JP2003528919A - 抵抗性乳癌の治療におけるフルベストラントの使用 - Google Patents
抵抗性乳癌の治療におけるフルベストラントの使用Info
- Publication number
- JP2003528919A JP2003528919A JP2001572110A JP2001572110A JP2003528919A JP 2003528919 A JP2003528919 A JP 2003528919A JP 2001572110 A JP2001572110 A JP 2001572110A JP 2001572110 A JP2001572110 A JP 2001572110A JP 2003528919 A JP2003528919 A JP 2003528919A
- Authority
- JP
- Japan
- Prior art keywords
- treatment
- fulvestrant
- breast cancer
- patients
- lesions
- 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
- 238000011282 treatment Methods 0.000 title claims abstract description 85
- 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 title claims abstract description 55
- 229960002258 fulvestrant Drugs 0.000 title claims abstract description 55
- 206010006187 Breast cancer Diseases 0.000 title claims abstract description 45
- 208000026310 Breast neoplasm Diseases 0.000 title claims abstract description 36
- 239000003886 aromatase inhibitor Substances 0.000 claims abstract description 22
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims abstract description 18
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims abstract description 16
- 229940122815 Aromatase inhibitor Drugs 0.000 claims abstract description 14
- 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 29
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical group N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 17
- 229960002932 anastrozole Drugs 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 15
- 229960001603 tamoxifen Drugs 0.000 claims description 14
- 238000002360 preparation method Methods 0.000 claims description 3
- 230000003902 lesion Effects 0.000 description 52
- 230000004044 response Effects 0.000 description 34
- 206010028980 Neoplasm Diseases 0.000 description 33
- 239000000203 mixture Substances 0.000 description 22
- 201000010099 disease Diseases 0.000 description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 21
- 238000011156 evaluation Methods 0.000 description 21
- 206010061818 Disease progression Diseases 0.000 description 20
- 230000005750 disease progression Effects 0.000 description 20
- 206010061728 Bone lesion Diseases 0.000 description 18
- 238000009472 formulation Methods 0.000 description 18
- 238000002591 computed tomography Methods 0.000 description 16
- 238000002560 therapeutic procedure Methods 0.000 description 16
- 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 description 15
- 239000008194 pharmaceutical composition Substances 0.000 description 15
- 229960003881 letrozole Drugs 0.000 description 14
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 13
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 13
- 229960003437 aminoglutethimide Drugs 0.000 description 13
- ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 description 13
- 238000007469 bone scintigraphy Methods 0.000 description 13
- 102000015694 estrogen receptors Human genes 0.000 description 13
- 108010038795 estrogen receptors Proteins 0.000 description 13
- 238000002347 injection Methods 0.000 description 12
- 239000007924 injection Substances 0.000 description 12
- 230000036961 partial effect Effects 0.000 description 12
- 239000000262 estrogen Substances 0.000 description 11
- 229940011871 estrogen Drugs 0.000 description 11
- 238000002595 magnetic resonance imaging Methods 0.000 description 11
- 229940079593 drug Drugs 0.000 description 10
- 239000000328 estrogen antagonist Substances 0.000 description 10
- JBTWLSYIZRCDFO-UHFFFAOYSA-N ethyl methyl carbonate Chemical compound CCOC(=O)OC JBTWLSYIZRCDFO-UHFFFAOYSA-N 0.000 description 10
- 229940046836 anti-estrogen Drugs 0.000 description 9
- 230000001833 anti-estrogenic effect Effects 0.000 description 9
- 230000000694 effects Effects 0.000 description 9
- 229940122361 Bisphosphonate Drugs 0.000 description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 229940046844 aromatase inhibitors Drugs 0.000 description 8
- 230000008901 benefit Effects 0.000 description 8
- 150000004663 bisphosphonates Chemical class 0.000 description 8
- 238000006243 chemical reaction Methods 0.000 description 8
- 238000012216 screening Methods 0.000 description 8
- 230000002411 adverse Effects 0.000 description 7
- 230000002018 overexpression Effects 0.000 description 7
- 208000037821 progressive disease Diseases 0.000 description 7
