JP2014508782A - ホルモン不応性乳癌の治療におけるｅｇｆｒファミリー受容体の阻害剤の使用 - Google Patents
ホルモン不応性乳癌の治療におけるｅｇｆｒファミリー受容体の阻害剤の使用 Download PDFInfo
- Publication number
- JP2014508782A JP2014508782A JP2013557943A JP2013557943A JP2014508782A JP 2014508782 A JP2014508782 A JP 2014508782A JP 2013557943 A JP2013557943 A JP 2013557943A JP 2013557943 A JP2013557943 A JP 2013557943A JP 2014508782 A JP2014508782 A JP 2014508782A
- Authority
- JP
- Japan
- Prior art keywords
- erbb3
- antibody
- inhibitor
- patient
- erbb2
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000003112 inhibitor Substances 0.000 title claims abstract description 81
- 208000018819 hormone-resistant breast carcinoma Diseases 0.000 title claims abstract description 45
- 238000011282 treatment Methods 0.000 title claims abstract description 45
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 title claims 3
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 title claims 3
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 title claims 3
- 238000000034 method Methods 0.000 claims abstract description 99
- 108090000556 Neuregulin-1 Proteins 0.000 claims abstract description 48
- 239000003886 aromatase inhibitor Substances 0.000 claims abstract description 38
- 229940122815 Aromatase inhibitor Drugs 0.000 claims abstract description 32
- 239000002246 antineoplastic agent Substances 0.000 claims abstract description 31
- 208000026310 Breast neoplasm Diseases 0.000 claims abstract description 28
- 229940088597 hormone Drugs 0.000 claims abstract description 18
- 239000005556 hormone Substances 0.000 claims abstract description 18
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 18
- 239000000833 heterodimer Substances 0.000 claims abstract description 17
- 229940102550 Estrogen receptor antagonist Drugs 0.000 claims abstract description 15
- 230000012010 growth Effects 0.000 claims abstract description 14
- 210000004881 tumor cell Anatomy 0.000 claims abstract description 9
- 102000048238 Neuregulin-1 Human genes 0.000 claims abstract 13
- 206010028980 Neoplasm Diseases 0.000 claims description 133
- 108010038795 estrogen receptors Proteins 0.000 claims description 80
- 102000015694 estrogen receptors Human genes 0.000 claims description 80
- 210000004027 cell Anatomy 0.000 claims description 56
- 239000000203 mixture Substances 0.000 claims description 55
- 229960003881 letrozole Drugs 0.000 claims description 44
- 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 44
- 201000011510 cancer Diseases 0.000 claims description 36
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims description 35
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims description 33
- 206010006187 Breast cancer Diseases 0.000 claims description 27
- 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 claims description 26
- 150000003384 small molecules Chemical group 0.000 claims description 24
- 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 23
- 229960000255 exemestane Drugs 0.000 claims description 23
- 230000004913 activation Effects 0.000 claims description 21
- 238000002560 therapeutic procedure Methods 0.000 claims description 19
- 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 claims description 16
- 229960005167 everolimus Drugs 0.000 claims description 16
- 230000026731 phosphorylation Effects 0.000 claims description 15
- 238000006366 phosphorylation reaction Methods 0.000 claims description 15
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 13
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 13
- 229960001603 tamoxifen Drugs 0.000 claims description 13
- 230000004614 tumor growth Effects 0.000 claims description 13
- 238000012360 testing method Methods 0.000 claims description 12
- 230000005764 inhibitory process Effects 0.000 claims description 11
- 230000001404 mediated effect Effects 0.000 claims description 10
- 230000011664 signaling Effects 0.000 claims description 10
- -1 taxanes Substances 0.000 claims description 10
- CLPFFLWZZBQMAO-UHFFFAOYSA-N 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 CLPFFLWZZBQMAO-UHFFFAOYSA-N 0.000 claims description 9
- 229960002932 anastrozole Drugs 0.000 claims description 9
- 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 9
- 229950011548 fadrozole Drugs 0.000 claims description 9
- 229960004421 formestane Drugs 0.000 claims description 9
- OSVMTWJCGUFAOD-KZQROQTASA-N formestane Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1O OSVMTWJCGUFAOD-KZQROQTASA-N 0.000 claims description 9
- 229960003437 aminoglutethimide Drugs 0.000 claims description 8
- ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 claims description 8
- 238000001574 biopsy Methods 0.000 claims description 8
- 229940127089 cytotoxic agent Drugs 0.000 claims description 8
- 239000000328 estrogen antagonist Substances 0.000 claims description 8
- 238000001802 infusion Methods 0.000 claims description 8
- 150000002596 lactones Chemical class 0.000 claims description 8
- 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 claims description 7
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 7
- 229940046836 anti-estrogen Drugs 0.000 claims description 7
- 230000001833 anti-estrogenic effect Effects 0.000 claims description 7
- 229960002258 fulvestrant Drugs 0.000 claims description 7
- 229960004622 raloxifene Drugs 0.000 claims description 7
- 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 claims description 7
- 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 claims description 7
- 229960005026 toremifene Drugs 0.000 claims description 7
- 238000004458 analytical method Methods 0.000 claims description 6
- 238000011260 co-administration Methods 0.000 claims description 6
- 229940121647 egfr inhibitor Drugs 0.000 claims description 6
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 6
- 239000002525 vasculotropin inhibitor Substances 0.000 claims description 6
- DODQJNMQWMSYGS-QPLCGJKRSA-N 4-[(z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-phenylbut-1-en-2-yl]phenol Chemical compound C=1C=C(O)C=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 DODQJNMQWMSYGS-QPLCGJKRSA-N 0.000 claims description 5
