapy Methods 0.000 description 17
- 201000010099 disease Diseases 0.000 description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 17
- 229940046844 aromatase inhibitors Drugs 0.000 description 16
- 210000000988 bone and bone Anatomy 0.000 description 15
- 238000002560 therapeutic procedure Methods 0.000 description 14
- 210000004556 brain Anatomy 0.000 description 13
- 150000001875 compounds Chemical class 0.000 description 13
- 241000699670 Mus sp. Species 0.000 description 12
- 102000003676 Glucocorticoid Receptors Human genes 0.000 description 11
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 11
- 102000007469 Actins Human genes 0.000 description 10
- 108010085238 Actins Proteins 0.000 description 10
- 101150064205 ESR1 gene Proteins 0.000 description 10
- 238000004458 analytical method Methods 0.000 description 10
- 210000004072 lung Anatomy 0.000 description 10
- 230000004083 survival effect Effects 0.000 description 10
- 230000004614 tumor growth Effects 0.000 description 10
- 102100032187 Androgen receptor Human genes 0.000 description 9
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 description 9
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 description 9
- 108010080146 androgen receptors Proteins 0.000 description 9
- 210000004907 gland Anatomy 0.000 description 9
- 230000001394 metastastic effect Effects 0.000 description 9
- 206010061289 metastatic neoplasm Diseases 0.000 description 9
- 210000001519 tissue Anatomy 0.000 description 9
- 206010061818 Disease progression Diseases 0.000 description 8
- 230000000694 effects Effects 0.000 description 8
- 210000004185 liver Anatomy 0.000 description 8
- 102000003998 progesterone receptors Human genes 0.000 description 8
- 108090000468 progesterone receptors Proteins 0.000 description 8
- 229940095743 selective estrogen receptor modulator Drugs 0.000 description 8
- 239000000333 selective estrogen receptor modulator Substances 0.000 description 8
- 102220497176 Small vasohibin-binding protein_T47D_mutation Human genes 0.000 description 7
- 210000000481 breast Anatomy 0.000 description 7
- 239000008194 pharmaceutical composition Substances 0.000 description 7
- 238000001262 western blot Methods 0.000 description 7
- 206010009944 Colon cancer Diseases 0.000 description 6
- 108020004414 DNA Proteins 0.000 description 6
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 6
- 238000001514 detection method Methods 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
- 230000004907 flux Effects 0.000 description 6
- 238000003384 imaging method Methods 0.000 description 6
- 238000003364 immunohistochemistry Methods 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 230000002829 reductive effect Effects 0.000 description 6
- 238000012163 sequencing technique Methods 0.000 description 6
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 5
- NIJJYAXOARWZEE-UHFFFAOYSA-N Valproic acid Chemical compound CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 description 5
- 238000009098 adjuvant therapy Methods 0.000 description 5
- 229940011871 estrogen Drugs 0.000 description 5
- 239000000262 estrogen Substances 0.000 description 5
- 230000007246 mechanism Effects 0.000 description 5
- 238000007481 next generation sequencing Methods 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 206010003693 Atrophic vulvovaginitis Diseases 0.000 description 4
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 description 4
- 108010000817 Leuprolide Proteins 0.000 description 4
- 239000005089 Luciferase Substances 0.000 description 4
- 208000001132 Osteoporosis Diseases 0.000 description 4
- 208000002495 Uterine Neoplasms Diseases 0.000 description 4
- 230000003213 activating effect Effects 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 208000029742 colonic neoplasm Diseases 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 229940121372 histone deacetylase inhibitor Drugs 0.000 description 4
- 239000003276 histone deacetylase inhibitor Substances 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- 201000002313 intestinal cancer Diseases 0.000 description 4
- 238000011528 liquid biopsy Methods 0.000 description 4
- -1 macrogols Substances 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 229920001223 polyethylene glycol Polymers 0.000 description 4
- 230000035755 proliferation Effects 0.000 description 4
- 102000005962 receptors Human genes 0.000 description 4
- 108020003175 receptors Proteins 0.000 description 4
- 230000001629 suppression Effects 0.000 description 4
- 206010046766 uterine cancer Diseases 0.000 description 4
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical group ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 206010065687 Bone loss Diseases 0.000 description 3
- 229940123587 Cell cycle inhibitor Drugs 0.000 description 3
- 206010008342 Cervix carcinoma Diseases 0.000 description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 3
- 101150029707 ERBB2 gene Proteins 0.000 description 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- 229940125497 HER2 kinase inhibitor Drugs 0.000 description 3
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 description 3
- 108060001084 Luciferase Proteins 0.000 description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 3
- 206010027452 Metastases to bone Diseases 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- 102100040678 Programmed cell death protein 1 Human genes 0.000 description 3
- 101710089372 Programmed cell death protein 1 Proteins 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 208000015634 Rectal Neoplasms Diseases 0.000 description 3
- 239000006146 Roswell Park Memorial Institute medium Substances 0.000 description 3
- 229940121991 Serotonin and norepinephrine reuptake inhibitor Drugs 0.000 description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 description 3
- 102000044159 Ubiquitin Human genes 0.000 description 3
- 108090000848 Ubiquitin Proteins 0.000 description 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 3
- 206010047741 Vulval cancer Diseases 0.000 description 3
- 208000004354 Vulvar Neoplasms Diseases 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 208000009956 adenocarcinoma Diseases 0.000 description 3
- NCNRHFGMJRPRSK-MDZDMXLPSA-N belinostat Chemical compound ONC(=O)\C=C\C1=CC=CC(S(=O)(=O)NC=2C=CC=CC=2)=C1 NCNRHFGMJRPRSK-MDZDMXLPSA-N 0.000 description 3
- 238000001574 biopsy Methods 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 239000000872 buffer Substances 0.000 description 3
- 230000005754 cellular signaling Effects 0.000 description 3
- 201000010881 cervical cancer Diseases 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 3
- 201000000330 endometrial stromal sarcoma Diseases 0.000 description 3
- 208000029179 endometrioid stromal sarcoma Diseases 0.000 description 3
- 201000004101 esophageal cancer Diseases 0.000 description 3
- 229940125641 estrogen receptor degrader Drugs 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 206010017758 gastric cancer Diseases 0.000 description 3