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 6
- 108700012941 GNRH1 Proteins 0.000 description 6
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 6
- 238000001959 radiotherapy Methods 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- 101100314454 Caenorhabditis elegans tra-1 gene Proteins 0.000 description 5
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 description 5
- 206010066901 Treatment failure Diseases 0.000 description 5
- 201000011510 cancer Diseases 0.000 description 5
- 210000000038 chest Anatomy 0.000 description 5
- 229940088597 hormone Drugs 0.000 description 5
- 239000005556 hormone Substances 0.000 description 5
- 238000003364 immunohistochemistry Methods 0.000 description 5
- 230000007170 pathology Effects 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 230000009885 systemic effect Effects 0.000 description 5
- -1 4,4,5,5,5-pentafluoropentylsulfinyl Chemical group 0.000 description 4
- 238000004458 analytical method Methods 0.000 description 4
- 230000000259 anti-tumor effect Effects 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 4
- 230000003054 hormonal effect Effects 0.000 description 4
- 210000004185 liver Anatomy 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- 206010061289 metastatic neoplasm Diseases 0.000 description 4
- 238000009806 oophorectomy Methods 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 229960003656 ricinoleic acid Drugs 0.000 description 4
- FEUQNCSVHBHROZ-UHFFFAOYSA-N ricinoleic acid Natural products CCCCCCC(O[Si](C)(C)C)CC=CCCCCCCCC(=O)OC FEUQNCSVHBHROZ-UHFFFAOYSA-N 0.000 description 4
- 238000002604 ultrasonography Methods 0.000 description 4
- 102100036475 Alanine aminotransferase 1 Human genes 0.000 description 3
- 108010082126 Alanine transaminase Proteins 0.000 description 3
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 3
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 3
- 208000020084 Bone disease Diseases 0.000 description 3
- 206010006002 Bone pain Diseases 0.000 description 3
- 239000003146 anticoagulant agent Substances 0.000 description 3
- 229940127219 anticoagulant drug Drugs 0.000 description 3
- 229960002903 benzyl benzoate Drugs 0.000 description 3
- 230000036772 blood pressure Effects 0.000 description 3
- 210000000988 bone and bone Anatomy 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 238000002648 combination therapy Methods 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 230000018109 developmental process Effects 0.000 description 3
- 230000012010 growth Effects 0.000 description 3
- 238000007918 intramuscular administration Methods 0.000 description 3
- 238000010255 intramuscular injection Methods 0.000 description 3
- 239000007927 intramuscular injection Substances 0.000 description 3
- 210000004072 lung Anatomy 0.000 description 3
- 235000018102 proteins Nutrition 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 230000009257 reactivity Effects 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 230000003637 steroidlike Effects 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 208000030507 AIDS Diseases 0.000 description 2
- 206010055113 Breast cancer metastatic Diseases 0.000 description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- 206010053567 Coagulopathies Diseases 0.000 description 2
- 208000032843 Hemorrhage Diseases 0.000 description 2
- 206010020880 Hypertrophy Diseases 0.000 description 2
- 206010027476 Metastases Diseases 0.000 description 2
- 206010027457 Metastases to liver Diseases 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 2
- 208000005250 Spontaneous Fractures Diseases 0.000 description 2
- 238000009098 adjuvant therapy Methods 0.000 description 2
- 230000001270 agonistic effect Effects 0.000 description 2
- 229940035676 analgesics Drugs 0.000 description 2
- 239000000730 antalgic agent Substances 0.000 description 2
- 238000013176 antiplatelet therapy Methods 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 235000019445 benzyl alcohol Nutrition 0.000 description 2
- 230000002146 bilateral effect Effects 0.000 description 2
- 208000034158 bleeding Diseases 0.000 description 2
- 230000000740 bleeding effect Effects 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000011976 chest X-ray Methods 0.000 description 2
- 230000035602 clotting Effects 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