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 5
- 206010027476 Metastases Diseases 0.000 claims description 5
- MCGDSOGUHLTADD-UHFFFAOYSA-N arzoxifene Chemical compound C1=CC(OC)=CC=C1C1=C(OC=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 MCGDSOGUHLTADD-UHFFFAOYSA-N 0.000 claims description 5
- 229950005529 arzoxifene Drugs 0.000 claims description 5
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 5
- 230000009401 metastasis Effects 0.000 claims description 5
- 229960002087 pertuzumab Drugs 0.000 claims description 5
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 5
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 5
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical group C1C[C@@H](OC(=O)C(C)(CO)CO)[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 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims description 4
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims description 4
- 210000004899 c-terminal region Anatomy 0.000 claims description 4
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 4
- 229960004891 lapatinib Drugs 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims description 4
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[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 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 4
- 229960002930 sirolimus Drugs 0.000 claims description 4
- 229960000235 temsirolimus Drugs 0.000 claims description 4
- QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 claims description 4
- GFNNBHLJANVSQV-UHFFFAOYSA-N tyrphostin AG 1478 Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=CC(Cl)=C1 GFNNBHLJANVSQV-UHFFFAOYSA-N 0.000 claims description 4
- SYYMNUFXRFAELA-BTQNPOSSSA-N 4-[4-[[(1r)-1-phenylethyl]amino]-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenol;hydrobromide Chemical compound Br.N([C@H](C)C=1C=CC=CC=1)C(C=1C=2)=NC=NC=1NC=2C1=CC=C(O)C=C1 SYYMNUFXRFAELA-BTQNPOSSSA-N 0.000 claims description 3
- 101710199605 Endoribonuclease Proteins 0.000 claims description 3
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 3
- KFHMLBXBRCITHF-UHFFFAOYSA-N PD158780 Chemical compound N1=CN=C2C=NC(NC)=CC2=C1NC1=CC=CC(Br)=C1 KFHMLBXBRCITHF-UHFFFAOYSA-N 0.000 claims description 3
- 101710113029 Serine/threonine-protein kinase Proteins 0.000 claims description 3
- 229940123237 Taxane Drugs 0.000 claims description 3
- 229960001686 afatinib Drugs 0.000 claims description 3
- 229960000397 bevacizumab Drugs 0.000 claims description 3
- 229960005395 cetuximab Drugs 0.000 claims description 3
- 229960002584 gefitinib Drugs 0.000 claims description 3
- 238000000338 in vitro Methods 0.000 claims description 3
- 238000010253 intravenous injection Methods 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 230000002018 overexpression Effects 0.000 claims description 3
- 229910052697 platinum Inorganic materials 0.000 claims description 3
- 239000003909 protein kinase inhibitor Substances 0.000 claims description 3
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 210000000481 breast Anatomy 0.000 claims description 2
- 229960001433 erlotinib Drugs 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 230000002611 ovarian Effects 0.000 claims description 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 4
- BUROJSBIWGDYCN-GAUTUEMISA-N AP 23573 Chemical compound C1C[C@@H](OP(C)(C)=O)[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 BUROJSBIWGDYCN-GAUTUEMISA-N 0.000 claims 2
- 229960001302 ridaforolimus Drugs 0.000 claims 2
- 241000234671 Ananas Species 0.000 claims 1
- 102100030011 Endoribonuclease Human genes 0.000 claims 1
- 206010029098 Neoplasm skin Diseases 0.000 claims 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 208000037841 lung tumor Diseases 0.000 claims 1
- 239000003087 receptor blocking agent Substances 0.000 claims 1
- 229950008834 seribantumab Drugs 0.000 description 51
- 241000699670 Mus sp. Species 0.000 description 35
- 102400000058 Neuregulin-1 Human genes 0.000 description 35
- 239000003814 drug Substances 0.000 description 21
- 150000001875 compounds Chemical class 0.000 description 16
- 102100035360 Cerebellar degeneration-related antigen 1 Human genes 0.000 description 14
- 239000008194 pharmaceutical composition Substances 0.000 description 13
- 230000001225 therapeutic effect Effects 0.000 description 11
- 101800001382 Betacellulin Proteins 0.000 description 10
- 102100029837 Probetacellulin Human genes 0.000 description 10
- 239000000427 antigen Substances 0.000 description 10
- 108091007433 antigens Proteins 0.000 description 10
- 102000036639 antigens Human genes 0.000 description 10
- 230000000694 effects Effects 0.000 description 10
- 102000005962 receptors Human genes 0.000 description 10
- 108020003175 receptors Proteins 0.000 description 10
- 229940124597 therapeutic agent Drugs 0.000 description 10
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 9
- 241000699666 Mus <mouse, genus> Species 0.000 description 9
- 230000014509 gene expression Effects 0.000 description 9
- 108090000623 proteins and genes Proteins 0.000 description 9
- 239000003124 biologic agent Substances 0.000 description 8
- 239000003795 chemical substances by application Substances 0.000 description 8
- 230000007423 decrease Effects 0.000 description 8
- 239000003937 drug carrier Substances 0.000 description 8
- 229940011871 estrogen Drugs 0.000 description 8
- 239000000262 estrogen Substances 0.000 description 8
- 108091027967 Small hairpin RNA Proteins 0.000 description 7
- 108020004459 Small interfering RNA Proteins 0.000 description 7
- 229940079593 drug Drugs 0.000 description 7
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 description 7
- 238000003364 immunohistochemistry Methods 0.000 description 7
- 230000002452 interceptive effect Effects 0.000 description 7
- 239000004055 small Interfering RNA Substances 0.000 description 7
- 241001465754 Metazoa Species 0.000 description 6