- 238000007490 hematoxylin and eosin (H&E) staining Methods 0.000 description 3
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 201000005202 lung cancer Diseases 0.000 description 3
- 208000020816 lung neoplasm Diseases 0.000 description 3
- 210000003712 lysosome Anatomy 0.000 description 3
- 230000001868 lysosomic effect Effects 0.000 description 3
- 210000005075 mammary gland Anatomy 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000002609 medium Substances 0.000 description 3
- 208000037819 metastatic cancer Diseases 0.000 description 3
- 208000011575 metastatic malignant neoplasm Diseases 0.000 description 3
- 230000002611 ovarian Effects 0.000 description 3
- 206010038038 rectal cancer Diseases 0.000 description 3
- 201000001275 rectum cancer Diseases 0.000 description 3
- OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 description 3
- OHRURASPPZQGQM-UHFFFAOYSA-N romidepsin Natural products O1C(=O)C(C(C)C)NC(=O)C(=CC)NC(=O)C2CSSCCC=CC1CC(=O)NC(C(C)C)C(=O)N2 OHRURASPPZQGQM-UHFFFAOYSA-N 0.000 description 3
- 108010091666 romidepsin Proteins 0.000 description 3
- 239000003775 serotonin noradrenalin reuptake inhibitor Substances 0.000 description 3
- 238000003307 slaughter Methods 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 206010041823 squamous cell carcinoma Diseases 0.000 description 3
- 238000010561 standard procedure Methods 0.000 description 3
- 201000011549 stomach cancer Diseases 0.000 description 3
- 229960001603 tamoxifen Drugs 0.000 description 3
- 206010046885 vaginal cancer Diseases 0.000 description 3
- 208000013139 vaginal neoplasm Diseases 0.000 description 3
- 201000005102 vulva cancer Diseases 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- SIFNOOUKXBRGGB-AREMUKBSSA-N (6r)-6-[2-[ethyl-[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol Chemical compound C1=CC(CCNCC)=CC=C1CN(CC)C1=CC(OC)=CC=C1[C@H]1CC2=CC=C(O)C=C2CC1 SIFNOOUKXBRGGB-AREMUKBSSA-N 0.000 description 2
- KOAITBOFZOEDOC-BJMVGYQFSA-N (E)-3-[4-[[2-(4-fluoro-2,6-dimethylbenzoyl)-6-hydroxy-1-benzothiophen-3-yl]oxy]phenyl]prop-2-enoic acid Chemical compound FC1=CC(=C(C(=O)C2=C(C3=C(S2)C=C(C=C3)O)OC2=CC=C(C=C2)/C=C/C(=O)O)C(=C1)C)C KOAITBOFZOEDOC-BJMVGYQFSA-N 0.000 description 2
- BURHGPHDEVGCEZ-KJGLQBJMSA-N (e)-3-[4-[(e)-2-(2-chloro-4-fluorophenyl)-1-(1h-indazol-5-yl)but-1-enyl]phenyl]prop-2-enoic acid Chemical compound C=1C=C(F)C=C(Cl)C=1C(/CC)=C(C=1C=C2C=NNC2=CC=1)\C1=CC=C(\C=C\C(O)=O)C=C1 BURHGPHDEVGCEZ-KJGLQBJMSA-N 0.000 description 2
- GQCXHIKRWBIQMD-AKJBCIBTSA-N 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol Chemical compound FC1=C(C(=CC(=C1)NC1CN(C1)CCCF)F)[C@H]1N([C@@H](CC2=C1NC1=CC=CC=C21)C)CC(CO)(F)F GQCXHIKRWBIQMD-AKJBCIBTSA-N 0.000 description 2
- 102100029361 Aromatase Human genes 0.000 description 2
- 102000008096 B7-H1 Antigen Human genes 0.000 description 2
- 108010074708 B7-H1 Antigen Proteins 0.000 description 2
- 208000010392 Bone Fractures Diseases 0.000 description 2
- 229940045513 CTLA4 antagonist Drugs 0.000 description 2
- 201000009030 Carcinoma Diseases 0.000 description 2
- 208000005443 Circulating Neoplastic Cells Diseases 0.000 description 2
- 102100039498 Cytotoxic T-lymphocyte protein 4 Human genes 0.000 description 2
- IGXWBGJHJZYPQS-SSDOTTSWSA-N D-Luciferin Chemical compound OC(=O)[C@H]1CSC(C=2SC3=CC=C(O)C=C3N=2)=N1 IGXWBGJHJZYPQS-SSDOTTSWSA-N 0.000 description 2
- CYCGRDQQIOGCKX-UHFFFAOYSA-N Dehydro-luciferin Natural products OC(=O)C1=CSC(C=2SC3=CC(O)=CC=C3N=2)=N1 CYCGRDQQIOGCKX-UHFFFAOYSA-N 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 description 2
- BJGNCJDXODQBOB-UHFFFAOYSA-N Fivefly Luciferin Natural products OC(=O)C1CSC(C=2SC3=CC(O)=CC=C3N=2)=N1 BJGNCJDXODQBOB-UHFFFAOYSA-N 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- 229940126088 GDC-9545 Drugs 0.000 description 2
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- BLCLNMBMMGCOAS-URPVMXJPSA-N Goserelin Chemical compound C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 BLCLNMBMMGCOAS-URPVMXJPSA-N 0.000 description 2
- 108010069236 Goserelin Proteins 0.000 description 2
- 101710113864 Heat shock protein 90 Proteins 0.000 description 2
- 102000003964 Histone deacetylase Human genes 0.000 description 2
- 108090000353 Histone deacetylase Proteins 0.000 description 2
- 208000033830 Hot Flashes Diseases 0.000 description 2
- 206010060800 Hot flush Diseases 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 208000018142 Leiomyosarcoma Diseases 0.000 description 2
- DDWFXDSYGUXRAY-UHFFFAOYSA-N Luciferin Natural products CCc1c(C)c(CC2NC(=O)C(=C2C=C)C)[nH]c1Cc3[nH]c4C(=C5/NC(CC(=O)O)C(C)C5CC(=O)O)CC(=O)c4c3C DDWFXDSYGUXRAY-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- WDHOIABIERMLGY-CMJOXMDJSA-N N-[1-(3-fluoropropyl)azetidin-3-yl]-6-[(6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-3,6,8,9-tetrahydropyrazolo[4,3-f]isoquinolin-6-yl]pyridin-3-amine Chemical compound FCCCN1CC(C1)NC=1C=NC(=CC=1)[C@H]1N([C@@H](CC2=C3C(=CC=C12)NN=C3)C)CC(F)(F)F WDHOIABIERMLGY-CMJOXMDJSA-N 0.000 description 2
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 2
- 108091007960 PI3Ks Proteins 0.000 description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 2
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 description 2
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
- 239000008156 Ringer's lactate solution Substances 0.000 description 2
- 102100023085 Serine/threonine-protein kinase mTOR Human genes 0.000 description 2
- 201000001880 Sexual dysfunction Diseases 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 description 2
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 2
- 241000021375 Xenogenes Species 0.000 description 2
- 201000001256 adenosarcoma Diseases 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 229960003094 belinostat Drugs 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- SZMJVTADHFNAIS-BJMVGYQFSA-N chidamide Chemical compound NC1=CC(F)=CC=C1NC(=O)C(C=C1)=CC=C1CNC(=O)\C=C\C1=CC=CN=C1 SZMJVTADHFNAIS-BJMVGYQFSA-N 0.000 description 2
- 229950009221 chidamide Drugs 0.000 description 2
- 229960002173 citrulline Drugs 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 230000005750 disease progression Effects 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- INVTYAOGFAGBOE-UHFFFAOYSA-N entinostat Chemical compound NC1=CC=CC=C1NC(=O)C(C=C1)=CC=C1CNC(=O)OCC1=CC=CN=C1 INVTYAOGFAGBOE-UHFFFAOYSA-N 0.000 description 2
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 description 2
- 229960005167 everolimus Drugs 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 208000005017 glioblastoma Diseases 0.000 description 2
- 229960002913 goserelin Drugs 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 208000030776 invasive breast carcinoma Diseases 0.000 description 2
- 229940011083 istodax Drugs 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 description 2