- 230000001086 cytosolic effect Effects 0.000 description 2
- 230000034994 death Effects 0.000 description 2
- 231100000517 death Toxicity 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 230000006866 deterioration Effects 0.000 description 2
- 238000009164 estrogen replacement therapy Methods 0.000 description 2
- 238000001794 hormone therapy Methods 0.000 description 2
- 238000009396 hybridization Methods 0.000 description 2
- 230000000155 isotopic effect Effects 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 230000007434 lytic lesion Effects 0.000 description 2
- 230000036210 malignancy Effects 0.000 description 2
- 230000001394 metastastic effect Effects 0.000 description 2
- 230000002611 ovarian Effects 0.000 description 2
- 239000000583 progesterone congener Substances 0.000 description 2
- 102000003998 progesterone receptors Human genes 0.000 description 2
- 108090000468 progesterone receptors Proteins 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 229940066675 ricinoleate Drugs 0.000 description 2
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 210000004872 soft tissue Anatomy 0.000 description 2
- 238000013517 stratification Methods 0.000 description 2
- 238000009121 systemic therapy Methods 0.000 description 2
- 238000010998 test method Methods 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 description 1
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 1
- 108091032973 (ribonucleotides)n+m Proteins 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
- AWGBKZRMLNVLAF-UHFFFAOYSA-N 3,5-dibromo-n,2-dihydroxybenzamide Chemical compound ONC(=O)C1=CC(Br)=CC(Br)=C1O AWGBKZRMLNVLAF-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 102000009027 Albumins Human genes 0.000 description 1
- 108010088751 Albumins Proteins 0.000 description 1
- 208000007848 Alcoholism Diseases 0.000 description 1
- 201000000736 Amenorrhea Diseases 0.000 description 1
- 206010001928 Amenorrhoea Diseases 0.000 description 1
- 206010003445 Ascites Diseases 0.000 description 1
- 108010003415 Aspartate Aminotransferases Proteins 0.000 description 1
- 102000004625 Aspartate Aminotransferases Human genes 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010008479 Chest Pain Diseases 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 230000004544 DNA amplification Effects 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- 102000001554 Hemoglobins Human genes 0.000 description 1
- 108010054147 Hemoglobins Proteins 0.000 description 1
- 206010019799 Hepatitis viral Diseases 0.000 description 1
- 101000889443 Homo sapiens Trefoil factor 1 Proteins 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 241000725303 Human immunodeficiency virus Species 0.000 description 1
- 206010025102 Lung infiltration Diseases 0.000 description 1
- 206010025282 Lymphoedema Diseases 0.000 description 1
- 241000489861 Maximus Species 0.000 description 1
- 206010027452 Metastases to bone Diseases 0.000 description 1
- 206010027458 Metastases to lung Diseases 0.000 description 1
- 206010067868 Skin mass Diseases 0.000 description 1
- 208000001871 Tachycardia Diseases 0.000 description 1
- 238000008050 Total Bilirubin Reagent Methods 0.000 description 1
- 102100039175 Trefoil factor 1 Human genes 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 210000004404 adrenal cortex Anatomy 0.000 description 1
- 230000008484 agonism Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 201000007930 alcohol dependence Diseases 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 231100000540 amenorrhea Toxicity 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940078010 arimidex Drugs 0.000 description 1
- 238000004820 blood count Methods 0.000 description 1
- 238000009534 blood test Methods 0.000 description 1
- 210000001185 bone marrow Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000000481 breast Anatomy 0.000 description 1
- 230000002308 calcification Effects 0.000 description 1
- 230000002612 cardiopulmonary effect Effects 0.000 description 1
- 230000001364 causal effect Effects 0.000 description 1
- 210000003679 cervix uteri Anatomy 0.000 description 1
- 230000009850 completed effect Effects 0.000 description 1
- 230000001010 compromised effect Effects 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 229940109239 creatinine Drugs 0.000 description 1