- 208000002495 Uterine Neoplasms Diseases 0.000 description 6
- 229940046844 aromatase inhibitors Drugs 0.000 description 6
- 235000018102 proteins Nutrition 0.000 description 6
- 102000004169 proteins and genes Human genes 0.000 description 6
- 101001034652 Homo sapiens Insulin-like growth factor 1 receptor Proteins 0.000 description 5
- 108700005091 Immunoglobulin Genes Proteins 0.000 description 5
- 102100039688 Insulin-like growth factor 1 receptor Human genes 0.000 description 5
- 206010033128 Ovarian cancer Diseases 0.000 description 5
- 101710100969 Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 description 5
- 150000001413 amino acids Chemical group 0.000 description 5
- 238000002648 combination therapy Methods 0.000 description 5
- 238000011161 development Methods 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 238000007912 intraperitoneal administration Methods 0.000 description 5
- 229940043355 kinase inhibitor Drugs 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 5
- 108090000765 processed proteins & peptides Proteins 0.000 description 5
- 102000003998 progesterone receptors Human genes 0.000 description 5
- 108090000468 progesterone receptors Proteins 0.000 description 5
- 238000010186 staining Methods 0.000 description 5
- 206010046766 uterine cancer Diseases 0.000 description 5
- 230000003442 weekly effect Effects 0.000 description 5
- 108010078554 Aromatase Proteins 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 description 4
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 239000013543 active substance Substances 0.000 description 4
- 239000003963 antioxidant agent Substances 0.000 description 4
- 235000006708 antioxidants Nutrition 0.000 description 4
- 238000003556 assay Methods 0.000 description 4
- 239000006185 dispersion Substances 0.000 description 4
- GTTBEUCJPZQMDZ-UHFFFAOYSA-N erlotinib hydrochloride Chemical compound [H+].[Cl-].C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 GTTBEUCJPZQMDZ-UHFFFAOYSA-N 0.000 description 4
- 239000012634 fragment Substances 0.000 description 4
- 238000002347 injection Methods 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- 238000007913 intrathecal administration Methods 0.000 description 4
- 238000001990 intravenous administration Methods 0.000 description 4
- 239000003446 ligand Substances 0.000 description 4
- 231100000682 maximum tolerated dose Toxicity 0.000 description 4
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 description 4
- 229920001184 polypeptide Polymers 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 102000004196 processed proteins & peptides Human genes 0.000 description 4
- 238000009097 single-agent therapy Methods 0.000 description 4
- 239000003981 vehicle Substances 0.000 description 4
- 238000001262 western blot Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 102100029361 Aromatase Human genes 0.000 description 3
- LQVXSNNAFNGRAH-QHCPKHFHSA-N BMS-754807 Chemical compound C([C@@]1(C)C(=O)NC=2C=NC(F)=CC=2)CCN1C(=NN1C=CC=C11)N=C1NC(=NN1)C=C1C1CC1 LQVXSNNAFNGRAH-QHCPKHFHSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 description 3
- 108091006905 Human Serum Albumin Proteins 0.000 description 3
- 102000008100 Human Serum Albumin Human genes 0.000 description 3
- 108060003951 Immunoglobulin Proteins 0.000 description 3
- 239000012828 PI3K inhibitor Substances 0.000 description 3
- 229930012538 Paclitaxel Natural products 0.000 description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 102100029986 Receptor tyrosine-protein kinase erbB-3 Human genes 0.000 description 3
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 description 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 3
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 description 3
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 3
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 3
- 239000005557 antagonist Substances 0.000 description 3
- 230000008901 benefit Effects 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
- 239000010432 diamond Substances 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 102000006602 glyceraldehyde-3-phosphate dehydrogenase Human genes 0.000 description 3
- 108020004445 glyceraldehyde-3-phosphate dehydrogenase Proteins 0.000 description 3
- 108091008039 hormone receptors Proteins 0.000 description 3
- 102000018358 immunoglobulin Human genes 0.000 description 3
- 239000003978 infusion fluid Substances 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 238000007918 intramuscular administration Methods 0.000 description 3
- 239000007951 isotonicity adjuster Substances 0.000 description 3
- 230000000670 limiting effect Effects 0.000 description 3
- 230000007774 longterm Effects 0.000 description 3
- 238000012423 maintenance Methods 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 239000012528 membrane Substances 0.000 description 3
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 description 3
- 229960001592 paclitaxel Drugs 0.000 description 3
- 201000002528 pancreatic cancer Diseases 0.000 description 3
- 229960001972 panitumumab Drugs 0.000 description 3
- 239000012188 paraffin wax Substances 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 210000002966 serum Anatomy 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- 230000004083 survival effect Effects 0.000 description 3
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 3
- 230000004797 therapeutic response Effects 0.000 description 3
- 238000011200 topical administration Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 239000004322 Butylated hydroxytoluene Substances 0.000 description 2
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 description 2
- 102100030013 Endoribonuclease Human genes 0.000 description 2
- 102000056372 ErbB-3 Receptor Human genes 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- 208000012766 Growth delay Diseases 0.000 description 2
- 101100118545 Holotrichia diomphalia EGF-like gene Proteins 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- 239000005517 L01XE01 - Imatinib Substances 0.000 description 2
