KR100802366B1 - 풀베스트란트 제제 - Google Patents
풀베스트란트 제제 Download PDFInfo
- Publication number
- KR100802366B1 KR100802366B1 KR1020027008855A KR20027008855A KR100802366B1 KR 100802366 B1 KR100802366 B1 KR 100802366B1 KR 1020027008855 A KR1020027008855 A KR 1020027008855A KR 20027008855 A KR20027008855 A KR 20027008855A KR 100802366 B1 KR100802366 B1 KR 100802366B1
- Authority
- KR
- South Korea
- Prior art keywords
- formulation
- pharmaceutically acceptable
- fulvestrant
- volume
- pharmaceutical formulation
- 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.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 110
- 238000009472 formulation Methods 0.000 title claims abstract description 99
- 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 96
- 229960002258 fulvestrant Drugs 0.000 title claims description 91
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 79
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 39
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 36
- JBTWLSYIZRCDFO-UHFFFAOYSA-N ethyl methyl carbonate Chemical compound CCOC(=O)OC JBTWLSYIZRCDFO-UHFFFAOYSA-N 0.000 claims abstract description 24
- 150000001875 compounds Chemical class 0.000 claims abstract description 16
- 229940066675 ricinoleate Drugs 0.000 claims abstract description 7
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 claims abstract description 7
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims description 45
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical group C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 claims description 45
- 229960002903 benzyl benzoate Drugs 0.000 claims description 23
- 238000010255 intramuscular injection Methods 0.000 claims description 16
- 239000007927 intramuscular injection Substances 0.000 claims description 16
- 235000019445 benzyl alcohol Nutrition 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 9
- 238000011282 treatment Methods 0.000 claims description 7
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims description 5
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims description 4
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims description 4
- 229940093471 ethyl oleate Drugs 0.000 claims description 4
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 claims description 3
- 229940074928 isopropyl myristate Drugs 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000002347 injection Methods 0.000 abstract description 21
- 239000007924 injection Substances 0.000 abstract description 21
- 238000013268 sustained release Methods 0.000 abstract description 11
- 239000012730 sustained-release form Substances 0.000 abstract description 11
- -1 4,4,5,5,5-pentafluoropentylsulfinyl Chemical group 0.000 abstract description 6
- 239000000243 solution Substances 0.000 abstract description 6
- 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 abstract description 3
- 239000003921 oil Substances 0.000 description 32
- 235000019198 oils Nutrition 0.000 description 32
- 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 18
- 150000001298 alcohols Chemical class 0.000 description 15
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound 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 14
- 239000000328 estrogen antagonist Substances 0.000 description 13
- 230000001833 anti-estrogenic effect Effects 0.000 description 12
- 229930182833 estradiol Natural products 0.000 description 12
- 229960005309 estradiol Drugs 0.000 description 12
- 239000000262 estrogen Substances 0.000 description 12
- 229940011871 estrogen Drugs 0.000 description 12
- DOMWKUIIPQCAJU-LJHIYBGHSA-N Hydroxyprogesterone caproate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)CCCCC)[C@@]1(C)CC2 DOMWKUIIPQCAJU-LJHIYBGHSA-N 0.000 description 11
- 229940046836 anti-estrogen Drugs 0.000 description 11
- 239000003759 ester based solvent Substances 0.000 description 11
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 10
- 230000000694 effects Effects 0.000 description 10
- 239000004359 castor oil Substances 0.000 description 8
- 235000019438 castor oil Nutrition 0.000 description 8
- 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 8
- 229950000801 hydroxyprogesterone caproate Drugs 0.000 description 8
- 150000003431 steroids Chemical class 0.000 description 8
- 102000015694 estrogen receptors Human genes 0.000 description 7
- 108010038795 estrogen receptors Proteins 0.000 description 7
- 229960003387 progesterone Drugs 0.000 description 7
- 239000000186 progesterone Substances 0.000 description 7
- 201000010099 disease Diseases 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
- 241000220438 Arachis Species 0.000 description 5
- 235000003911 Arachis Nutrition 0.000 description 5