- RGLRXNKKBLIBQS-XNHQSDQCSA-N leuprolide acetate Chemical compound CC(O)=O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 RGLRXNKKBLIBQS-XNHQSDQCSA-N 0.000 description 2
- 229960004338 leuprorelin Drugs 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- 229940087857 lupron Drugs 0.000 description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 229960003194 meglumine Drugs 0.000 description 2
- 235000010755 mineral Nutrition 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 229960003301 nivolumab Drugs 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 230000003000 nontoxic effect Effects 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 201000002528 pancreatic cancer Diseases 0.000 description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 description 2
- FPOHNWQLNRZRFC-ZHACJKMWSA-N panobinostat Chemical compound CC=1NC2=CC=CC=C2C=1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FPOHNWQLNRZRFC-ZHACJKMWSA-N 0.000 description 2
- 229960005184 panobinostat Drugs 0.000 description 2
- 230000036961 partial effect Effects 0.000 description 2
- 229960002621 pembrolizumab Drugs 0.000 description 2
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 description 2
- VLTRZXGMWDSKGL-UHFFFAOYSA-N perchloric acid Chemical compound OCl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-N 0.000 description 2
- 235000019260 propionic acid Nutrition 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- FECGNJPYVFEKOD-VMPITWQZSA-N resminostat Chemical compound C1=CC(CN(C)C)=CC=C1S(=O)(=O)N1C=C(\C=C\C(=O)NO)C=C1 FECGNJPYVFEKOD-VMPITWQZSA-N 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 238000009094 second-line therapy Methods 0.000 description 2
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 231100000872 sexual dysfunction Toxicity 0.000 description 2
- 238000009097 single-agent therapy Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 238000010186 staining Methods 0.000 description 2
- JJAHTWIKCUJRDK-UHFFFAOYSA-N succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate Chemical compound C1CC(CN2C(C=CC2=O)=O)CCC1C(=O)ON1C(=O)CCC1=O JJAHTWIKCUJRDK-UHFFFAOYSA-N 0.000 description 2
- SUVMJBTUFCVSAD-UHFFFAOYSA-N sulforaphane Chemical compound CS(=O)CCCCN=C=S SUVMJBTUFCVSAD-UHFFFAOYSA-N 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 229960001612 trastuzumab emtansine Drugs 0.000 description 2
- 235000013311 vegetables Nutrition 0.000 description 2
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 description 2
- 229960000237 vorinostat Drugs 0.000 description 2
- 230000003442 weekly effect Effects 0.000 description 2
- 229940061261 zolinza Drugs 0.000 description 2
- QBYIENPQHBMVBV-HFEGYEGKSA-N (2R)-2-hydroxy-2-phenylacetic acid Chemical compound O[C@@H](C(O)=O)c1ccccc1.O[C@@H](C(O)=O)c1ccccc1 QBYIENPQHBMVBV-HFEGYEGKSA-N 0.000 description 1
- GRZXWCHAXNAUHY-NSISKUIASA-N (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl]-3-(propan-2-ylamino)-1-propanone Chemical compound C1([C@H](C(=O)N2CCN(CC2)C=2C=3[C@H](C)C[C@@H](O)C=3N=CN=2)CNC(C)C)=CC=C(Cl)C=C1 GRZXWCHAXNAUHY-NSISKUIASA-N 0.000 description 1
- NNWYWNRCBPYLML-GWCFXTLKSA-N (2s)-2-amino-n-[(2s)-1-[4-(hydroxymethyl)anilino]-1-oxopropan-2-yl]-3-methylbutanamide Chemical group CC(C)[C@H](N)C(=O)N[C@@H](C)C(=O)NC1=CC=C(CO)C=C1 NNWYWNRCBPYLML-GWCFXTLKSA-N 0.000 description 1
- KDVXAPCZVZMPMU-XBBWARJSSA-N (2s)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C([C@H]2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-XBBWARJSSA-N 0.000 description 1
- SJXNPGGVGZXKKI-NYYWCZLTSA-N (E)-3-[4-[[2-[2-(1,1-difluoroethyl)-4-fluorophenyl]-6-hydroxy-1-benzothiophen-3-yl]oxy]phenyl]prop-2-enoic acid Chemical compound FC(C)(F)C1=C(C=CC(=C1)F)C1=C(C2=C(S1)C=C(C=C2)O)OC1=CC=C(C=C1)/C=C/C(=O)O SJXNPGGVGZXKKI-NYYWCZLTSA-N 0.000 description 1
- LAMIXXKAWNLXOC-INIZCTEOSA-N (S)-HDAC-42 Chemical compound O=C([C@@H](C(C)C)C=1C=CC=CC=1)NC1=CC=C(C(=O)NO)C=C1 LAMIXXKAWNLXOC-INIZCTEOSA-N 0.000 description 1
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- DFBDRVGWBHBJNR-BBNFHIFMSA-N (e)-3-[3,5-difluoro-4-[(1r,3r)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H](N2CC(C)(C)F)C)=C(F)C=C(\C=C\C(O)=O)C=C1F DFBDRVGWBHBJNR-BBNFHIFMSA-N 0.000 description 1
- PRXXYMVLYKJITB-IZZDOVSWSA-N (e)-n-(2-aminophenyl)-3-[1-[4-(1-methylpyrazol-4-yl)phenyl]sulfonylpyrrol-3-yl]prop-2-enamide Chemical compound C1=NN(C)C=C1C1=CC=C(S(=O)(=O)N2C=C(\C=C\C(=O)NC=3C(=CC=CC=3)N)C=C2)C=C1 PRXXYMVLYKJITB-IZZDOVSWSA-N 0.000 description 1
- AUGCSOFQTDKPSO-RGVLZGJSSA-N (e)-n-[3-(dimethylamino)propyl]-n'-hydroxy-2-(naphthalen-1-yloxymethyl)oct-2-enediamide Chemical compound C1=CC=C2C(OC/C(C(=O)NCCCN(C)C)=C\CCCCC(=O)NO)=CC=CC2=C1 AUGCSOFQTDKPSO-RGVLZGJSSA-N 0.000 description 1
- OQCYTSHIQNPJIC-QURGRASLSA-N 1-[(e)-2-bromo-1,2-diphenylethenyl]-4-ethylbenzene Chemical compound C1=CC(CC)=CC=C1C(\C=1C=CC=CC=1)=C(\Br)C1=CC=CC=C1 OQCYTSHIQNPJIC-QURGRASLSA-N 0.000 description 1
- WLXGQMVCYPUOLM-UHFFFAOYSA-N 1-hydroxyethanesulfonic acid Chemical compound CC(O)S(O)(=O)=O WLXGQMVCYPUOLM-UHFFFAOYSA-N 0.000 description 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
- WXBXVVIUZANZAU-UHFFFAOYSA-N 2E-decenoic acid Natural products CCCCCCCC=CC(O)=O WXBXVVIUZANZAU-UHFFFAOYSA-N 0.000 description 1
- MAUCONCHVWBMHK-UHFFFAOYSA-N 3-[(dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)-oxomethyl]phenoxy]ethyl]-2-benzofurancarboxamide Chemical compound O1C2=CC=CC=C2C(CN(C)C)=C1C(=O)NCCOC1=CC=C(C(=O)NO)C=C1 MAUCONCHVWBMHK-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- PRDJGNVQBVXXEO-UHFFFAOYSA-N 3-cyanopropyl carbamimidothioate Chemical compound NC(=N)SCCCC#N PRDJGNVQBVXXEO-UHFFFAOYSA-N 0.000 description 1
- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 description 1
- SUVMJBTUFCVSAD-JTQLQIEISA-N 4-Methylsulfinylbutyl isothiocyanate Natural products C[S@](=O)CCCCN=C=S SUVMJBTUFCVSAD-JTQLQIEISA-N 0.000 description 1
- JHENVVKNLBODLB-UHFFFAOYSA-N 4-[[1-(2,5-dioxopyrrolidin-1-yl)-2h-pyridin-2-yl]disulfanyl]butanoic acid Chemical compound OC(=O)CCCSSC1C=CC=CN1N1C(=O)CCC1=O JHENVVKNLBODLB-UHFFFAOYSA-N 0.000 description 1
- JDUBGYFRJFOXQC-KRWDZBQOSA-N 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide Chemical compound C1([C@H](CCO)NC(=O)C2(CCN(CC2)C=2C=3C=CNC=3N=CN=2)N)=CC=C(Cl)C=C1 JDUBGYFRJFOXQC-KRWDZBQOSA-N 0.000 description 1
- WRFYIYOXJWKONR-UHFFFAOYSA-N 4-bromo-2-methoxyaniline Chemical compound COC1=CC(Br)=CC=C1N WRFYIYOXJWKONR-UHFFFAOYSA-N 0.000 description 1
- KEWSCDNULKOKTG-UHFFFAOYSA-N 4-cyano-4-ethylsulfanylcarbothioylsulfanylpentanoic acid Chemical compound CCSC(=S)SC(C)(C#N)CCC(O)=O KEWSCDNULKOKTG-UHFFFAOYSA-N 0.000 description 1
- KISZAGQTIXIVAR-VWLOTQADSA-N 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid Chemical compound ClC1=C(C=CC(=C1)Cl)C1=C(C2=C(CCC1)C=C(C=C2)C(=O)O)C1=CC=C(C=C1)O[C@@H]1CN(CC1)CCCF KISZAGQTIXIVAR-VWLOTQADSA-N 0.000 description 1
- PLIVFNIUGLLCEK-UHFFFAOYSA-N 7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-n-hydroxyheptanamide Chemical compound C=12C=C(OCCCCCCC(=O)NO)C(OC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 PLIVFNIUGLLCEK-UHFFFAOYSA-N 0.000 description 1