- 239000002147 L01XE04 - Sunitinib Substances 0.000 description 2
- 229940124647 MEK inhibitor Drugs 0.000 description 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 description 2
- 102000038030 PI3Ks Human genes 0.000 description 2
- 108091007960 PI3Ks Proteins 0.000 description 2
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 102100033237 Pro-epidermal growth factor Human genes 0.000 description 2
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 230000002730 additional effect Effects 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 230000000996 additive effect Effects 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 description 2
- 229960005471 androstenedione Drugs 0.000 description 2
- AEMFNILZOJDQLW-UHFFFAOYSA-N androstenedione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 AEMFNILZOJDQLW-UHFFFAOYSA-N 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 230000000259 anti-tumor effect Effects 0.000 description 2
- 239000003429 antifungal agent Substances 0.000 description 2
- 229940121375 antifungal agent Drugs 0.000 description 2
- 230000004071 biological effect Effects 0.000 description 2
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 2
- 229940095259 butylated hydroxytoluene Drugs 0.000 description 2
- 231100000504 carcinogenesis Toxicity 0.000 description 2
- 230000010261 cell growth Effects 0.000 description 2
- 230000022534 cell killing Effects 0.000 description 2
- 239000013592 cell lysate Substances 0.000 description 2
- 239000006285 cell suspension Substances 0.000 description 2
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- 229950006647 cixutumumab Drugs 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 230000001934 delay Effects 0.000 description 2
- 238000001739 density measurement Methods 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 239000002612 dispersion medium Substances 0.000 description 2
- 238000009261 endocrine therapy Methods 0.000 description 2
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 229950008085 figitumumab Drugs 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 108010084091 heregulin beta1 Proteins 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 description 2
- 238000003018 immunoassay Methods 0.000 description 2
- 238000001361 intraarterial administration Methods 0.000 description 2
- 230000003834 intracellular effect Effects 0.000 description 2
- 229950009645 istiratumab Drugs 0.000 description 2
- 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 description 2
- 229960002367 lasofoxifene Drugs 0.000 description 2
- 239000000787 lecithin Substances 0.000 description 2
- 235000010445 lecithin Nutrition 0.000 description 2
- 229940067606 lecithin Drugs 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 229950008001 matuzumab Drugs 0.000 description 2
- 229950010203 nimotuzumab Drugs 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 230000000069 prophylactic effect Effects 0.000 description 2
- 238000000159 protein binding assay Methods 0.000 description 2
- 238000001959 radiotherapy Methods 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 230000004044 response Effects 0.000 description 2
- 230000007781 signaling event Effects 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 235000000346 sugar Nutrition 0.000 description 2
- 150000008163 sugars Chemical class 0.000 description 2
- 238000002198 surface plasmon resonance spectroscopy Methods 0.000 description 2
- 238000001356 surgical procedure Methods 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000002195 synergetic effect Effects 0.000 description 2
- 230000008685 targeting Effects 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 229960000575 trastuzumab Drugs 0.000 description 2
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 description 2
- QIJRTFXNRTXDIP-UHFFFAOYSA-N (1-carboxy-2-sulfanylethyl)azanium;chloride;hydrate Chemical compound O.Cl.SCC(N)C(O)=O QIJRTFXNRTXDIP-UHFFFAOYSA-N 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N (R)-alpha-Tocopherol Natural products OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 1
- NHBKXEKEPDILRR-UHFFFAOYSA-N 2,3-bis(butanoylsulfanyl)propyl butanoate Chemical compound CCCC(=O)OCC(SC(=O)CCC)CSC(=O)CCC NHBKXEKEPDILRR-UHFFFAOYSA-N 0.000 description 1
- 108010088751 Albumins Proteins 0.000 description 1
- 102000009027 Albumins Human genes 0.000 description 1
- 102100038778 Amphiregulin Human genes 0.000 description 1
- 108010033760 Amphiregulin Proteins 0.000 description 1
- 101100067974 Arabidopsis thaliana POP2 gene Proteins 0.000 description 1
- 206010005949 Bone cancer Diseases 0.000 description 1
- 208000018084 Bone neoplasm Diseases 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 206010055113 Breast cancer metastatic Diseases 0.000 description 1
- 208000005623 Carcinogenesis Diseases 0.000 description 1
- 229920002157 Cellulin Polymers 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 230000004544 DNA amplification Effects 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 102000001301 EGF receptor Human genes 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- 238000012286 ELISA Assay Methods 0.000 description 1
- 239000006145 Eagle's minimal essential medium Substances 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- 206010014759 Endometrial neoplasm Diseases 0.000 description 1
- 102100030323 Epigen Human genes 0.000 description 1
- 108010016906 Epigen Proteins 0.000 description 1
- 101800000155 Epiregulin Proteins 0.000 description 1
- 108010007005 Estrogen Receptor alpha Proteins 0.000 description 1
- 102100038595 Estrogen receptor Human genes 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- 102000006771 Gonadotropins Human genes 0.000 description 1
- 108010086677 Gonadotropins Proteins 0.000 description 1
- 101150054472 HER2 gene Proteins 0.000 description 1
- 239000012981 Hank's balanced salt solution Substances 0.000 description 1
- 101100118549 Homo sapiens EGFR gene Proteins 0.000 description 1