- 206010006187 Breast cancer Diseases 0.000 description 5
- 208000026310 Breast neoplasm Diseases 0.000 description 5
- 239000003098 androgen Substances 0.000 description 5
- 229960001603 tamoxifen Drugs 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- DBPWSSGDRRHUNT-CEGNMAFCSA-N 17α-hydroxyprogesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 DBPWSSGDRRHUNT-CEGNMAFCSA-N 0.000 description 4
- MNWFXJYAOYHMED-UHFFFAOYSA-M heptanoate Chemical compound CCCCCCC([O-])=O MNWFXJYAOYHMED-UHFFFAOYSA-M 0.000 description 4
- 238000001556 precipitation Methods 0.000 description 4
- 239000008159 sesame oil Substances 0.000 description 4
- 235000011803 sesame oil Nutrition 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 241000283973 Oryctolagus cuniculus Species 0.000 description 3
- 210000000481 breast Anatomy 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 238000007918 intramuscular administration Methods 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- 230000003211 malignant effect Effects 0.000 description 3
- 238000007911 parenteral administration Methods 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 229940071643 prefilled syringe Drugs 0.000 description 3
- 210000005000 reproductive tract Anatomy 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 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 2
- KXUGUWTUFUWYRS-UHFFFAOYSA-N 1-methylimidazole-4-sulfonyl chloride Chemical compound CN1C=NC(S(Cl)(=O)=O)=C1 KXUGUWTUFUWYRS-UHFFFAOYSA-N 0.000 description 2
- DBPWSSGDRRHUNT-UHFFFAOYSA-N 17alpha-hydroxy progesterone Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C(=O)C)(O)C1(C)CC2 DBPWSSGDRRHUNT-UHFFFAOYSA-N 0.000 description 2
- ORGPUALGNXTPAW-UHFFFAOYSA-N 2,6-dichloro-n-(1-cyanocycloheptyl)benzamide Chemical compound ClC1=CC=CC(Cl)=C1C(=O)NC1(C#N)CCCCCC1 ORGPUALGNXTPAW-UHFFFAOYSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 description 2
- 201000009273 Endometriosis Diseases 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- APTGJECXMIKIET-WOSSHHRXSA-N Norethindrone enanthate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)CCCCCC)[C@@]1(C)CC2 APTGJECXMIKIET-WOSSHHRXSA-N 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- PPYHLSBUTAPNGT-BKWLFHPQSA-N Testosterone isocaproate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCC(C)C)[C@@]1(C)CC2 PPYHLSBUTAPNGT-BKWLFHPQSA-N 0.000 description 2
- PDMMFKSKQVNJMI-BLQWBTBKSA-N Testosterone propionate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CC)[C@@]1(C)CC2 PDMMFKSKQVNJMI-BLQWBTBKSA-N 0.000 description 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 2
- NKJYZYWCGKSMSV-BDPSOKNUSA-N [(8r,9s,10r,13s,14s,17r)-17-acetyl-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-yl] heptanoate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)CCCCCC)[C@@]1(C)CC2 NKJYZYWCGKSMSV-BDPSOKNUSA-N 0.000 description 2
- GRAAWEGTURLYKP-MVTMSODMSA-N [(8r,9s,10r,13s,14s,17s)-13-methyl-3-oxo-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl] undecanoate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCCCCCC)[C@@]1(C)CC2 GRAAWEGTURLYKP-MVTMSODMSA-N 0.000 description 2
- IVRCALGRJCHPRV-BZDYCCQFSA-N [(8r,9s,13s,14s,17s)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] cyclohexanecarboxylate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H](C4=CC=C(O)C=C4CC3)CC[C@@]21C)C(=O)C1CCCCC1 IVRCALGRJCHPRV-BZDYCCQFSA-N 0.000 description 2
- 238000002679 ablation Methods 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 238000007792 addition Methods 0.000 description 2
- 229940087168 alpha tocopherol Drugs 0.000 description 2
- 230000037182 bone density Effects 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 230000007850 degeneration Effects 0.000 description 2
- 229940005558 delestrogen Drugs 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 229960002899 hydroxyprogesterone Drugs 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 239000012299 nitrogen atmosphere Substances 0.000 description 2
- 239000000346 nonvolatile oil Substances 0.000 description 2
- 229960002082 norethindrone enanthate Drugs 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- 230000000704 physical effect Effects 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- WBHHMMIMDMUBKC-XLNAKTSKSA-N ricinelaidic acid Chemical compound CCCCCC[C@@H](O)C\C=C\CCCCCCCC(O)=O WBHHMMIMDMUBKC-XLNAKTSKSA-N 0.000 description 2
- 229960003656 ricinoleic acid Drugs 0.000 description 2
- FEUQNCSVHBHROZ-UHFFFAOYSA-N ricinoleic acid Natural products CCCCCCC(O[Si](C)(C)C)CC=CCCCCCCCC(=O)OC FEUQNCSVHBHROZ-UHFFFAOYSA-N 0.000 description 2
- 238000005063 solubilization Methods 0.000 description 2
- 230000007928 solubilization Effects 0.000 description 2