- 101150092476 ABCA1 gene Proteins 0.000 description 1
- 102100024387 AF4/FMR2 family member 3 Human genes 0.000 description 1
- 108700005241 ATP Binding Cassette Transporter 1 Proteins 0.000 description 1
- 102100033618 ATP-binding cassette sub-family A member 2 Human genes 0.000 description 1
- 229940125815 AZD9833 Drugs 0.000 description 1
- 102100040202 Apolipoprotein B-100 Human genes 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 206010003694 Atrophy Diseases 0.000 description 1
- 102100026434 BCAS3 microtubule associated cell migration factor Human genes 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 102100022544 Bone morphogenetic protein 7 Human genes 0.000 description 1
- 206010006002 Bone pain Diseases 0.000 description 1
- 108010014064 CCCTC-Binding Factor Proteins 0.000 description 1
- 108010021064 CTLA-4 Antigen Proteins 0.000 description 1
- 101100314454 Caenorhabditis elegans tra-1 gene Proteins 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 206010007275 Carcinoid tumour Diseases 0.000 description 1
- 201000000274 Carcinosarcoma Diseases 0.000 description 1
- 102000003952 Caspase 3 Human genes 0.000 description 1
- 108090000397 Caspase 3 Proteins 0.000 description 1
- 102000005600 Cathepsins Human genes 0.000 description 1
- 108010084457 Cathepsins Proteins 0.000 description 1
- 102100025064 Cellular tumor antigen p53 Human genes 0.000 description 1
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 description 1
- 102100037637 Cholesteryl ester transfer protein Human genes 0.000 description 1
- 206010052360 Colorectal adenocarcinoma Diseases 0.000 description 1
- 208000036493 Contralateral breast cancer Diseases 0.000 description 1
- 208000037845 Cutaneous squamous cell carcinoma Diseases 0.000 description 1
- 102100032640 Cytochrome P450 2F1 Human genes 0.000 description 1
- 102000053602 DNA Human genes 0.000 description 1
- 102100034578 Desmoglein-2 Human genes 0.000 description 1
- 102100032245 Dynein axonemal heavy chain 2 Human genes 0.000 description 1
- 102100031648 Dynein axonemal heavy chain 5 Human genes 0.000 description 1
- 102100034745 E3 ubiquitin-protein ligase HERC2 Human genes 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- 108700024394 Exon Proteins 0.000 description 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 206010064571 Gene mutation Diseases 0.000 description 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 102100033366 Glutathione hydrolase 1 proenzyme Human genes 0.000 description 1
- 102100028972 HLA class I histocompatibility antigen, A alpha chain Human genes 0.000 description 1
- 108010075704 HLA-A Antigens Proteins 0.000 description 1
- 102100022132 High affinity immunoglobulin epsilon receptor subunit gamma Human genes 0.000 description 1
- 102100027755 Histone-lysine N-methyltransferase 2C Human genes 0.000 description 1
- 102100029768 Histone-lysine N-methyltransferase SETD1A Human genes 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 101000833166 Homo sapiens AF4/FMR2 family member 3 Proteins 0.000 description 1
- 101000801645 Homo sapiens ATP-binding cassette sub-family A member 2 Proteins 0.000 description 1
- 101000889953 Homo sapiens Apolipoprotein B-100 Proteins 0.000 description 1
- 101000919395 Homo sapiens Aromatase Proteins 0.000 description 1
- 101000766273 Homo sapiens BCAS3 microtubule associated cell migration factor Proteins 0.000 description 1
- 101000899361 Homo sapiens Bone morphogenetic protein 7 Proteins 0.000 description 1
- 101000880514 Homo sapiens Cholesteryl ester transfer protein Proteins 0.000 description 1
- 101000941738 Homo sapiens Cytochrome P450 2F1 Proteins 0.000 description 1
- 101000889276 Homo sapiens Cytotoxic T-lymphocyte protein 4 Proteins 0.000 description 1
- 101000924314 Homo sapiens Desmoglein-2 Proteins 0.000 description 1
- 101001016199 Homo sapiens Dynein axonemal heavy chain 2 Proteins 0.000 description 1
- 101000866368 Homo sapiens Dynein axonemal heavy chain 5 Proteins 0.000 description 1
- 101000872516 Homo sapiens E3 ubiquitin-protein ligase HERC2 Proteins 0.000 description 1
- 101000997558 Homo sapiens Glutathione hydrolase 1 proenzyme Proteins 0.000 description 1
- 101000824104 Homo sapiens High affinity immunoglobulin epsilon receptor subunit gamma Proteins 0.000 description 1
- 101001008892 Homo sapiens Histone-lysine N-methyltransferase 2C Proteins 0.000 description 1
- 101000865038 Homo sapiens Histone-lysine N-methyltransferase SETD1A Proteins 0.000 description 1
- 101000998020 Homo sapiens Keratin, type I cytoskeletal 18 Proteins 0.000 description 1
- 101000975496 Homo sapiens Keratin, type II cytoskeletal 8 Proteins 0.000 description 1
- 101001042362 Homo sapiens Leukemia inhibitory factor receptor Proteins 0.000 description 1
- 101001051093 Homo sapiens Low-density lipoprotein receptor Proteins 0.000 description 1
- 101000731007 Homo sapiens Membrane-associated progesterone receptor component 2 Proteins 0.000 description 1
- 101000958409 Homo sapiens Mitogen-activated protein kinase kinase kinase 10 Proteins 0.000 description 1
- 101000623901 Homo sapiens Mucin-16 Proteins 0.000 description 1
- 101000635935 Homo sapiens Myosin-IIIa Proteins 0.000 description 1
- 101000624947 Homo sapiens Nesprin-1 Proteins 0.000 description 1
- 101000990908 Homo sapiens Neutrophil collagenase Proteins 0.000 description 1
- 101000830386 Homo sapiens Neutrophil defensin 3 Proteins 0.000 description 1
- 101000633516 Homo sapiens Nuclear receptor subfamily 2 group F member 6 Proteins 0.000 description 1
- 101000735213 Homo sapiens Palladin Proteins 0.000 description 1
- 101001045218 Homo sapiens Peroxisomal multifunctional enzyme type 2 Proteins 0.000 description 1
- 101000734702 Homo sapiens Proline-, glutamic acid- and leucine-rich protein 1 Proteins 0.000 description 1
- 101000775052 Homo sapiens Protein AHNAK2 Proteins 0.000 description 1
- 101000855004 Homo sapiens Protein Wnt-7a Proteins 0.000 description 1
- 101000896576 Homo sapiens Putative cytochrome P450 2D7 Proteins 0.000 description 1
- 101001092176 Homo sapiens Ras-GEF domain-containing family member 1B Proteins 0.000 description 1
- 101001099871 Homo sapiens Ras-related protein Rab-42 Proteins 0.000 description 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 description 1
- 101000606537 Homo sapiens Receptor-type tyrosine-protein phosphatase delta Proteins 0.000 description 1
- 101001123846 Homo sapiens Serine/threonine-protein kinase Nek1 Proteins 0.000 description 1
- 101001074042 Homo sapiens Transcriptional activator GLI3 Proteins 0.000 description 1
- 101000851515 Homo sapiens Transmembrane channel-like protein 8 Proteins 0.000 description 1
- 101000892398 Homo sapiens Tryptophan 2,3-dioxygenase Proteins 0.000 description 1
- 101000851865 Homo sapiens Tryptophan 5-hydroxylase 2 Proteins 0.000 description 1
- 101000801232 Homo sapiens Tumor necrosis factor receptor superfamily member 1B Proteins 0.000 description 1