- 229940127089 cytotoxic agent Drugs 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 229940000406 drug candidate Drugs 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 238000009261 endocrine therapy Methods 0.000 description 1
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- 230000001076 estrogenic effect Effects 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
- 230000005713 exacerbation Effects 0.000 description 1
- 230000007717 exclusion Effects 0.000 description 1
- 229940087861 faslodex Drugs 0.000 description 1
- 229940087476 femara Drugs 0.000 description 1
- VWUXBMIQPBEWFH-LQKBAPIOSA-N fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4C3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-LQKBAPIOSA-N 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 238000005534 hematocrit Methods 0.000 description 1
- 230000002008 hemorrhagic effect Effects 0.000 description 1
- 231100000753 hepatic injury Toxicity 0.000 description 1
- 210000001624 hip Anatomy 0.000 description 1
- 229940125697 hormonal agent Drugs 0.000 description 1
- 238000002991 immunohistochemical analysis Methods 0.000 description 1
- 238000011532 immunohistochemical staining Methods 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 201000004933 in situ carcinoma Diseases 0.000 description 1
- 238000007901 in situ hybridization Methods 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 229940074928 isopropyl myristate Drugs 0.000 description 1
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 description 1
- 229940075495 isopropyl palmitate Drugs 0.000 description 1
- 229960004125 ketoconazole Drugs 0.000 description 1
- 210000000265 leukocyte Anatomy 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 238000011866 long-term treatment Methods 0.000 description 1
- 210000001165 lymph node Anatomy 0.000 description 1
- 206010025226 lymphangitis Diseases 0.000 description 1
- 208000002502 lymphedema Diseases 0.000 description 1
- 230000002101 lytic effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 210000005015 mediastinal lymph node Anatomy 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000005906 menstruation Effects 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- 210000000440 neutrophil Anatomy 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 229940085033 nolvadex Drugs 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000001582 osteoblastic effect Effects 0.000 description 1
- 230000000010 osteolytic effect Effects 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 210000004197 pelvis Anatomy 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000009546 plain radiography Methods 0.000 description 1
- 238000003752 polymerase chain reaction Methods 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 229960005205 prednisolone Drugs 0.000 description 1
- 238000004393 prognosis Methods 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 230000004202 respiratory function Effects 0.000 description 1
- WBHHMMIMDMUBKC-XLNAKTSKSA-N ricinelaidic acid Chemical compound CCCCCC[C@@H](O)C\C=C\CCCCCCCC(O)=O WBHHMMIMDMUBKC-XLNAKTSKSA-N 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000000405 serological effect Effects 0.000 description 1
- 208000020352 skin basal cell carcinoma Diseases 0.000 description 1
- 201000010106 skin squamous cell carcinoma Diseases 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 230000006794 tachycardia Effects 0.000 description 1
- WZDGZWOAQTVYBX-XOINTXKNSA-N tibolone Chemical compound C([C@@H]12)C[C@]3(C)[C@@](C#C)(O)CC[C@H]3[C@@H]1[C@H](C)CC1=C2CCC(=O)C1 WZDGZWOAQTVYBX-XOINTXKNSA-N 0.000 description 1
- 229960001023 tibolone Drugs 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
- 201000001862 viral hepatitis Diseases 0.000 description 1
- 208000037911 visceral disease Diseases 0.000 description 1
- 230000008673 vomiting Effects 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
- A61K31/56—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
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0008172.9 | 2000-04-05 | ||
| GBGB0008172.9A GB0008172D0 (en) | 2000-04-05 | 2000-04-05 | Therapy |
| PCT/GB2001/001500 WO2001074366A1 (en) | 2000-04-05 | 2001-04-02 | Use of fulvestrant in the treatment of resistant breast cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003528919A true JP2003528919A (ja) | 2003-09-30 |