- 239000011877 solvent mixture Substances 0.000 description 2
- 229960003410 testosterone decanoate Drugs 0.000 description 2
- 229960001642 testosterone isocaproate Drugs 0.000 description 2
- 229960001712 testosterone propionate Drugs 0.000 description 2
- 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 2
- 229960000984 tocofersolan Drugs 0.000 description 2
- MEHHPFQKXOUFFV-OWSLCNJRSA-N trenbolone Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](C)([C@H](CC3)O)C=C3)C3=C21 MEHHPFQKXOUFFV-OWSLCNJRSA-N 0.000 description 2
- 229960000312 trenbolone Drugs 0.000 description 2
- GQJSFWYQKNQCIK-APFRJGHOSA-N trenbolone hexahydrobenzylcarbonate Chemical compound O([C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3C=C[C@@]21C)C(=O)OCC1CCCCC1 GQJSFWYQKNQCIK-APFRJGHOSA-N 0.000 description 2
- 229950005402 trenbolone hexahydrobenzylcarbonate Drugs 0.000 description 2
- 239000002076 α-tocopherol Substances 0.000 description 2
- 235000004835 α-tocopherol Nutrition 0.000 description 2
- 241000282693 Cercopithecidae Species 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 102000006771 Gonadotropins Human genes 0.000 description 1
- 108010086677 Gonadotropins Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 240000007817 Olea europaea Species 0.000 description 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 1
- 206010064390 Tumour invasion Diseases 0.000 description 1
- 238000011298 ablation treatment Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000008484 agonism Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 239000003886 aromatase inhibitor Substances 0.000 description 1
- 229940046844 aromatase inhibitors Drugs 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- MTZQAGJQAFMTAQ-UHFFFAOYSA-N benzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1 MTZQAGJQAFMTAQ-UHFFFAOYSA-N 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 239000008364 bulk solution Substances 0.000 description 1
- 230000009400 cancer invasion Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 230000021615 conjugation Effects 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 150000002009 diols Chemical class 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000013020 final formulation Substances 0.000 description 1
- 239000002622 gonadotropin Substances 0.000 description 1
- 208000021760 high fever Diseases 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000002267 hypothalamic effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007972 injectable composition Substances 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
- 230000002045 lasting effect Effects 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 238000013160 medical therapy Methods 0.000 description 1
- FJQXCDYVZAHXNS-UHFFFAOYSA-N methadone hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 FJQXCDYVZAHXNS-UHFFFAOYSA-N 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 230000001376 precipitating effect Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 229940062451 progesterone 50 mg Drugs 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 238000007614 solvation Methods 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 1
- 229960005026 toremifene Drugs 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 125000005457 triglyceride group Chemical group 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 230000001836 utereotrophic effect Effects 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0000313.7A GB0000313D0 (en) | 2000-01-10 | 2000-01-10 | Formulation |
| GB0000313.7 | 2000-01-10 | ||
| GB0008837.7 | 2000-04-12 | ||
| GBGB0008837.7A GB0008837D0 (en) | 2000-01-10 | 2000-04-12 | Formulation |
| PCT/GB2001/000049 WO2001051056A1 (en) | 2000-01-10 | 2001-01-08 | Fulvestrant formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20020073499A KR20020073499A (ko) | 2002-09-26 |
| KR100802366B1 true KR100802366B1 (ko) | 2008-02-13 |
Family
ID=26243352
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020027008855A Expired - Lifetime KR100802366B1 (ko) | 2000-01-10 | 2001-01-08 | 풀베스트란트 제제 |
Country Status (41)
Families Citing this family (98)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0000313D0 (en) * | 2000-01-10 | 2000-03-01 | Astrazeneca Uk Ltd | Formulation |
| HUP0400115A3 (en) * | 2001-07-07 | 2005-11-28 | Astrazeneca Ab | Pharmaceutical composition for the intramuscular administration of fulvestrant |
| GB0116620D0 (en) * | 2001-07-07 | 2001-08-29 | Astrazeneca Ab | Formulation |
| EP2316921B1 (en) | 2002-05-24 | 2014-05-14 | Merck Sharp & Dohme Corp. | Neutralizing human anti-IGFR antibody |
| TW200404552A (en) * | 2002-05-30 | 2004-04-01 | Akzo Nobel Nv | Self administered contraception |