- 101000617285 Homo sapiens Tyrosine-protein phosphatase non-receptor type 6 Proteins 0.000 description 1
- 101000734214 Homo sapiens Unconventional prefoldin RPB5 interactor 1 Proteins 0.000 description 1
- 101001104102 Homo sapiens X-linked retinitis pigmentosa GTPase regulator Proteins 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- PIWKPBJCKXDKJR-UHFFFAOYSA-N Isoflurane Chemical compound FC(F)OC(Cl)C(F)(F)F PIWKPBJCKXDKJR-UHFFFAOYSA-N 0.000 description 1
- 102100033421 Keratin, type I cytoskeletal 18 Human genes 0.000 description 1
- 102100023972 Keratin, type II cytoskeletal 8 Human genes 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 241000713666 Lentivirus Species 0.000 description 1
- 102100021747 Leukemia inhibitory factor receptor Human genes 0.000 description 1
- 108010017736 Leukocyte Immunoglobulin-like Receptor B1 Proteins 0.000 description 1
- 102100025584 Leukocyte immunoglobulin-like receptor subfamily B member 1 Human genes 0.000 description 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 108010075654 MAP Kinase Kinase Kinase 1 Proteins 0.000 description 1
- 108700012912 MYCN Proteins 0.000 description 1
- 101150022024 MYCN gene Proteins 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 102100032400 Membrane-associated progesterone receptor component 2 Human genes 0.000 description 1
- 102100033115 Mitogen-activated protein kinase kinase kinase 1 Human genes 0.000 description 1
- 102100038243 Mitogen-activated protein kinase kinase kinase 10 Human genes 0.000 description 1
- 102100025725 Mothers against decapentaplegic homolog 4 Human genes 0.000 description 1
- 101710143112 Mothers against decapentaplegic homolog 4 Proteins 0.000 description 1
- 102100023123 Mucin-16 Human genes 0.000 description 1
- 102100030743 Myosin-IIIa Human genes 0.000 description 1
- HRNLUBSXIHFDHP-UHFFFAOYSA-N N-(2-aminophenyl)-4-[[[4-(3-pyridinyl)-2-pyrimidinyl]amino]methyl]benzamide Chemical compound NC1=CC=CC=C1NC(=O)C(C=C1)=CC=C1CNC1=NC=CC(C=2C=NC=CC=2)=N1 HRNLUBSXIHFDHP-UHFFFAOYSA-N 0.000 description 1
- 108700026495 N-Myc Proto-Oncogene Proteins 0.000 description 1
- QGZYDVAGYRLSKP-UHFFFAOYSA-N N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)-5-pyrimidinecarboxamide Chemical compound N1=CC(C(=O)NCCCCCCC(=O)NO)=CN=C1N(C=1C=CC=CC=1)C1=CC=CC=C1 QGZYDVAGYRLSKP-UHFFFAOYSA-N 0.000 description 1
- PAWIYAYFNXQGAP-UHFFFAOYSA-N N-hydroxy-2-[4-[[(1-methyl-3-indolyl)methylamino]methyl]-1-piperidinyl]-5-pyrimidinecarboxamide Chemical compound C12=CC=CC=C2N(C)C=C1CNCC(CC1)CCN1C1=NC=C(C(=O)NO)C=N1 PAWIYAYFNXQGAP-UHFFFAOYSA-N 0.000 description 1
- 102100030124 N-myc proto-oncogene protein Human genes 0.000 description 1
- 206010061309 Neoplasm progression Diseases 0.000 description 1
- 102100023306 Nesprin-1 Human genes 0.000 description 1
- 102100030411 Neutrophil collagenase Human genes 0.000 description 1
- 102100024761 Neutrophil defensin 3 Human genes 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- 102100029528 Nuclear receptor subfamily 2 group F member 6 Human genes 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 102100035031 Palladin Human genes 0.000 description 1
- 206010061336 Pelvic neoplasm Diseases 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 102100022587 Peroxisomal multifunctional enzyme type 2 Human genes 0.000 description 1
- 102100033616 Phospholipid-transporting ATPase ABCA1 Human genes 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 102100034729 Proline-, glutamic acid- and leucine-rich protein 1 Human genes 0.000 description 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 description 1
- 102100031838 Protein AHNAK2 Human genes 0.000 description 1
- 102100020729 Protein Wnt-7a Human genes 0.000 description 1
- 102100021702 Putative cytochrome P450 2D7 Human genes 0.000 description 1
- IWYDHOAUDWTVEP-UHFFFAOYSA-N R-2-phenyl-2-hydroxyacetic acid Natural products OC(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-N 0.000 description 1
- 102100033810 RAC-alpha serine/threonine-protein kinase Human genes 0.000 description 1
- 102100035583 Ras-GEF domain-containing family member 1B Human genes 0.000 description 1
- 102100038506 Ras-related protein Rab-42 Human genes 0.000 description 1
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 description 1
- 102100039666 Receptor-type tyrosine-protein phosphatase delta Human genes 0.000 description 1
- 206010038019 Rectal adenocarcinoma Diseases 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 102100028751 Serine/threonine-protein kinase Nek1 Human genes 0.000 description 1
- 208000000453 Skin Neoplasms Diseases 0.000 description 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 1
- 101000611441 Solanum lycopersicum Pathogenesis-related leaf protein 6 Proteins 0.000 description 1
- 102100024470 Stabilin-2 Human genes 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- 102000004398 TNF receptor-associated factor 1 Human genes 0.000 description 1
- 108090000920 TNF receptor-associated factor 1 Proteins 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 102100035559 Transcriptional activator GLI3 Human genes 0.000 description 1
- 102100027671 Transcriptional repressor CTCF Human genes 0.000 description 1
- 102100036770 Transmembrane channel-like protein 8 Human genes 0.000 description 1
- 102100040653 Tryptophan 2,3-dioxygenase Human genes 0.000 description 1
- 108010078814 Tumor Suppressor Protein p53 Proteins 0.000 description 1
- 102100033733 Tumor necrosis factor receptor superfamily member 1B Human genes 0.000 description 1
- 102100021657 Tyrosine-protein phosphatase non-receptor type 6 Human genes 0.000 description 1
- 102100033622 Unconventional prefoldin RPB5 interactor 1 Human genes 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 206010046799 Uterine leiomyosarcoma Diseases 0.000 description 1
- 102100040092 X-linked retinitis pigmentosa GTPase regulator Human genes 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 201000008395 adenosquamous carcinoma Diseases 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 229940070192 amcenestrant Drugs 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000037444 atrophy Effects 0.000 description 1
- 229960000817 bazedoxifene Drugs 0.000 description 1
- UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical compound C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 229940077840 beleodaq Drugs 0.000 description 1
- JUHORIMYRDESRB-UHFFFAOYSA-N benzathine Chemical compound C=1C=CC=CC=1CNCCNCC1=CC=CC=C1 JUHORIMYRDESRB-UHFFFAOYSA-N 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- 229940092714 benzenesulfonic acid Drugs 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- SUMDYPCJJOFFON-UHFFFAOYSA-N beta-hydroxyethanesulfonic acid Natural products OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 description 1
- 206010005084 bladder transitional cell carcinoma Diseases 0.000 description 1