- 101000851181 Homo sapiens Epidermal growth factor receptor Proteins 0.000 description 1
- 101000871708 Homo sapiens Proheparin-binding EGF-like growth factor Proteins 0.000 description 1
- 101001010819 Homo sapiens Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 description 1
- 108010067060 Immunoglobulin Variable Region Proteins 0.000 description 1
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 description 1
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 description 1
- 239000002067 L01XE06 - Dasatinib Substances 0.000 description 1
- 102100020870 La-related protein 6 Human genes 0.000 description 1
- 108050008265 La-related protein 6 Proteins 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 229920004011 Macrolon® Polymers 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 description 1
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 description 1
- 241000699660 Mus musculus Species 0.000 description 1
- 229930193140 Neomycin Natural products 0.000 description 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 1
- 208000035327 Oestrogen receptor positive breast cancer Diseases 0.000 description 1
- 108700020796 Oncogene Proteins 0.000 description 1
- QIUASFSNWYMDFS-NILGECQDSA-N PX-866 Chemical compound CC(=O)O[C@@H]1C[C@]2(C)C(=O)CC[C@H]2C2=C1[C@@]1(C)[C@@H](COC)OC(=O)\C(=C\N(CC=C)CC=C)C1=C(O)C2=O QIUASFSNWYMDFS-NILGECQDSA-N 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 102100025498 Proepiregulin Human genes 0.000 description 1
- 102100033762 Proheparin-binding EGF-like growth factor Human genes 0.000 description 1
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 description 1
- 102100029981 Receptor tyrosine-protein kinase erbB-4 Human genes 0.000 description 1
- 101710100963 Receptor tyrosine-protein kinase erbB-4 Proteins 0.000 description 1
- 108020004511 Recombinant DNA Proteins 0.000 description 1
- 206010070308 Refractory cancer Diseases 0.000 description 1
- 238000011579 SCID mouse model Methods 0.000 description 1
- 101100123851 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) HER1 gene 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
- 102000006747 Transforming Growth Factor alpha Human genes 0.000 description 1
- 101800004564 Transforming growth factor alpha Proteins 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 description 1
- 229940028652 abraxane Drugs 0.000 description 1
- 239000003070 absorption delaying agent Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 210000000577 adipose tissue Anatomy 0.000 description 1
- 229940087168 alpha tocopherol Drugs 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 230000003388 anti-hormonal effect Effects 0.000 description 1
- 238000009175 antibody therapy Methods 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 239000008365 aqueous carrier Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000005899 aromatization reaction Methods 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 235000010385 ascorbyl palmitate Nutrition 0.000 description 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 108010080308 biregulin Proteins 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 201000008274 breast adenocarcinoma Diseases 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- 235000019282 butylated hydroxyanisole Nutrition 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229960004562 carboplatin Drugs 0.000 description 1
- 230000032823 cell division Effects 0.000 description 1
- 210000003855 cell nucleus Anatomy 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 229960004926 chlorobutanol Drugs 0.000 description 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 1
- 229960004316 cisplatin Drugs 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 229960001305 cysteine hydrochloride Drugs 0.000 description 1
- 229960002482 dalotuzumab Drugs 0.000 description 1
- 229960002448 dasatinib Drugs 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 231100000517 death Toxicity 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 229910003460 diamond Inorganic materials 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- UGMCXQCYOVCMTB-UHFFFAOYSA-K dihydroxy(stearato)aluminium Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[Al](O)O UGMCXQCYOVCMTB-UHFFFAOYSA-K 0.000 description 1
- 239000000539 dimer Substances 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 229960003668 docetaxel Drugs 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 231100000371 dose-limiting toxicity Toxicity 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 210000004696 endometrium Anatomy 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 108700020302 erbB-2 Genes Proteins 0.000 description 1
- 229940082789 erbitux Drugs 0.000 description 1
- 239000002834 estrogen receptor modulator Substances 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 210000003722 extracellular fluid Anatomy 0.000 description 1
- 239000012894 fetal calf serum Substances 0.000 description 1
- 230000008014 freezing Effects 0.000 description 1
- 238000007710 freezing Methods 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 238000002695 general anesthesia Methods 0.000 description 1
- 229940080856 gleevec Drugs 0.000 description 1
- 235000019410 glycyrrhizin Nutrition 0.000 description 1
- 239000002622 gonadotropin Substances 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 239000003667 hormone antagonist Substances 0.000 description 1
- 208000027706 hormone receptor-positive breast cancer Diseases 0.000 description 1
- 102000057750 human ERBB3 Human genes 0.000 description 1
- 210000004408 hybridoma Anatomy 0.000 description 1
- 229960003445 idelalisib Drugs 0.000 description 1
- YKLIKGKUANLGSB-HNNXBMFYSA-N idelalisib Chemical compound C1([C@@H](NC=2[C]3N=CN=C3N=CN=2)CC)=NC2=CC=CC(F)=C2C(=O)N1C1=CC=CC=C1 YKLIKGKUANLGSB-HNNXBMFYSA-N 0.000 description 1
- 229960002411 imatinib Drugs 0.000 description 1
- 229940072221 immunoglobulins Drugs 0.000 description 1
- 238000011532 immunohistochemical staining Methods 0.000 description 1