| US20050152858A1 (en) * | 2003-07-11 | 2005-07-14 | Isp Investments Inc. | Solubilizing agents for active or functional organic compounds |
| PE20050928A1 (es) * | 2003-11-21 | 2005-11-08 | Schering Corp | Combinaciones terapeuticas de anticuerpo anti-igfr1 |
| EP1623713A1 (en) * | 2004-07-09 | 2006-02-08 | Proskelia SAS | Cominations of pure anti-estrogen with aromatase inhibitors |
| MX2007012896A (es) * | 2005-04-15 | 2007-12-10 | Schering Corp | Metodos y composiciones para tratamiento o prevencion de cancer. |
| US20090227552A1 (en) * | 2005-09-26 | 2009-09-10 | Kellie Ann Hooley | Fulvestrant formulations |
| RU2338538C1 (ru) * | 2007-02-09 | 2008-11-20 | Государственное учебно-научное учреждение Химический факультет Московского государственного университета им. М.В. Ломоносова | Антигипотензивное средство |
| CA2716576A1 (en) | 2008-03-07 | 2009-09-11 | Nageswara R. Palepu | Fulvestrant formulations |
| AU2014200332B2 (en) * | 2008-04-28 | 2016-10-06 | Diurnal Limited | Lipid composition |
| GB0807605D0 (en) | 2008-04-28 | 2008-06-04 | Diurnal Ltd | Lipid composition |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| US20100317635A1 (en) | 2009-06-16 | 2010-12-16 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
| JP2013528223A (ja) | 2010-06-10 | 2013-07-08 | アラゴン ファーマシューティカルズ，インク． | エストロゲン受容体モジュレーターおよびその用途 |
| US8853423B2 (en) | 2010-06-17 | 2014-10-07 | Seragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
| EP2616078B1 (en) | 2010-09-16 | 2019-12-25 | Shimoda Biotech (Pty) Ltd | Fulvestrant compositions and methods of use |
| CA2836831C (en) * | 2011-05-20 | 2015-06-02 | Capital, Business Y Gestion De Finanzas S.L. | Pharmaceutical composition |
| CN102391341B (zh) * | 2011-08-09 | 2013-05-22 | 福建省微生物研究所 | 制备6,7-脱氢-17β-烃酰氧基诺龙的方法 |
| CN103070871B (zh) * | 2011-10-26 | 2015-04-15 | 正大天晴药业集团股份有限公司 | 一种氟维司群的药物组合物 |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| BR112014012444B1 (pt) | 2011-11-23 | 2021-12-14 | Therapeuticsmd, Inc | Composição farmacêutica compreendendo estradiol solubilizado, progesterona e um agente de solubilização, bem como usos desta para tratar um sintoma relacionado à menopausa em uma mulher |
| US9193714B2 (en) | 2011-12-14 | 2015-11-24 | Seragon Pharmaceuticals, Inc. | Fluorinated estrogen receptor modulators and uses thereof |
| PE20150099A1 (es) | 2011-12-16 | 2015-01-30 | Olema Pharmaceuticals Inc | Compuestos novedosos de benzopirano, composiciones y usos de los mismos |
| CN102600064A (zh) * | 2012-03-31 | 2012-07-25 | 西安力邦制药有限公司 | 氟维司群或其衍生物缓释制剂及其制备方法 |
| CN102600073B (zh) * | 2012-03-31 | 2014-01-01 | 莱普德制药有限公司 | 以乳酸酯为基础的氟维司群或其衍生物油性制剂及其制备方法 |
| CA2869377C (en) * | 2012-04-09 | 2022-11-08 | Scidose, Llc | Fulvestrant formulations |
| US11179468B2 (en) | 2012-04-09 | 2021-11-23 | Eagle Pharmaceuticals, Inc. | Fulvestrant formulations |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| CA2909418A1 (en) | 2013-04-18 | 2014-10-23 | Xi'an Libang Pharmaceutical Technology Co., Ltd. | Ester derivative of 7-.alpha.-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)n onyl]-estra-1,3,5(10)-triene-3,17.beta.-diol having anticancer activity and preparation method thereof |
| US10392667B2 (en) | 2013-06-07 | 2019-08-27 | Medical Prognosis Institute A/S | Methods and devices for predicting treatment efficacy of fulvestrant in cancer patients |
| WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
| WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
| CN104337761B (zh) * | 2013-08-07 | 2019-03-26 | 江苏豪森药业集团有限公司 | 氟维司群药物组合物 |
| JP2016529308A (ja) * | 2013-09-06 | 2016-09-23 | サラー ウッディン アハメド， | フルベストラント組成物 |
| US9271990B2 (en) | 2014-02-14 | 2016-03-01 | Fresenius Kabi Usa, Llc | Fulvestrant formulations |
| SG11201607334YA (en) | 2014-03-13 | 2016-10-28 | Hoffmann La Roche | Therapeutic combinations with estrogen receptor modulators |
| CA2947767A1 (en) | 2014-05-22 | 2015-11-26 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US10098894B2 (en) | 2014-07-29 | 2018-10-16 | Therapeuticsmd, Inc. | Transdermal cream |
| CN107108611B (zh) | 2014-12-18 | 2020-09-25 | 豪夫迈·罗氏有限公司 | 四氢-吡啶并[3,4-b]吲哚雌激素受体调节剂及其用途 |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| DK3355884T3 (da) | 2015-10-01 | 2021-08-02 | Olema Pharmaceuticals Inc | Tetrahydro-1h-pyrido[3,4-b]indol-antiøstrogenlægemidler |
| BR112018007486A2 (pt) | 2015-10-13 | 2018-10-23 | Nevakar Llc | composição de fulvestrant pronta para injetar e método para a fabricação de um artigo contendo uma composição de fulvestrant pronta para injetar |
| WO2017100715A1 (en) | 2015-12-09 | 2017-06-15 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective estrogen receptor downregulator compounds |