- 201000001528 bladder urothelial carcinoma Diseases 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 229950003738 broparestrol Drugs 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- BPKIGYQJPYCAOW-FFJTTWKXSA-I calcium;potassium;disodium;(2s)-2-hydroxypropanoate;dichloride;dihydroxide;hydrate Chemical compound O.[OH-].[OH-].[Na+].[Na+].[Cl-].[Cl-].[K+].[Ca+2].C[C@H](O)C([O-])=O BPKIGYQJPYCAOW-FFJTTWKXSA-I 0.000 description 1
- BMLSTPRTEKLIPM-UHFFFAOYSA-I calcium;potassium;disodium;hydrogen carbonate;dichloride;dihydroxide;hydrate Chemical compound O.[OH-].[OH-].[Na+].[Na+].[Cl-].[Cl-].[K+].[Ca+2].OC([O-])=O BMLSTPRTEKLIPM-UHFFFAOYSA-I 0.000 description 1
- 229940125164 camizestrant Drugs 0.000 description 1
- 229940022399 cancer vaccine Drugs 0.000 description 1
- 238000009566 cancer vaccine Methods 0.000 description 1
- 229950009671 capivasertib Drugs 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 208000002458 carcinoid tumor Diseases 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 125000002091 cationic group Chemical group 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000011748 cell maturation Effects 0.000 description 1
- 239000006285 cell suspension Substances 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 229960002798 cetrimide Drugs 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 229910052729 chemical element Inorganic materials 0.000 description 1
- 238000004296 chiral HPLC Methods 0.000 description 1
- VDANGULDQQJODZ-UHFFFAOYSA-N chloroprocaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1Cl VDANGULDQQJODZ-UHFFFAOYSA-N 0.000 description 1
- 229960002023 chloroprocaine Drugs 0.000 description 1
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 description 1
- 229960001231 choline Drugs 0.000 description 1
- 238000013375 chromatographic separation Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 208000009060 clear cell adenocarcinoma Diseases 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 1
- 201000010897 colon adenocarcinoma Diseases 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 208000030381 cutaneous melanoma Diseases 0.000 description 1
- GLNWREBYRLDPQP-MHZLTWQESA-N cyclopentyl (2s)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate Chemical compound C1=CC(NC(=O)CCCCCCC(=O)NO)=CC=C1CN[C@@H](C=1C=CC=CC=1)C(=O)OC1CCCC1 GLNWREBYRLDPQP-MHZLTWQESA-N 0.000 description 1
- 230000000593 degrading effect Effects 0.000 description 1
- 229960001251 denosumab Drugs 0.000 description 1
- 229940089052 depakene Drugs 0.000 description 1
- 229940075925 depakote Drugs 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
- 229940043237 diethanolamine Drugs 0.000 description 1
- FKGKZBBDJSKCIS-UHFFFAOYSA-N diethyl-[[6-[[4-(hydroxycarbamoyl)phenyl]carbamoyloxymethyl]naphthalen-2-yl]methyl]azanium;chloride;hydrate Chemical compound O.[Cl-].C1=CC2=CC(C[NH+](CC)CC)=CC=C2C=C1COC(=O)NC1=CC=C(C(=O)NO)C=C1 FKGKZBBDJSKCIS-UHFFFAOYSA-N 0.000 description 1
- 238000007847 digital PCR Methods 0.000 description 1
- 229940098766 effexor Drugs 0.000 description 1
- 229950005473 elacestrant Drugs 0.000 description 1
- 239000008387 emulsifying waxe Substances 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 230000002357 endometrial effect Effects 0.000 description 1
- 210000001163 endosome Anatomy 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- 229940012017 ethylenediamine Drugs 0.000 description 1
- 238000001640 fractional crystallisation Methods 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 235000011087 fumaric acid Nutrition 0.000 description 1
- 229960002870 gabapentin Drugs 0.000 description 1
- 201000006585 gastric adenocarcinoma Diseases 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 239000002474 gonadorelin antagonist Substances 0.000 description 1
- 229940121381 gonadotrophin releasing hormone (gnrh) antagonists Drugs 0.000 description 1
- 210000004013 groin Anatomy 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 229940022353 herceptin Drugs 0.000 description 1
- 230000001744 histochemical effect Effects 0.000 description 1
- 108091008039 hormone receptors Proteins 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
- 229940071870 hydroiodic acid Drugs 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 229940126389 imlunestrant Drugs 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000010874 in vitro model Methods 0.000 description 1
- 238000011503 in vivo imaging Methods 0.000 description 1
- 238000012623 in vivo measurement Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 229950006331 ipatasertib Drugs 0.000 description 1
- 229960005386 ipilimumab Drugs 0.000 description 1
- 229960002725 isoflurane Drugs 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- XZEUAXYWNKYKPL-WDYNHAJCSA-N levormeloxifene Chemical compound C1([C@H]2[C@@H](C3=CC=C(C=C3OC2(C)C)OC)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 XZEUAXYWNKYKPL-WDYNHAJCSA-N 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 238000004020 luminiscence type Methods 0.000 description 1
- 201000005243 lung squamous cell carcinoma Diseases 0.000 description 1
- 239000012139 lysis buffer Substances 0.000 description 1
- 230000002132 lysosomal effect Effects 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 229960002510 mandelic acid Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 210000003470 mitochondria Anatomy 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 229940126619 mouse monoclonal antibody Drugs 0.000 description 1
- 201000010879 mucinous adenocarcinoma Diseases 0.000 description 1
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 description 1
- QRGHOAATPOLDPF-VQFNDLOPSA-N nanatinostat Chemical compound N1=CC(C(=O)NO)=CN=C1N1C[C@@H]([C@@H]2NCC=3N=C4C=CC(F)=CC4=CC=3)[C@@H]2C1 QRGHOAATPOLDPF-VQFNDLOPSA-N 0.000 description 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-N naphthalene-2-sulfonic acid Chemical compound C1=CC=CC2=CC(S(=O)(=O)O)=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 238000009806 oophorectomy Methods 0.000 description 1
- 238000003305 oral gavage Methods 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 229960003327 ormeloxifene Drugs 0.000 description 1
- 229960003969 ospemifene Drugs 0.000 description 1
- LUMKNAVTFCDUIE-VHXPQNKSSA-N ospemifene Chemical compound C1=CC(OCCO)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 LUMKNAVTFCDUIE-VHXPQNKSSA-N 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 235000019371 penicillin G benzathine Nutrition 0.000 description 1
- 230000001175 peptic effect Effects 0.000 description 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 1
- 201000002628 peritoneum cancer Diseases 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- BMIJYAZXNZEMLI-UHFFFAOYSA-N piridocaine Chemical compound NC1=CC=CC=C1C(=O)OCCC1NCCCC1 BMIJYAZXNZEMLI-UHFFFAOYSA-N 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- JHDKZFFAIZKUCU-ZRDIBKRKSA-N pracinostat Chemical compound ONC(=O)/C=C/C1=CC=C2N(CCN(CC)CC)C(CCCC)=NC2=C1 JHDKZFFAIZKUCU-ZRDIBKRKSA-N 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000004237 preparative chromatography Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 230000017854 proteolysis Effects 0.000 description 1