| JP2003528919A5 JP2003528919A5 (enExample) | 2008-05-08 |
Family
ID=9889101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001572110A Pending JP2003528919A (ja) | 2000-04-05 | 2001-04-02 | 抵抗性乳癌の治療におけるフルベストラントの使用 |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US20030158166A1 (enExample) |
| EP (2) | EP1272195B1 (enExample) |
| JP (1) | JP2003528919A (enExample) |
| KR (1) | KR100757764B1 (enExample) |
| CN (1) | CN1431905A (enExample) |
| AT (1) | ATE306270T1 (enExample) |
| AU (2) | AU4437201A (enExample) |
| BR (1) | BR0109789A (enExample) |
| CA (1) | CA2403608A1 (enExample) |
| CH (1) | CH1272195H1 (enExample) |
| CZ (1) | CZ303096B6 (enExample) |
| DE (1) | DE60113975T2 (enExample) |
| DK (1) | DK1272195T3 (enExample) |
| EE (1) | EE05026B1 (enExample) |
| ES (1) | ES2248300T3 (enExample) |
| GB (1) | GB0008172D0 (enExample) |
| HU (1) | HU230064B1 (enExample) |
| IL (2) | IL151932A0 (enExample) |
| IS (1) | IS2869B (enExample) |
| MX (1) | MXPA02009744A (enExample) |
| NO (1) | NO329949B1 (enExample) |
| NZ (1) | NZ539603A (enExample) |
| PL (1) | PL201175B1 (enExample) |
| RU (1) | RU2265438C2 (enExample) |
| SK (1) | SK287779B6 (enExample) |
| UA (1) | UA80388C2 (enExample) |
| WO (1) | WO2001074366A1 (enExample) |
| ZA (1) | ZA200207538B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021525278A (ja) * | 2018-05-24 | 2021-09-24 | カシーヴ バイオサイエンシズ，リミテッド・ライアビリティ・カンパニー | フルベストラントのプロドラッグ |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0116620D0 (en) * | 2001-07-07 | 2001-08-29 | Astrazeneca Ab | Formulation |
| EP1406662A1 (en) * | 2001-07-07 | 2004-04-14 | AstraZeneca AB | Pharmaceutical formulation for the intramuscular administration of fulvestrant |
| EP1623713A1 (en) * | 2004-07-09 | 2006-02-08 | Proskelia SAS | Cominations of pure anti-estrogen with aromatase inhibitors |
| US8557863B2 (en) * | 2005-09-27 | 2013-10-15 | Robert Benson Aylor | Suppression and prevention of tumors |
| WO2007062093A2 (en) * | 2005-11-22 | 2007-05-31 | Incyte Corporation | Combination therapy for the treatment of cancer comprising a metalloprotease inhibitor |
| US7910108B2 (en) * | 2006-06-05 | 2011-03-22 | Incyte Corporation | Sheddase inhibitors combined with CD30-binding immunotherapeutics for the treatment of CD30 positive diseases |
| RU2013154048A (ru) * | 2011-05-09 | 2015-06-20 | Юниверсити Оф Вирджиния Пэтент Фаундейшн | Композиции и способы лечения рака |
| CA2836831C (en) | 2011-05-20 | 2015-06-02 | Capital, Business Y Gestion De Finanzas S.L. | Pharmaceutical composition |
| EP3092027A4 (en) * | 2014-01-10 | 2017-09-06 | Atossa Genetics Inc. | Transpapillary methods and compositions for diagnosing and treating breast conditions |
| US9421264B2 (en) * | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| EP3681491A4 (en) | 2017-09-11 | 2021-06-30 | Atossa Therapeutics, Inc. | PROCESS FOR MANUFACTURING AND USE OF ENDOXIFES |
| WO2021003433A1 (en) | 2019-07-03 | 2021-01-07 | Atossa Therapeutics, Inc. | Sustained release compositions of endoxifen |
| CA3210276A1 (en) * | 2020-02-29 | 2021-09-02 | Frances E. Carr | Use of thyromimetics for the treatment of cancer |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6362371B1 (en) * | 1998-06-08 | 2002-03-26 | Advanced Medicine, Inc. | β2- adrenergic receptor agonists |
| US6465445B1 (en) * | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
-
2000
- 2000-04-05 GB GBGB0008172.9A patent/GB0008172D0/en not_active Ceased
-
2001
- 2001-02-04 UA UA2002118734A patent/UA80388C2/uk unknown
- 2001-04-02 WO PCT/GB2001/001500 patent/WO2001074366A1/en not_active Ceased
- 2001-04-02 AU AU4437201A patent/AU4437201A/xx active Pending
- 2001-04-02 DK DK01917289T patent/DK1272195T3/da active
- 2001-04-02 US US10/240,656 patent/US20030158166A1/en not_active Abandoned
- 2001-04-02 ES ES01917289T patent/ES2248300T3/es not_active Expired - Lifetime
- 2001-04-02 JP JP2001572110A patent/JP2003528919A/ja active Pending
- 2001-04-02 HU HU0300339A patent/HU230064B1/hu unknown
- 2001-04-02 RU RU2002129355/14A patent/RU2265438C2/ru active
- 2001-04-02 KR KR1020027013366A patent/KR100757764B1/ko not_active Expired - Lifetime
- 2001-04-02 IL IL15193201A patent/IL151932A0/xx active IP Right Grant
- 2001-04-02 CN CN01810539A patent/CN1431905A/zh active Pending