| WO2017173071A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical composition |
| WO2017173044A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd Inc. | Steroid hormone compositions in medium chain oils |
| EP3441073B1 (en) | 2016-04-06 | 2022-02-23 | FUJIFILM Corporation | Medicinal composition comprising fulvestrant |
| WO2017174757A1 (en) | 2016-04-08 | 2017-10-12 | F. Hoffmann-La Roche Ag | Tetrahydroisoquinoline estrogen receptor modulators and uses thereof |
| US11590077B2 (en) | 2016-05-06 | 2023-02-28 | Eagle Pharmaceuticals, Inc. | Fulvestrant formulations and methods of their use |
| IL285928B2 (en) * | 2016-05-06 | 2025-06-01 | Eagle Pharmaceuticals Inc | Fulvestrant formulations and methods of their use |
| EP3466430B1 (en) | 2016-05-31 | 2020-04-29 | FUJIFILM Corporation | Pharmaceutical composition |
| JP2019521983A (ja) | 2016-06-16 | 2019-08-08 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | テトラヒドロ−ピリド［３，４−ｂ］インドールエストロゲン受容体モジュレーター及びその使用 |
| JP7018026B2 (ja) * | 2016-06-16 | 2022-02-09 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | ヘテロアリールエストロゲン受容体モジュレーター及びその使用 |
| US20180002344A1 (en) | 2016-06-16 | 2018-01-04 | Genentech, Inc. | Heteroaryl estrogen receptor modulators and uses thereof |
| CN107789320B (zh) * | 2016-08-31 | 2021-06-22 | 鲁南制药集团股份有限公司 | 一种氟维司群缓释注射液及其制备工艺 |
| IL272924B2 (en) | 2017-09-11 | 2024-01-01 | Atossa Therapeutics Inc | Methods for making and using endoxifen |
| CN111479556B (zh) * | 2017-11-08 | 2023-09-01 | 伊格尔制药公司 | 氟维司群制剂及其使用方法 |
| CA3081602A1 (en) | 2017-11-16 | 2019-05-23 | Novartis Ag | Combination therapies |
| CN111465398A (zh) * | 2018-01-31 | 2020-07-28 | 富士胶片株式会社 | 注射用制剂的制造方法 |
| RU2684330C1 (ru) * | 2018-02-02 | 2019-04-08 | Закрытое Акционерное Общество "Биокад" | Композиции фулвестранта |
| CA3101421C (en) | 2018-05-24 | 2024-06-18 | Kashiv Biosciences, Llc | Prodrugs of fulvestrant |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| CN111035613A (zh) * | 2018-10-12 | 2020-04-21 | 江苏恒瑞医药股份有限公司 | 一种包含氟维司群的可注射的药物组合物及其制备方法 |
| JP2022508055A (ja) | 2018-11-01 | 2022-01-19 | サイロス ファーマシューティカルズ， インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤 |
| KR20210106437A (ko) | 2018-12-20 | 2021-08-30 | 노파르티스 아게 | 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물 |
| AU2020222345B2 (en) | 2019-02-15 | 2022-11-17 | Novartis Ag | 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| US12479817B2 (en) | 2019-02-15 | 2025-11-25 | Novartis Ag | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| US20230092679A1 (en) | 2019-05-20 | 2023-03-23 | Novartis Ag | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| CA3145867A1 (en) | 2019-07-03 | 2021-01-07 | Atossa Therapeutics, Inc. | Sustained release compositions of endoxifen |
| KR20220034129A (ko) | 2019-07-07 | 2022-03-17 | 올레마 파마슈티컬스 인코포레이티드 | 에스트로겐 수용체 길항제 요법 |
| RU2722988C1 (ru) * | 2019-11-19 | 2020-06-05 | федеральное государственное бюджетное образовательное учреждение высшего образования "Башкирский государственный медицинский университет" Министерства здравоохранения Российской Федерации | Способ моделирования проканцерогенного действия фулвестранта на яичники потомства женского пола у лабораторных мышей |
| CN113260353B (zh) * | 2019-12-11 | 2024-11-29 | 上海云晟研新生物科技有限公司 | 氟维司群药物组合物、其制备方法及应用 |
| JP2023506958A (ja) | 2019-12-20 | 2023-02-20 | ノバルティス アーゲー | 骨髄線維症および骨髄異形成症候群を処置するための、デシタビンまたは抗ｐｄ－１抗体スパルタリズマブを伴うかまたは伴わない抗ｔｉｍ－３抗体ｍｂｇ４５３および抗ｔｇｆ－ベータ抗体ｎｉｓ７９３の組合せ |
| US11633405B2 (en) | 2020-02-07 | 2023-04-25 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical formulations |
| WO2021260528A1 (en) | 2020-06-23 | 2021-12-30 | Novartis Ag | Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives |
| WO2022029573A1 (en) | 2020-08-03 | 2022-02-10 | Novartis Ag | Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| US20240042051A1 (en) | 2020-11-24 | 2024-02-08 | Francesca Rocchetti | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| EP4251648A2 (en) | 2020-11-24 | 2023-10-04 | Novartis AG | Anti-cd48 antibodies, antibody drug conjugates, and uses thereof |
| CN117794929A (zh) | 2021-02-02 | 2024-03-29 | 法国施维雅药厂 | 选择性bcl-xl protac化合物及使用方法 |
| TW202304979A (zh) | 2021-04-07 | 2023-02-01 | 瑞士商諾華公司 | 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途 |
| AR125874A1 (es) | 2021-05-18 | 2023-08-23 | Novartis Ag | Terapias de combinación |
| JP2024545690A (ja) * | 2021-12-20 | 2024-12-10 | サムヤン、ホールディングス、コーポレーション | 溶解度が改善されたフルベストラントの医薬組成物及びその製造方法 |
| KR20250027281A (ko) | 2022-05-20 | 2025-02-25 | 노파르티스 아게 | Epha2 bcl-xl 억제제 항체-약물 접합체 및 그의 사용 방법 |
| AU2023273734A1 (en) | 2022-05-20 | 2024-12-12 | Les Laboratoires Servier | Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof |
| IL322700A (en) | 2023-03-10 | 2025-10-01 | Novartis Ag | Antibody-drug conjugates that inhibit fennerase and methods of using them |
| WO2025111450A1 (en) | 2023-11-22 | 2025-05-30 | Les Laboratoires Servier | Anti-cd74 antibody-drug conjugates and methods of use thereof |
| WO2025215536A1 (en) | 2024-04-10 | 2025-10-16 | Novartis Ag | Macrocyclic panras inhibitors for the treatment of cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0346014A1 (en) * | 1988-06-06 | 1989-12-13 | Zeneca Limited | Therapeutic product for the treatment of peri- or postmenopausal conditions |
| WO1996019997A1 (de) * | 1994-12-23 | 1996-07-04 | Schering Aktiengesellschaft | Progesteronantagonistisch- und antiöstrogen wirksame verbindungen zur gemeinsamen verwendung für die weibliche kontrazeption |
| WO1997021440A1 (en) * | 1995-12-12 | 1997-06-19 | Zeneca Limited | A solution for oral administration containing ici 182,780 |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB817241A (en) | 1957-08-21 | 1959-07-29 | Vismara Francesco Spa | Oily solutions for parenteral administration containing adreno-cortical hormones |
| FR6241E (fr) | 1905-04-19 | 1906-10-10 | Ktiengesellschaft | Système de refroidissement du piston des moteurs à explosions et des compresseurs |
| DE947335C (de) | 1954-10-19 | 1956-08-16 | Schering Ag | Verfahren zur Herstellung stabiler oeliger Loesungen von Oestron |
| US2983649A (en) | 1957-10-15 | 1961-05-09 | Francesco Vismara Societa Per | Ricinoleic acid ester solutions of adreno-cortical hormones |
| GB1060632A (en) * | 1962-09-11 | 1967-03-08 | Olin Mathieson | Steroid compositions |
| US3164520A (en) * | 1962-10-29 | 1965-01-05 | Olin Mathieson | Injectable steroid compositions containing at least 75% benzyl benzoate |
| JPS4327327Y1 (enExample) | 1965-01-07 | 1968-11-12 | ||
| NL151903B (nl) | 1965-03-24 | 1977-01-17 | Schering Ag | Werkwijze ter bereiding van een injectievloeistof door een steroid op te lossen in een mengsel van ricinusolie en benzylbenzoaat. |
| USRE28690E (en) * | 1965-05-05 | 1976-01-20 | Schering Aktiengesellschaft | 17α-Ethinyl-18-methyl-19-nortestosterone esters |
| GB1207571A (en) * | 1967-01-13 | 1970-10-07 | Takeda Chemical Industries Ltd | Injectable composition |
| SU549118A1 (ru) | 1973-04-02 | 1977-03-05 | Способ синхронизации половой охоты у циклирующих свиноматок | |
| SU676284A1 (ru) | 1975-06-26 | 1979-07-30 | Научно-Исследовательский Институт Животноводства | Способ синхронизации половой охоты у самок домашних животных |
| DE2548413A1 (de) | 1975-10-27 | 1977-04-28 | Schering Ag | Depotpraeparate in oeliger ungesaettigter loesung zur intramuskulaeren injektion |
| US4048310A (en) | 1976-02-24 | 1977-09-13 | E. R. Squibb & Sons, Inc. | Topical steroid formulation in form of lotion or cream |
| US4048309A (en) | 1976-02-24 | 1977-09-13 | E. R. Squibb & Sons, Inc. | Topical steroid ointment formulations |
| NL7711916A (nl) * | 1977-10-29 | 1979-05-02 | Akzo Nv | Werkwijze ter bereiding van sterk geconcen- treerde farmaceutische preparaten van steroiden. |
| DE2907460A1 (de) * | 1978-03-07 | 1979-09-13 | Sandoz Ag | Neue resorbierbare galenische kompositionen |
| GB8327256D0 (en) * | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| DE3708942A1 (de) | 1987-03-18 | 1988-09-29 | Schering Ag | 19,11ss-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3733478A1 (de) | 1987-10-01 | 1989-04-13 | Schering Ag | Antigestagen- und antioestrogenwirksame verbindungen zur geburtseinleitung und zum schwangerschaftsabbruch sowie zur behandlung gynaekologischer stoerungen und hormonabhaengiger tumore |
| EP0310542B1 (de) * | 1987-10-01 | 1994-06-08 | Schering Aktiengesellschaft | Antigestagen- und antiöstrogenwirksame Verbindungen zur Behandlung hormonabhängiger Tumoren |
| JPH04327327A (ja) | 1991-04-25 | 1992-11-16 | Toyoda Gosei Co Ltd | スリーブとホースの加締め用ダイス |
| CN1102095A (zh) | 1993-10-30 | 1995-05-03 | 浙江医科大学 | 长效雄激素类制剂——十一酸睾丸注射液 |
| IL111991A (en) | 1994-01-28 | 2000-07-26 | Abbott Lab | Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent |
| US20010006963A1 (en) | 1995-03-16 | 2001-07-05 | Ursula Lachnit-Fixson | Once-a-month injection as a depot contraceptive and for hormone replacement therapy for perimenopausal and premenopausal women |
| DE19510861A1 (de) | 1995-03-16 | 1996-09-19 | Schering Ag | Einmonatsspritze als Depot-Kontrazeptivum und für die Hormonersatztherapie für peri- und praemenopausale Frauen |
| EP0760237A1 (en) | 1995-08-30 | 1997-03-05 | Cipla Limited | Oil-in-water microemulsions |
| JPH09208496A (ja) * | 1996-01-30 | 1997-08-12 | Takeda Chem Ind Ltd | Ｌｈ−ｒｈ拮抗物質含有組成物 |
| DE19613972A1 (de) | 1996-04-09 | 1997-10-16 | Bayer Ag | Injektionsformulierungen von Avermectinen und Milbemycinen auf Basis von Rizinusöl |