- 230000004063 proteosomal degradation Effects 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 229960004622 raloxifene Drugs 0.000 description 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 description 1
- 201000001281 rectum adenocarcinoma Diseases 0.000 description 1
- 230000008929 regeneration Effects 0.000 description 1
- 238000011069 regeneration method Methods 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 229950002821 resminostat Drugs 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 238000003757 reverse transcription PCR Methods 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 229940073462 rintodestrant Drugs 0.000 description 1
- 229960003452 romidepsin Drugs 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 201000000849 skin cancer Diseases 0.000 description 1
- 201000003708 skin melanoma Diseases 0.000 description 1
- 201000010106 skin squamous cell carcinoma Diseases 0.000 description 1
- 208000000587 small cell lung carcinoma Diseases 0.000 description 1
- 201000002314 small intestine cancer Diseases 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000008354 sodium chloride injection Substances 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 229940010817 stavzor Drugs 0.000 description 1
- 230000000707 stereoselective effect Effects 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 229960005559 sulforaphane Drugs 0.000 description 1
- 235000015487 sulforaphane Nutrition 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229950009112 tefinostat Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- UWHCKJMYHZGTIT-UHFFFAOYSA-N tetraethylene glycol Chemical compound OCCOCCOCCOCCO UWHCKJMYHZGTIT-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229960005026 toremifene Drugs 0.000 description 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- WXBXVVIUZANZAU-CMDGGOBGSA-N trans-2-decenoic acid Chemical compound CCCCCCC\C=C\C(O)=O WXBXVVIUZANZAU-CMDGGOBGSA-N 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- 229960000575 trastuzumab Drugs 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 239000000107 tumor biomarker Substances 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000004565 tumor cell growth Effects 0.000 description 1
- 230000005751 tumor progression Effects 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- 229960000604 valproic acid Drugs 0.000 description 1
- 229960004688 venlafaxine Drugs 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 229940055760 yervoy Drugs 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163280769P | 2021-11-18 | 2021-11-18 | |
| US63/280,769 | 2021-11-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW202333666A true TW202333666A (zh) | 2023-09-01 |
Family
ID=79163840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW111143872A TW202333666A (zh) | 2021-11-18 | 2022-11-17 | 抗芳香酶er﹢癌症之拉索昔芬(lasofoxifene)治療 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20230149350A1 (enExample) |
| EP (1) | EP4433048A1 (enExample) |
| JP (1) | JP2024538402A (enExample) |
| KR (1) | KR20240132447A (enExample) |
| CN (1) | CN118574612A (enExample) |
| AU (2) | AU2022389457B2 (enExample) |
| CA (1) | CA3238899A1 (enExample) |
| GB (1) | GB202116903D0 (enExample) |
| IL (1) | IL312895A (enExample) |
| MX (1) | MX2024005959A (enExample) |
| TW (1) | TW202333666A (enExample) |
| WO (1) | WO2023091553A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12023321B2 (en) | 2021-11-18 | 2024-07-02 | Sermonix Pharmaceuticals, Inc. | Lasofoxifene treatment of aromatase-resistant ER+cancer |
| US12414924B2 (en) | 2016-10-11 | 2025-09-16 | Duke University | Lasofoxifene treatment of breast cancer |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025043004A1 (en) * | 2023-08-21 | 2025-02-27 | Duke University | Treatment of solid cancer with lasofoxifene |
| WO2025075631A1 (en) * | 2023-10-06 | 2025-04-10 | Sermonix Pharmaceuticals, Inc. | Lasofoxifene treatment of endocrine therapy resistant er+ cancer |
| WO2025165887A1 (en) * | 2024-01-30 | 2025-08-07 | Sermonix Pharmaceuticals, Inc. | Lasofoxifene treatment of er+ cancers with constitutively active esr1 mutations |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6060503A (en) | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| US5552412A (en) | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
| UA51676C2 (uk) | 1995-11-02 | 2002-12-16 | Пфайзер Інк. | (-)цис-6(s)-феніл-5(r)[4-(2-піролідин-1-ілетокси)феніл]-5,6,7,8-тетрагідронафталін-2-ол d-тартрат, спосіб його одержання, спосіб лікування захворювань, що піддаються лікуванню агоністами естрогену, та фармацевтична композиція |
| IL120266A (en) | 1996-02-28 | 2005-05-17 | Pfizer | Use of estrogen antagonists and estrogen agonists in the preparation of medicaments for inhibiting pathological conditions |
| HN1996000101A (es) | 1996-02-28 | 1997-06-26 | Inc Pfizer | Terapia combinada para la osteoporosis |
| US20040044080A1 (en) | 1997-10-28 | 2004-03-04 | Place Virgil A. | Treatment of dyspareunia with topically administered nitroglycerin formulations |
| YU26700A (sh) | 1999-05-24 | 2002-06-19 | Pfizer Products Inc. | Postupak za cis-1-(2-(4-(6-metoksi-2-fenil-1,2,3,4- tetrahidronaftalen-1-il)fenoksi)etil)pirolidin |
| EP1086692A3 (en) | 1999-07-28 | 2003-07-09 | Pfizer Products Inc. | Estrogen agonists and antagonists for multiple indications |
| US6436977B1 (en) | 1999-09-29 | 2002-08-20 | Pfizer Inc. | Dosing regimens for lasofoxifene |
| CO5271697A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona |
| BR0108107A (pt) | 2000-01-28 | 2003-03-11 | Endorech Inc | Moduladores seletivos dos receptores de estrogênio em combinação com estrogênios; kits e composições farmacêuticas para praticar tal combinação; bem como a administração da referida combinação |
| DE10039199A1 (de) | 2000-08-10 | 2002-02-21 | Schering Ag | Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen |
| JP2004507465A (ja) | 2000-08-11 | 2004-03-11 | ワイス | エストロゲン受容体陽性癌腫の治療方法 |
| WO2002056903A2 (en) | 2001-01-17 | 2002-07-25 | Praecis Pharmaceuticals Inc. | Methods for treating hormone associated conditions using a combination of lhrh antagonists and specific estrogen receptor modulators |
| AU781168B2 (en) | 2001-01-26 | 2005-05-12 | Pfizer Products Inc. | Method of treating certain cancers using an estrogen agonist/antagonist |
| RU2278861C2 (ru) | 2002-03-28 | 2006-06-27 | Пфайзер Продактс Инк. | Очищенный лазофоксифен и способ очистки рацемического лазофоксифена рекристаллизацией |
| PA8576201A1 (es) | 2002-07-10 | 2004-05-26 | Pfizer Prod Inc | Composicion farmaceutica que tiene una distribucion y potencia uniforme de farmaco |
| US8835413B2 (en) | 2004-10-20 | 2014-09-16 | Endorecherche, Inc. | Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women |
| US20090012052A1 (en) | 2006-11-09 | 2009-01-08 | Ore Pharmaceuticals Inc. | Method for treating er+ breast cancer |