- 238000007901 in situ hybridization Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 230000002601 intratumoral effect Effects 0.000 description 1
- 229940084651 iressa Drugs 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 208000014018 liver neoplasm Diseases 0.000 description 1
- 238000011866 long-term treatment Methods 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 239000006166 lysate Substances 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 108010082117 matrigel Proteins 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 230000001394 metastastic effect Effects 0.000 description 1
- 206010061289 metastatic neoplasm Diseases 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 238000001471 micro-filtration Methods 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 239000003226 mitogen Substances 0.000 description 1
- 230000011278 mitosis Effects 0.000 description 1
- 230000000394 mitotic effect Effects 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- LBWFXVZLPYTWQI-IPOVEDGCSA-N n-[2-(diethylamino)ethyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide;(2s)-2-hydroxybutanedioic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O.CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C LBWFXVZLPYTWQI-IPOVEDGCSA-N 0.000 description 1
- 229960004927 neomycin Drugs 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 102000006255 nuclear receptors Human genes 0.000 description 1
- 108020004017 nuclear receptors Proteins 0.000 description 1
- 102000039446 nucleic acids Human genes 0.000 description 1
- 108020004707 nucleic acids Proteins 0.000 description 1
- 150000007523 nucleic acids Chemical class 0.000 description 1
- 238000011580 nude mouse model Methods 0.000 description 1
- 150000002895 organic esters Chemical class 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 238000009521 phase II clinical trial Methods 0.000 description 1
- MQIHULHVANZSER-XPQLPGEHSA-N phenyl (2e,4e)-hexa-2,4-dienoate Chemical compound C\C=C\C=C\C(=O)OC1=CC=CC=C1 MQIHULHVANZSER-XPQLPGEHSA-N 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 230000003169 placental effect Effects 0.000 description 1
- 229920000515 polycarbonate Polymers 0.000 description 1
- 239000004417 polycarbonate Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
- 150000003077 polyols Chemical class 0.000 description 1
- 238000004393 prognosis Methods 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 239000000473 propyl gallate Substances 0.000 description 1
- 235000010388 propyl gallate Nutrition 0.000 description 1
- 229940075579 propyl gallate Drugs 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 235000019833 protease Nutrition 0.000 description 1
- 230000001698 pyrogenic effect Effects 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 208000016691 refractory malignant neoplasm Diseases 0.000 description 1
- 230000004043 responsiveness Effects 0.000 description 1
- 238000003757 reverse transcription PCR Methods 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 210000003079 salivary gland Anatomy 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000010187 selection method Methods 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 201000000849 skin cancer Diseases 0.000 description 1
- WBHQBSYUUJJSRZ-UHFFFAOYSA-M sodium bisulfate Chemical compound [Na+].OS([O-])(=O)=O WBHQBSYUUJJSRZ-UHFFFAOYSA-M 0.000 description 1
- 229910000342 sodium bisulfate Inorganic materials 0.000 description 1
- 229940100996 sodium bisulfate Drugs 0.000 description 1
- CSMWJXBSXGUPGY-UHFFFAOYSA-L sodium dithionate Chemical compound [Na+].[Na+].[O-]S(=O)(=O)S([O-])(=O)=O CSMWJXBSXGUPGY-UHFFFAOYSA-L 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000012414 sterilization procedure Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 229960001796 sunitinib Drugs 0.000 description 1
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 229940034785 sutent Drugs 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940120982 tarceva Drugs 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
- RCINICONZNJXQF-XAZOAEDWSA-N taxol® Chemical compound O([C@@H]1[C@@]2(CC(C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3(C21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-XAZOAEDWSA-N 0.000 description 1
- 229940063683 taxotere Drugs 0.000 description 1
- 238000011285 therapeutic regimen Methods 0.000 description 1
- AOBORMOPSGHCAX-DGHZZKTQSA-N tocofersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-DGHZZKTQSA-N 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 102000027257 transmembrane receptors Human genes 0.000 description 1
- 108091008578 transmembrane receptors Proteins 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 230000004565 tumor cell growth Effects 0.000 description 1
- 230000005740 tumor formation Effects 0.000 description 1
- 229940094060 tykerb Drugs 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- 235000004835 α-tocopherol Nutrition 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
-
- 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
- A61K31/56—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
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/46—Hybrid immunoglobulins
- C07K16/468—Immunoglobulins having two or more different antigen binding sites, e.g. multifunctional antibodies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161451848P | 2011-03-11 | 2011-03-11 | |
| US61/451,848 | 2011-03-11 | ||
| US201261604281P | 2012-02-28 | 2012-02-28 | |
| US61/604,281 | 2012-02-28 | ||
| PCT/US2012/028792 WO2012125573A2 (en) | 2011-03-11 | 2012-03-12 | Use of inhibitors of egfr-family receptors in the treatment of hormone refractory breast cancers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014508782A true JP2014508782A (ja) | 2014-04-10 |
| JP2014508782A5 JP2014508782A5 (enExample) | 2015-04-30 |
Family
ID=45894680
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013557943A Pending JP2014508782A (ja) | 2011-03-11 | 2012-03-12 | ホルモン不応性乳癌の治療におけるｅｇｆｒファミリー受容体の阻害剤の使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20140134170A1 (enExample) |