| GB9608719D0 (en) | 1996-04-26 | 1996-07-03 | Scherer Ltd R P | Pharmaceutical compositions |
| JPH10203982A (ja) * | 1996-07-05 | 1998-08-04 | Takeda Chem Ind Ltd | 視機能障害の予防・治療剤 |
| US5952338A (en) | 1996-07-05 | 1999-09-14 | Takeda Chemical Industries, Ltd. | Agent for prophylaxis and treatment of disturbance of visual function |
| DE19635525A1 (de) * | 1996-08-20 | 1998-02-26 | Schering Ag | 7alpha-(xi-Aminoalkyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha(xi-Aminoalkyl-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| DE19638045A1 (de) | 1996-09-18 | 1998-03-19 | Bayer Ag | Injektionsformulierungen von Avermectinen und Milbemycinen |
| JPH10152438A (ja) * | 1996-11-22 | 1998-06-09 | Takeda Chem Ind Ltd | １−アザキサントン誘導体またはその塩の安定化方法および１−アザキサントン誘導体含有組成物 |
| JPH11158200A (ja) * | 1997-09-26 | 1999-06-15 | Takeda Chem Ind Ltd | ヒト成長ホルモン・亜鉛複合体及びその用途 |
| US6191107B1 (en) | 1997-09-26 | 2001-02-20 | Takeda Chemical Industries, Ltd. | Complex of human growth hormone and zinc |
| HU228617B1 (en) | 1997-12-03 | 2013-04-29 | Merial Llc | Long acting injectable formulations containing hydrogenated castor oil |
| AU777572B2 (en) | 1999-04-01 | 2004-10-21 | Board Of Regents, The University Of Texas System | Compositions and methods for treating lymphoma |
| GB0000313D0 (en) | 2000-01-10 | 2000-03-01 | Astrazeneca Uk Ltd | Formulation |
| JP4327327B2 (ja) | 2000-04-03 | 2009-09-09 | ロボテック株式会社 | 固定スプレー揺動装置 |
| HUP0400115A3 (en) | 2001-07-07 | 2005-11-28 | Astrazeneca Ab | Pharmaceutical composition for the intramuscular administration of fulvestrant |
| GB0912999D0 (en) | 2009-07-27 | 2009-09-02 | Astrazeneca Ab | Method-803 |
-
2000
- 2000-01-10 GB GBGB0000313.7A patent/GB0000313D0/en not_active Ceased
- 2000-04-12 GB GBGB0008837.7A patent/GB0008837D0/en not_active Ceased
-
2001
- 2001-01-08 CA CA002351004A patent/CA2351004C/en not_active Expired - Fee Related
- 2001-01-08 ES ES10180667.7T patent/ES2543384T3/es not_active Expired - Lifetime
- 2001-01-08 KR KR1020027008855A patent/KR100802366B1/ko not_active Expired - Lifetime
- 2001-01-08 MX MXPA02006698A patent/MXPA02006698A/es active IP Right Grant
- 2001-01-08 SI SI200131044T patent/SI2266573T1/sl unknown
- 2001-01-08 SI SI200130446T patent/SI1250138T2/sl unknown
- 2001-01-08 EP EP01900186.6A patent/EP1250138B2/en not_active Expired - Lifetime
- 2001-01-08 HK HK03101532.0A patent/HK1049286B/en not_active IP Right Cessation
- 2001-01-08 EP EP10180667.7A patent/EP2266573B1/en not_active Expired - Lifetime
- 2001-01-08 AU AU23863/01A patent/AU762080B2/en not_active Expired
- 2001-01-08 RU RU2002121507A patent/RU2263507C9/ru active
- 2001-01-08 SK SK984-2002A patent/SK287221B6/sk not_active IP Right Cessation
- 2001-01-08 ES ES01900186.6T patent/ES2248272T5/es not_active Expired - Lifetime
- 2001-01-08 US US10/169,777 patent/US20030125387A1/en not_active Abandoned
- 2001-01-08 PL PL356030A patent/PL202525B1/pl unknown
- 2001-01-08 BR BRPI0107445-8A patent/BR0107445B1/pt active IP Right Grant
- 2001-01-08 WO PCT/GB2001/000049 patent/WO2001051056A1/en not_active Ceased
- 2001-01-08 HU HU0204137A patent/HU230162B1/hu not_active IP Right Cessation
- 2001-01-08 EP EP10180661.0A patent/EP2286818B1/en not_active Expired - Lifetime
- 2001-01-08 EG EG20010017A patent/EG24074A/xx active
- 2001-01-08 EE EEP200200387A patent/EE05421B1/xx unknown
- 2001-01-08 DK DK01900186.6T patent/DK1250138T4/en active
- 2001-01-08 PT PT101806677T patent/PT2266573E/pt unknown
- 2001-01-08 AT AT01900186T patent/ATE306928T1/de active
- 2001-01-08 GB GB0100407A patent/GB2359254B/en not_active Expired - Lifetime
- 2001-01-08 CZ CZ2002-2384A patent/CZ304689B6/cs not_active IP Right Cessation
- 2001-01-08 EP EP05016921A patent/EP1669073A3/en not_active Withdrawn
- 2001-01-08 IL IL15023001A patent/IL150230A0/xx active IP Right Grant
- 2001-01-08 HK HK03105241.3A patent/HK1052884B/zh not_active IP Right Cessation
- 2001-01-08 DE DE60114145.8T patent/DE60114145T3/de not_active Expired - Lifetime
- 2001-01-08 DK DK10180667.7T patent/DK2266573T3/en active
- 2001-01-08 JP JP2001551480A patent/JP3713237B2/ja not_active Expired - Lifetime
- 2001-01-08 CN CNB018035469A patent/CN1222292C/zh not_active Ceased
- 2001-01-09 BE BE2001/0021A patent/BE1013477A3/fr not_active IP Right Cessation
- 2001-01-09 PT PT102548A patent/PT102548A/pt not_active Application Discontinuation
- 2001-01-09 IT IT000005A patent/ITTO20010005A1/it unknown
- 2001-01-09 US US09/756,291 patent/US6774122B2/en not_active Expired - Lifetime
- 2001-01-10 CO CO01001317A patent/CO5280206A1/es not_active Application Discontinuation
- 2001-01-10 MY MYPI20010107A patent/MY118583A/en unknown
- 2001-01-10 IT IT2001TO000008A patent/ITTO20010008A1/it unknown