| US20110015134A1 (en) | 2007-04-16 | 2011-01-20 | Retsky Michael W | Method of treatment for early stage cancer |
| CZ2007373A3 (cs) | 2007-05-29 | 2008-12-10 | Zentiva, A. S | Zpusob prípravy lasofoxifenu |
| CA2725390C (en) | 2008-04-08 | 2014-09-23 | Syndax Pharmaceuticals, Inc. | Use of a hdac inhibitor and a her-2 inhibitor in the treatment of breast cancer |
| WO2009137543A2 (en) | 2008-05-06 | 2009-11-12 | Ore Pharmaceuticals Inc. | Methods for breast cancer screening and treatment |
| CN102405047B (zh) * | 2009-01-30 | 2014-07-09 | 葛兰素史密斯克莱有限责任公司 | 结晶型的n-{(1s)-2-氨基-1-[(3-氟苯基)甲基]乙基}-5-氯-4-(4-氯-1-甲基-1h-吡唑-5-基)-2-噻吩甲酰胺盐酸盐 |
| EP2239570A1 (en) | 2009-04-10 | 2010-10-13 | PamGene B.V. | Method for determining the estrogen receptor status of breast cancer |
| MX373926B (es) | 2009-05-27 | 2020-07-10 | Ptc Therapeutics Inc | Metodos para tratar cancer y estados no neoplasicos. |
| US20130253035A1 (en) | 2010-08-16 | 2013-09-26 | Duke University | Camkk-beta as a target for treating cancer |
| US20120052508A1 (en) | 2010-08-27 | 2012-03-01 | Rutgers, The State University Of New Jersey | Genetic markers and diagnostic methods for resistance of breast cancer to hormonal therapies |
| US20140134170A1 (en) | 2011-03-11 | 2014-05-15 | Merrimack Pharmaceuticals, Inc. | Use of inhibitors of egfr-family receptors in the treatment of hormone refractory breast cancers |
| AU2012255920A1 (en) | 2011-05-18 | 2013-11-07 | Merck Sharp & Dohme Corp. | Therapeutic anti-IGF1R combinations |
| WO2013056178A2 (en) | 2011-10-14 | 2013-04-18 | Foundation Medicine, Inc. | Novel estrogen receptor mutations and uses thereof |
| EP2791128A4 (en) | 2011-12-16 | 2015-04-22 | Olema Pharmaceuticals Inc | NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF |
| US20160038506A1 (en) | 2012-02-14 | 2016-02-11 | Repros Therapeutics Inc. | Selective Estrogen Receptor Modulators With Short Half-Lives and Uses Thereof |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US20160030389A1 (en) | 2013-03-13 | 2016-02-04 | Alevere Medical Corporation | Use of indole compounds for fat reduction and skin and soft tissue tightening |
| US9204286B1 (en) | 2013-03-15 | 2015-12-01 | Sprint Communications Company L.P. | System and method of branding and labeling a mobile device |
| WO2015136016A2 (en) | 2014-03-13 | 2015-09-17 | F. Hoffmann-La Roche Ag | Therapeutic combinations with estrogen receptor modulators |
| SG11201607339VA (en) | 2014-03-13 | 2016-10-28 | Hoffmann La Roche | Methods and compositions for modulating estrogen receptor mutants |
| US9421264B2 (en) | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| ES3055185T3 (en) | 2014-03-28 | 2026-02-10 | Univ Duke | Treatment of an estrogen receptor positive breast cancer using a selective estrogen receptor modulator |
| CN113101292B (zh) | 2014-05-08 | 2023-07-11 | 上海市生物医药技术研究院 | 双炔失碳酯组合物和疾病治疗方法 |
| KR20170078811A (ko) | 2014-11-07 | 2017-07-07 | 리폭센 테크놀로지즈 리미티드 | 원발성 호르몬 저항성 자궁내막암 및 유방암 치료 방법 |
| AU2016247674A1 (en) | 2015-04-14 | 2017-10-19 | Atossa Genetics Inc. | Compositions and methods of treatment of breast disorders and estrogen-related disorders |
| KR20250152679A (ko) | 2015-04-29 | 2025-10-23 | 래디어스 파마슈티컬스, 인코포레이티드 | 암을 치료하는 방법 |
| ES2909576T3 (es) | 2016-10-11 | 2022-05-09 | Univ Duke | Tratamiento con lasofoxifeno del cáncer de mama ER+ |
| WO2018071437A1 (en) | 2016-10-11 | 2018-04-19 | Sermonix Pharmaceuticals, Llc | Lasofoxifene treatment of vva and osteoporosis in survivors of breast cancer and other malignancies |
| CN115737637A (zh) | 2017-01-10 | 2023-03-07 | 王巍 | 拉索昔芬调节膜结合雌激素信号的应用及治疗癌症的方法 |
| CN107861293A (zh) * | 2017-12-21 | 2018-03-30 | 惠科股份有限公司 | 液晶显示器及其背光模组 |
| US11497730B2 (en) | 2018-04-10 | 2022-11-15 | Duke University | Lasofoxifene treatment of breast cancer |
| JP7571006B2 (ja) | 2018-08-17 | 2024-10-22 | ジェネンテック, インコーポレイテッド | 乳がんの処置のための診断的および治療的方法 |
| EP4412649A4 (en) | 2021-10-05 | 2025-11-05 | Univ Duke | Compositions containing small molecule tumor immunity regulators and their methods of use |
| GB202116903D0 (en) | 2021-11-18 | 2022-01-05 | Sermonix Pharmaceuticals Inc | Lasofoxifene treatment of aromatase-resistant er+ cancer |
| JP2025517483A (ja) | 2022-05-25 | 2025-06-05 | サーモニックス ファーマシューティカルズ, インコーポレイテッド | Cdk4/6阻害剤で進行したer+乳がんのラソフォキシフェン併用処置 |
-
2021
- 2021-11-24 GB GBGB2116903.2A patent/GB202116903D0/en not_active Ceased
-
2022
- 2022-11-17 CN CN202280089063.1A patent/CN118574612A/zh active Pending
- 2022-11-17 CA CA3238899A patent/CA3238899A1/en active Pending
- 2022-11-17 KR KR1020247020057A patent/KR20240132447A/ko active Pending
- 2022-11-17 US US17/989,382 patent/US20230149350A1/en not_active Abandoned
- 2022-11-17 TW TW111143872A patent/TW202333666A/zh unknown
- 2022-11-17 WO PCT/US2022/050218 patent/WO2023091553A1/en not_active Ceased
- 2022-11-17 IL IL312895A patent/IL312895A/en unknown
- 2022-11-17 JP JP2024529563A patent/JP2024538402A/ja active Pending
- 2022-11-17 MX MX2024005959A patent/MX2024005959A/es unknown
- 2022-11-17 EP EP22839032.4A patent/EP4433048A1/en active Pending
- 2022-11-17 AU AU2022389457A patent/AU2022389457B2/en active Active
-
2023
- 2023-05-30 US US18/325,883 patent/US12023321B2/en active Active
-
2024
- 2024-07-04 US US18/764,277 patent/US12433866B2/en active Active
-
2025
- 2025-03-13 AU AU2025201821A patent/AU2025201821B2/en active Active
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12414924B2 (en) | 2016-10-11 | 2025-09-16 | Duke University | Lasofoxifene treatment of breast cancer |
| US12023321B2 (en) | 2021-11-18 | 2024-07-02 | Sermonix Pharmaceuticals, Inc. | Lasofoxifene treatment of aromatase-resistant ER+cancer |
| US12433866B2 (en) | 2021-11-18 | 2025-10-07 | Sermonix Pharmaceuticals, Inc. | Lasofoxifene treatment of aromatase-resistant ER+ cancer |
Also Published As
| Publication number | Publication date |
|---|---|
| US20230321035A1 (en) | 2023-10-12 |
| WO2023091553A1 (en) | 2023-05-25 |
| CN118574612A (zh) | 2024-08-30 |
| IL312895A (en) | 2024-07-01 |
| US12023321B2 (en) | 2024-07-02 |
| US20230149350A1 (en) | 2023-05-18 |
| CA3238899A1 (en) | 2023-05-25 |
| US12433866B2 (en) | 2025-10-07 |
| JP2024538402A (ja) | 2024-10-18 |
| AU2022389457B2 (en) | 2024-12-19 |
| AU2022389457A1 (en) | 2024-07-04 |
| US20240358677A1 (en) | 2024-10-31 |
| MX2024005959A (es) | 2024-08-14 |
| GB202116903D0 (en) | 2022-01-05 |
| KR20240132447A (ko) | 2024-09-03 |
| AU2025201821A1 (en) | 2025-04-03 |
| EP4433048A1 (en) | 2024-09-25 |
| AU2025201821B2 (en) | 2026-03-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TW202333666A (zh) | 抗芳香酶er﹢癌症之拉索昔芬(lasofoxifene)治療 | |
| US12414924B2 (en) | Lasofoxifene treatment of breast cancer | |
| WO2025075631A1 (en) | Lasofoxifene treatment of endocrine therapy resistant er+ cancer | |
| HK40077706A (en) | Lasofoxifene treatment of er+ breast cancer | |
| HK40005311B (en) | Lasofoxifene treatment of er+ breast cancer | |
| HK40005311A (en) | Lasofoxifene treatment of er+ breast cancer |