| EP (1) | EP2683741A2 (enExample) |
| JP (1) | JP2014508782A (enExample) |
| KR (1) | KR20140044796A (enExample) |
| CN (1) | CN103562226A (enExample) |
| AU (1) | AU2012229147B2 (enExample) |
| BR (1) | BR112013022882A2 (enExample) |
| CA (1) | CA2828075A1 (enExample) |
| EA (1) | EA201300996A1 (enExample) |
| MX (1) | MX2013010379A (enExample) |
| SG (1) | SG192844A1 (enExample) |
| WO (1) | WO2012125573A2 (enExample) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019505555A (ja) * | 2016-02-18 | 2019-02-28 | ウニベルシタ デリィ ストゥディ ディ ジェノバ | がん治療における抗エストロゲン剤有効性の増強のための擬絶食の使用 |
| JP2019142969A (ja) * | 2014-05-08 | 2019-08-29 | シャンハイ インスティテュート オブ プランド パレントフッド リサーチ | アノルドリン組成物および疾患を処置するための方法 |
| JP2020520377A (ja) * | 2017-05-17 | 2020-07-09 | メルス ナムローゼ フェンノートシャップ | 乳癌のためのＥｒｂＢ−２／ＥｒｂＢ−３二重特異性抗体と内分泌療法との組み合わせ |
| US11773170B2 (en) | 2017-08-09 | 2023-10-03 | Merus N.V. | Antibodies that bind EGFR and cMET |
| US11780925B2 (en) | 2017-03-31 | 2023-10-10 | Merus N.V. | ErbB-2 and ErbB3 binding bispecific antibodies for use in the treatment of cells that have an NRG1 fusion gene |
| US11820825B2 (en) | 2014-02-28 | 2023-11-21 | Merus N.V. | Methods of treating a subject having an EGFR-positive and/or ErbB-3-positive tumor |
| US12139548B2 (en) | 2014-02-28 | 2024-11-12 | Merus N.V. | Antibody that binds ErbB-2 and ErbB-3 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20131113T1 (hr) * | 2007-02-16 | 2014-01-17 | Merrimack Pharmaceuticals, Inc. | Protutijela protiv erbb3 i njihova uporaba |
| JP2013522237A (ja) * | 2010-03-11 | 2013-06-13 | メリマック ファーマシューティカルズ インコーポレーティッド | トリプルネガティブおよび基底様乳癌の治療におけるｅｒｂｂ３阻害剤の使用 |
| US9155802B2 (en) | 2010-11-01 | 2015-10-13 | Symphogen A/S | Pan-HER antibody composition |
| WO2013164689A2 (en) | 2012-05-02 | 2013-11-07 | Lantto, Johan | Humanized pan-her antibody compositions |
| WO2015100459A2 (en) | 2013-12-27 | 2015-07-02 | Merrimack Pharmaceuticals, Inc. | Biomarker profiles for predicting outcomes of cancer therapy with erbb3 inhibitors and/or chemotherapies |
| HK1248539A1 (zh) | 2015-04-17 | 2018-10-19 | 梅里麦克制药股份有限公司 | 借助塞里班土单抗的组合治疗 |
| US10184006B2 (en) | 2015-06-04 | 2019-01-22 | Merrimack Pharmaceuticals, Inc. | Biomarkers for predicting outcomes of cancer therapy with ErbB3 inhibitors |
| AU2017235450A1 (en) * | 2016-03-15 | 2018-08-16 | Merrimack Pharmaceuticals, Inc. | Methods for treating ER+, HER2-, HRG+ breast cancer using combination therapies comprising an anti-ErbB3 antibody |
| BR112019007254A2 (pt) | 2016-10-11 | 2019-07-02 | Duke University | tratamento lasofoxifeno de câncer de mama er+ |
| US10624874B2 (en) | 2017-01-10 | 2020-04-21 | Zhejiang Jiachi Development Pharmaceuticals Ltd | Lasofoxifene modulation of membrane-initiated estrogen signals and methods for tumor treatment |
| WO2019185164A1 (en) | 2018-03-29 | 2019-10-03 | Hummingbird Bioscience Holdings Pte. Ltd. | Her3 antigen-binding molecules |
| WO2019199891A1 (en) | 2018-04-10 | 2019-10-17 | Duke University | Lasofoxifene treatment of breast cancer |
| CN115843256A (zh) * | 2020-10-15 | 2023-03-24 | 上海翰森生物医药科技有限公司 | 抗erbb3抗体或其抗原结合片段及其医药用途 |
| GB202116903D0 (en) | 2021-11-18 | 2022-01-05 | Sermonix Pharmaceuticals Inc | Lasofoxifene treatment of aromatase-resistant er+ cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009500005A (ja) * | 2005-06-15 | 2009-01-08 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 二重特異的単鎖Ｆｖ抗体分子およびその使用方法 |
| WO2009126920A2 (en) * | 2008-04-11 | 2009-10-15 | Merrimack Pharmaceuticals, Inc. | Human serum albumin linkers and conjugates thereof |
| WO2010059315A1 (en) * | 2008-11-18 | 2010-05-27 | Merrimack Pharmaceuticals, Inc. | Human serum albumin linkers and conjugates thereof |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5183884A (en) | 1989-12-01 | 1993-02-02 | United States Of America | Dna segment encoding a gene for a receptor related to the epidermal growth factor receptor |
| WO1994004679A1 (en) | 1991-06-14 | 1994-03-03 | Genentech, Inc. | Method for making humanized antibodies |
| EP2258726A1 (en) | 1995-06-14 | 2010-12-08 | The Regents of the University of California | High affinity human antibodies to c-erbB-2 |
| US5968511A (en) | 1996-03-27 | 1999-10-19 | Genentech, Inc. | ErbB3 antibodies |
| US6949245B1 (en) | 1999-06-25 | 2005-09-27 | Genentech, Inc. | Humanized anti-ErbB2 antibodies and treatment with anti-ErbB2 antibodies |
| US7390632B2 (en) | 1999-09-30 | 2008-06-24 | Tumor Biology Investment Group, Inc. | Soluble ErbB3 receptor isoforms |
| US7612042B2 (en) | 2001-05-31 | 2009-11-03 | Tumor Biology Investment Group, Inc. | Methods for inhibiting heregulin and treating cancer |
| EP1283053A1 (en) | 2001-08-09 | 2003-02-12 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Inhibitors of HER3 activity |
| CN100424175C (zh) | 2002-03-26 | 2008-10-08 | 上海泽生科技开发有限公司 | ErbB-3 用于肿瘤治疗的方法和组合物 |
| US7332580B2 (en) | 2002-04-05 | 2008-02-19 | The Regents Of The University Of California | Bispecific single chain Fv antibody molecules and methods of use thereof |
| AR056857A1 (es) | 2005-12-30 | 2007-10-24 | U3 Pharma Ag | Anticuerpos dirigidos hacia her-3 (receptor del factor de crecimiento epidérmico humano-3) y sus usos |
| HRP20131113T1 (hr) * | 2007-02-16 | 2014-01-17 | Merrimack Pharmaceuticals, Inc. | Protutijela protiv erbb3 i njihova uporaba |
| PL2132229T3 (pl) | 2007-03-01 | 2016-12-30 | Kompozycje rekombinowanych przeciwciał anty-receptor czynnika wzrostu naskórka | |
| JP2010526797A (ja) | 2007-05-11 | 2010-08-05 | エンゾン ファーマシューティカルズ，インコーポレーテッド | Ｈｅｒ３のモジュレーションのためのｒｎａアンタゴニスト化合物 |
| BRPI0917871A2 (pt) | 2008-08-15 | 2017-06-20 | Merrimack Pharmaceuticals Inc | agente terapêutico anti-erbb3 para uso em terapia de um tumor, métodos para predizer responsividade de um tumor de um agente terapêutco anti-erbb3, para selecionar terapia anti-erbb3 para um paciente, para predizer a resposta de células ao tratamento com um agente terapêutico, para identificar um biomarcador, e para evitar administração de uma droga para câncer anti-erbb3, e, kit para predizer a resposta das células ao tratamento com um agente terapêutico |