- 2001-01-10 CH CH00029/01A patent/CH696260A5/de not_active IP Right Cessation
- 2001-01-10 DE DE10100779A patent/DE10100779A1/de not_active Ceased
- 2001-01-10 ES ES200100057A patent/ES2186517B2/es not_active Expired - Fee Related
- 2001-01-10 AR ARP010100100A patent/AR027510A1/es not_active Application Discontinuation
- 2001-01-10 TW TW090100514A patent/TWI259086B/zh active
- 2001-01-10 FR FR0100248A patent/FR2803516B1/fr not_active Expired - Lifetime
- 2001-01-10 NL NL1017075A patent/NL1017075C2/nl not_active IP Right Cessation
- 2001-08-01 UA UA2002086628A patent/UA75879C2/uk unknown
-
2002
- 2002-05-24 ZA ZA200204165A patent/ZA200204165B/xx unknown
- 2002-06-13 IL IL150230A patent/IL150230A/en unknown
- 2002-06-18 BG BG106833A patent/BG65776B1/bg unknown
- 2002-07-03 NO NO20023227A patent/NO336286B1/no not_active IP Right Cessation
- 2002-07-03 IS IS6454A patent/IS2932B/is unknown
-
2003
- 2003-10-23 JP JP2003362875A patent/JP2004107353A/ja not_active Ceased
-
2004
- 2004-06-22 US US10/872,784 patent/US7456160B2/en not_active Expired - Lifetime
-
2008
- 2008-10-15 US US12/285,887 patent/US8329680B2/en not_active Expired - Fee Related
-
2011
- 2011-06-20 JP JP2011135962A patent/JP2011190275A/ja active Pending
-
2012
- 2012-09-04 US US13/602,667 patent/US8466139B2/en not_active Expired - Fee Related
-
2015
- 2015-06-08 NO NO20150741A patent/NO337329B1/no not_active IP Right Cessation
- 2015-07-22 CY CY20151100648T patent/CY1116520T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0346014A1 (en) * | 1988-06-06 | 1989-12-13 | Zeneca Limited | Therapeutic product for the treatment of peri- or postmenopausal conditions |
| WO1996019997A1 (de) * | 1994-12-23 | 1996-07-04 | Schering Aktiengesellschaft | Progesteronantagonistisch- und antiöstrogen wirksame verbindungen zur gemeinsamen verwendung für die weibliche kontrazeption |
| WO1997021440A1 (en) * | 1995-12-12 | 1997-06-19 | Zeneca Limited | A solution for oral administration containing ici 182,780 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR100802366B1 (ko) | 풀베스트란트 제제 | |
| HK1150021B (en) | Fulvestrant formulation | |
| HK1153393A (en) | Fulvestrant formulation |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20020709 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20051216 Comment text: Request for Examination of Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20061113 Patent event code: PE09021S01D |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20070607 Patent event code: PE09021S01D |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20080114 |
|
| GRNT | Written decision to grant | ||
| PR0701 | Registration of establishment |
Comment text: Registration of Establishment Patent event date: 20080201 Patent event code: PR07011E01D |
|
| PR1002 | Payment of registration fee |
Payment date: 20080204 End annual number: 3 Start annual number: 1 |
|
| PG1601 | Publication of registration | ||
| PR1001 | Payment of annual fee |
Payment date: 20110201 Start annual number: 4 End annual number: 4 |
|
| PR1001 | Payment of annual fee |
Payment date: 20120131 Start annual number: 5 End annual number: 5 |
|
| FPAY | Annual fee payment |
Payment date: 20130117 Year of fee payment: 6 |
|
| PR1001 | Payment of annual fee |
Payment date: 20130117 Start annual number: 6 End annual number: 6 |
|
| FPAY | Annual fee payment |
Payment date: 20140121 Year of fee payment: 7 |
|
| PR1001 | Payment of annual fee |
Payment date: 20140121 Start annual number: 7 End annual number: 7 |
|
| FPAY | Annual fee payment |
Payment date: 20150116 Year of fee payment: 8 |
|
| PR1001 | Payment of annual fee |
Payment date: 20150116 Start annual number: 8 End annual number: 8 |
|
| FPAY | Annual fee payment |
Payment date: 20160104 Year of fee payment: 9 |
|
| PR1001 | Payment of annual fee |
Payment date: 20160104 Start annual number: 9 End annual number: 9 |
|
| FPAY | Annual fee payment |
Payment date: 20170102 Year of fee payment: 10 |
|
| PR1001 | Payment of annual fee |
Payment date: 20170102 Start annual number: 10 End annual number: 10 |
|
| FPAY | Annual fee payment |
Payment date: 20180103 Year of fee payment: 11 |
|
| PR1001 | Payment of annual fee |
Payment date: 20180103 Start annual number: 11 End annual number: 11 |
|
| FPAY | Annual fee payment |
Payment date: 20190103 Year of fee payment: 12 |
|
| PR1001 | Payment of annual fee |
Payment date: 20190103 Start annual number: 12 End annual number: 12 |
|
| FPAY | Annual fee payment |
Payment date: 20200103 Year of fee payment: 13 |
|
| PR1001 | Payment of annual fee |
Payment date: 20200103 Start annual number: 13 End annual number: 13 |
|
| PC1801 | Expiration of term |
Termination date: 20210708 Termination category: Expiration of duration |