- 2001-04-02 DE DE60113975T patent/DE60113975T2/de not_active Expired - Lifetime
- 2001-04-02 CA CA002403608A patent/CA2403608A1/en not_active Abandoned
- 2001-04-02 CZ CZ20023309A patent/CZ303096B6/cs not_active IP Right Cessation
- 2001-04-02 BR BR0109789-0A patent/BR0109789A/pt not_active Application Discontinuation
- 2001-04-02 AU AU2001244372A patent/AU2001244372B2/en not_active Expired
- 2001-04-02 CH CH01917289T patent/CH1272195H1/de unknown
- 2001-04-02 SK SK1429-2002A patent/SK287779B6/sk not_active IP Right Cessation
- 2001-04-02 EP EP01917289A patent/EP1272195B1/en not_active Expired - Lifetime
- 2001-04-02 NZ NZ539603A patent/NZ539603A/en not_active IP Right Cessation
- 2001-04-02 PL PL357936A patent/PL201175B1/pl unknown
- 2001-04-02 EP EP05007561A patent/EP1586323A1/en not_active Withdrawn
- 2001-04-02 AT AT01917289T patent/ATE306270T1/de active
- 2001-04-02 MX MXPA02009744A patent/MXPA02009744A/es active IP Right Grant
- 2001-04-02 EE EEP200200574A patent/EE05026B1/xx unknown
-
2002
- 2002-09-19 ZA ZA200207538A patent/ZA200207538B/en unknown
- 2002-09-25 IL IL151932A patent/IL151932A/en unknown
- 2002-10-01 IS IS6576A patent/IS2869B/is unknown
- 2002-10-02 NO NO20024735A patent/NO329949B1/no not_active IP Right Cessation
-
2010
- 2010-09-30 US US12/895,369 patent/US20110183949A1/en not_active Abandoned
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021525278A (ja) * | 2018-05-24 | 2021-09-24 | カシーヴ バイオサイエンシズ，リミテッド・ライアビリティ・カンパニー | フルベストラントのプロドラッグ |
| JP7384903B2 (ja) | 2018-05-24 | 2023-11-21 | ケーアイ ファーマシューティカルズ，リミテッド・ライアビリティ・カンパニー | フルベストラントのプロドラッグ |
| JP2024016210A (ja) * | 2018-05-24 | 2024-02-06 | ケーアイ ファーマシューティカルズ，リミテッド・ライアビリティ・カンパニー | フルベストラントのプロドラッグ |
| JP7653092B2 (ja) | 2018-05-24 | 2025-03-28 | シヴァンカ リサーチ リミテッド ライアビリティ カンパニー | フルベストラントのプロドラッグ |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20110183949A1 (en) | Use of Fulvestrant in the Treatment of Resistant Breast Cancer | |
| Paridaens et al. | Mature results of a randomized phase II multicenter study of exemestane versus tamoxifen as first-line hormone therapy for postmenopausal women with metastatic breast cancer | |
| Bajetta et al. | Double-blind, randomised, multicentre endocrine trial comparing two letrozole doses, in postmenopausal breast cancer patients | |
| Baumann et al. | Estrogen receptor modulators and down regulators: Optimal use in postmenopausal women with breast cancer | |
| AU2001244372A1 (en) | Use of fulvestrant in the treatment of resistant breast cancer | |
| JP2023504436A (ja) | 乳がんの治療のための併用療法 | |
| RU2320339C2 (ru) | Применение анастрозола для лечения женщин в постклимактерическом периоде, которые страдают ранним раком молочной железы | |
| US20250186393A1 (en) | Treatment of breast cancer with amcenestrant | |
| Izuo et al. | Oral high-dose medroxyprogesterone acetate (MAP) in treatment of advanced breast cancer: A preliminary report of clinical and experimental studies | |
| Barnadas et al. | An overview of letrozole in postmenopausal women with hormone-responsive breast cancer | |
| Williams et al. | Multicenter study of trilostane: a new hormonal agent in advanced postmenopausal breast cancer. | |
| HK1081842A (en) | Use of fulvestrant in the treatment of resistant breast cancer | |
| HK1051498B (en) | Use of fulvestrant in the treatment of resistant breast cancer | |
| US20050080062A1 (en) | Breast cancer treatment regimen | |
| KR20260006644A (ko) | 유방암 치료에 사용하기 위한 카피바서티브, cdk4/6 억제제 및 풀베스트란트의 조합 | |
| VICARIO et al. | Clinical and endocrine effects of megestrol-acetate in women with pretreated advanced breast-cancer | |
| i Alsina et al. | Selective Estrogen Receptor Modulators. Antonio Cano | |
| Genazzani et al. | 2004 OUTLOOK ON HORMONE REPLACEMENT THERAPY |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20080324 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20080324 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20110907 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20111206 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20111207 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20111213 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20111214 |
|
| RD02 | Notification of acceptance of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7422 Effective date: 20111216 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20120508 |