| CN102356092B (zh) | 2009-03-20 | 2014-11-05 | 霍夫曼-拉罗奇有限公司 | 双特异性抗-her抗体 |
| US8362215B2 (en) | 2009-04-29 | 2013-01-29 | Trellis Bioscience, Llc | Antibodies immunoreactive with heregulin-coupled HER3 |
| CA2777242A1 (en) * | 2009-10-14 | 2011-04-21 | Merrimack Pharmaceuticals, Inc. | Bispecific binding agents targeting igf-1r and erbb3 signalling and uses thereof |
| JP2013522237A (ja) * | 2010-03-11 | 2013-06-13 | メリマック ファーマシューティカルズ インコーポレーティッド | トリプルネガティブおよび基底様乳癌の治療におけるｅｒｂｂ３阻害剤の使用 |
| WO2011136911A2 (en) | 2010-04-09 | 2011-11-03 | Aveo Pharmaceuticals, Inc. | Anti-erbb3 antibodies |
| UY33498A (es) * | 2010-07-09 | 2013-01-03 | Sanofi Aventis | Combinaciones de inhibidores de quinasas para el tratamiento de cancer |
-
2012
- 2012-03-12 JP JP2013557943A patent/JP2014508782A/ja active Pending
- 2012-03-12 EP EP12711080.7A patent/EP2683741A2/en not_active Withdrawn
- 2012-03-12 MX MX2013010379A patent/MX2013010379A/es unknown
- 2012-03-12 SG SG2013062856A patent/SG192844A1/en unknown
- 2012-03-12 BR BR112013022882A patent/BR112013022882A2/pt not_active IP Right Cessation
- 2012-03-12 WO PCT/US2012/028792 patent/WO2012125573A2/en not_active Ceased
- 2012-03-12 EA EA201300996A patent/EA201300996A1/ru unknown
- 2012-03-12 CN CN201280012969.XA patent/CN103562226A/zh active Pending
- 2012-03-12 AU AU2012229147A patent/AU2012229147B2/en not_active Ceased
- 2012-03-12 CA CA2828075A patent/CA2828075A1/en not_active Abandoned
- 2012-03-12 US US14/004,598 patent/US20140134170A1/en not_active Abandoned
- 2012-03-12 KR KR1020137026392A patent/KR20140044796A/ko not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009500005A (ja) * | 2005-06-15 | 2009-01-08 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 二重特異的単鎖Ｆｖ抗体分子およびその使用方法 |
| WO2009126920A2 (en) * | 2008-04-11 | 2009-10-15 | Merrimack Pharmaceuticals, Inc. | Human serum albumin linkers and conjugates thereof |
| WO2010059315A1 (en) * | 2008-11-18 | 2010-05-27 | Merrimack Pharmaceuticals, Inc. | Human serum albumin linkers and conjugates thereof |
Non-Patent Citations (2)
| Title |
|---|
| JPN5014005170; ＮＩＥ ＬＩＮ: 'ＥＦＦＩＣＡＣＹ ＯＦ ＭＭ１２１ ＩＮ ＥＲ＋ ＡＮＤ ＴＲＩＰＬＥ ＮＥＧＡＴＩＶＥ ＢＲＥＡＳＴ ＣＡＮＣＥＲ ＳＴＵＤＩＥＳ' ＰＲＯＣＥＥＤＩＮＧＳ ＯＦ ＴＨＥ ＡＮＮＵＡＬ ＭＥＥＴＩＮＧ ＯＦ ＴＨＥ ＡＭＥＲＩＣＡＮ ＡＳＳＯＣＩＡＴＩＯＮ ＦＯＲ ＣＡＮＣＥＲ ＲＥＳＥＡＲＣＨ Ｖ５１, 20100417, Ｐ４３６, ＡＭＥＲＩＣＡＮ ＡＳＳＯＣＩＡＴＩＯＮ ＦＯＲ ＣＡＮＣＥＲ ＲＥＳＥＡＲＣＨ * |
| JPN6015051314; ＰＲＡＲ，Ａ． ａｎｄ ＢＡＳＥＬＧＡ， Ｊ．: Ｎａｔ Ｃｌｉｎ Ｐｒａｃｔ Ｏｎｃｏｌ Ｖｏｌ．５， Ｎｏ．９, 2008, ｐ．５３１-４２ * |
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11820825B2 (en) | 2014-02-28 | 2023-11-21 | Merus N.V. | Methods of treating a subject having an EGFR-positive and/or ErbB-3-positive tumor |
| US12139548B2 (en) | 2014-02-28 | 2024-11-12 | Merus N.V. | Antibody that binds ErbB-2 and ErbB-3 |
| US10857158B2 (en) | 2014-05-08 | 2020-12-08 | Zhejiang Jiachi Development Pharmaceuticals Ltd | Anordrin compositions and methods for treating diseases |
| US11911397B2 (en) | 2014-05-08 | 2024-02-27 | Zhejiang Jiachi Development Pharmaceuticals Ltd | Anordrin compositions and methods for treating diseases |
| JP2019142969A (ja) * | 2014-05-08 | 2019-08-29 | シャンハイ インスティテュート オブ プランド パレントフッド リサーチ | アノルドリン組成物および疾患を処置するための方法 |
| JP2019505555A (ja) * | 2016-02-18 | 2019-02-28 | ウニベルシタ デリィ ストゥディ ディ ジェノバ | がん治療における抗エストロゲン剤有効性の増強のための擬絶食の使用 |
| JP7071272B2 (ja) | 2016-02-18 | 2022-05-18 | ウニベルシタ デリィ ストゥディ ディ ジェノバ | がん治療における抗エストロゲン剤有効性の増強のための擬絶食の使用 |
| US11780925B2 (en) | 2017-03-31 | 2023-10-10 | Merus N.V. | ErbB-2 and ErbB3 binding bispecific antibodies for use in the treatment of cells that have an NRG1 fusion gene |
| US12247078B2 (en) | 2017-03-31 | 2025-03-11 | Merus N.V. | ERBB-2 and ERBB-3 binding bispecific antibodies for use in the treatment of cells that have an NRG1 fusion gene |
| JP2023085422A (ja) * | 2017-05-17 | 2023-06-20 | メルス ナムローゼ フェンノートシャップ | 乳癌のためのＥｒｂＢ－２／ＥｒｂＢ－３二重特異性抗体と内分泌療法との組み合わせ |
| JP7296891B2 (ja) | 2017-05-17 | 2023-06-23 | メルス ナムローゼ フェンノートシャップ | 乳癌のためのＥｒｂＢ－２／ＥｒｂＢ－３二重特異性抗体と内分泌療法との組み合わせ |
| JP2020520377A (ja) * | 2017-05-17 | 2020-07-09 | メルス ナムローゼ フェンノートシャップ | 乳癌のためのＥｒｂＢ−２／ＥｒｂＢ−３二重特異性抗体と内分泌療法との組み合わせ |
| US12195551B2 (en) | 2017-05-17 | 2025-01-14 | Merus N.V. | Combination of an ErbB-2/ErbB-3 bispecific antibody with endocrine therapy for breast cancer |
| US11773170B2 (en) | 2017-08-09 | 2023-10-03 | Merus N.V. | Antibodies that bind EGFR and cMET |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20140044796A (ko) | 2014-04-15 |
| BR112013022882A2 (pt) | 2016-12-20 |
| SG192844A1 (en) | 2013-09-30 |
| MX2013010379A (es) | 2014-03-27 |
| WO2012125573A2 (en) | 2012-09-20 |
| EP2683741A2 (en) | 2014-01-15 |
| AU2012229147B2 (en) | 2015-12-24 |
| AU2012229147A1 (en) | 2013-03-14 |
| EA201300996A1 (ru) | 2014-01-30 |
| NZ614427A (en) | 2015-08-28 |
| CA2828075A1 (en) | 2012-09-20 |
| WO2012125573A3 (en) | 2012-12-27 |
| CN103562226A (zh) | 2014-02-05 |
| US20140134170A1 (en) | 2014-05-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6185102B2 (ja) | トリプルネガティブおよび基底様乳癌の治療におけるｅｒｂｂ３阻害剤の使用 | |
| AU2012229147B2 (en) | Use of inhibitors of EGFR-family receptors in the treatment of hormone refractory breast cancers | |
| KR20140023921A (ko) | ＥｒｂＢ 경로 저해제들에 대한 저항성을 극복하는 방법 | |
| CN110036030A (zh) | 癌症的组合疗法 | |
| JP2014527035A (ja) | 婦人科悪性腫瘍を治療するためのパクリタキセルとの組み合わせの抗ＥｒｂＢ３抗体 | |
| WO2022223006A1 (zh) | 抗pd-1抗体联合一线化疗治疗晚期非小细胞肺癌的用途 | |
| US20240317884A1 (en) | Method for allowing immune cells infiltration in tumors | |
| NZ614427B2 (en) | Use of inhibitors of egfr-family receptors in the treatment of hormone refractory breast cancers | |
| HK1174254B (en) | Use of erbb3 inhibitors in the treatment of triple negative breast cancer |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20150310 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20150310 |
|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7424 Effective date: 20150410 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20151221 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20160523 |