JP2003512301A - アロマターゼ阻害剤と更なる生理活性化合物とを含む併用治療法 - Google Patents

アロマターゼ阻害剤と更なる生理活性化合物とを含む併用治療法

Info

Publication number: JP2003512301A
Authority: JP; Japan
Prior art keywords: antitumor; amount; effective; tumor; agent
Prior art date: 1999-05-18
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

JP2000617927A

Other languages

English (en)

Japanese (ja)

Inventor

デイ・サツレ，エンリコ

ザツケオ，テイツイアーナ

テデスキ，ミケーレ

Original Assignee

フアルマシア・エ・アツプジヨン・エツセ・ピー・アー

Priority date (The priority date 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 date listed.)

1999-05-18

Filing date

2000-04-14

Publication date

2003-04-02

2000-04-14 Application filed by フアルマシア・エ・アツプジヨン・エツセ・ピー・アー filed Critical フアルマシア・エ・アツプジヨン・エツセ・ピー・アー

2003-04-02 Publication of JP2003512301A publication Critical patent/JP2003512301A/ja

Status Withdrawn legal-status Critical Current

Links

239000003886 aromatase inhibitor Substances 0.000 title claims abstract description 44
229940122815 Aromatase inhibitor Drugs 0.000 title claims abstract description 37
150000001875 compounds Chemical class 0.000 title claims description 18
238000002648 combination therapy Methods 0.000 title description 3
230000000975 bioactive effect Effects 0.000 title 1
230000000259 anti-tumor effect Effects 0.000 claims abstract description 83
239000002246 antineoplastic agent Substances 0.000 claims abstract description 42
206010006187 Breast cancer Diseases 0.000 claims abstract description 31
208000026310 Breast neoplasm Diseases 0.000 claims abstract description 30
239000000203 mixture Substances 0.000 claims abstract description 25
239000003085 diluting agent Substances 0.000 claims abstract description 6
239000003937 drug carrier Substances 0.000 claims abstract description 5
206010028980 Neoplasm Diseases 0.000 claims description 50
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 35
229960000255 exemestane Drugs 0.000 claims description 35
238000000034 method Methods 0.000 claims description 35
238000011282 treatment Methods 0.000 claims description 34
AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-VTZDEGQISA-N 0.000 claims description 28
HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims description 28
229960001904 epirubicin Drugs 0.000 claims description 28
AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 26
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 claims description 21
229960003668 docetaxel Drugs 0.000 claims description 21
230000000694 effects Effects 0.000 claims description 18
229930012538 Paclitaxel Natural products 0.000 claims description 13
239000000654 additive Substances 0.000 claims description 13
229960004679 doxorubicin Drugs 0.000 claims description 13
229960001592 paclitaxel Drugs 0.000 claims description 13
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 claims description 13
CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical group ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 12
XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims description 12
XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims description 12
229960004397 cyclophosphamide Drugs 0.000 claims description 12
229960000908 idarubicin Drugs 0.000 claims description 12
230000003637 steroidlike Effects 0.000 claims description 12
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 11
GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 11
229960002932 anastrozole Drugs 0.000 claims description 11
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 11
-1 borozole Chemical compound 0.000 claims description 11
229950011548 fadrozole Drugs 0.000 claims description 11
229960002949 fluorouracil Drugs 0.000 claims description 11
229960004421 formestane Drugs 0.000 claims description 11
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 11
229960003881 letrozole Drugs 0.000 claims description 11
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 11
241000282412 Homo Species 0.000 claims description 10
229960002066 vinorelbine Drugs 0.000 claims description 10
GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims description 10
229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims description 9
239000000365 Topoisomerase I Inhibitor Substances 0.000 claims description 9
230000000340 anti-metabolite Effects 0.000 claims description 9
229940100197 antimetabolite Drugs 0.000 claims description 9
239000002256 antimetabolite Substances 0.000 claims description 9
239000008194 pharmaceutical composition Substances 0.000 claims description 9
JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims description 8
229940100198 alkylating agent Drugs 0.000 claims description 8
239000002168 alkylating agent Substances 0.000 claims description 8
229940079593 drug Drugs 0.000 claims description 8
239000003814 drug Substances 0.000 claims description 8
229960003048 vinblastine Drugs 0.000 claims description 8
JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims description 8
GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims description 7
GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims description 7
FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 7
229940046844 aromatase inhibitors Drugs 0.000 claims description 7
229960004117 capecitabine Drugs 0.000 claims description 7
229960001924 melphalan Drugs 0.000 claims description 7
SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 claims description 7
229960000485 methotrexate Drugs 0.000 claims description 7
229960000303 topotecan Drugs 0.000 claims description 7
UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims description 7
229940122803 Vinca alkaloid Drugs 0.000 claims description 6
229940045799 anthracyclines and related substance Drugs 0.000 claims description 6
229960004768 irinotecan Drugs 0.000 claims description 6
UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 6
238000002360 preparation method Methods 0.000 claims description 6
229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims description 5
239000000317 Topoisomerase II Inhibitor Substances 0.000 claims description 5
229960003437 aminoglutethimide Drugs 0.000 claims description 5
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 5
PYKYMHQGRFAEBM-UHFFFAOYSA-N anthraquinone Natural products CCC(=O)c1c(O)c2C(=O)C3C(C=CC=C3O)C(=O)c2cc1CC(=O)OC PYKYMHQGRFAEBM-UHFFFAOYSA-N 0.000 claims description 5
230000000118 anti-neoplastic effect Effects 0.000 claims description 5
229940034982 antineoplastic agent Drugs 0.000 claims description 5
239000003795 chemical substances by application Substances 0.000 claims description 5
231100000782 microtubule inhibitor Toxicity 0.000 claims description 5
229960001156 mitoxantrone Drugs 0.000 claims description 5
KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 claims description 5
GGPPBTSXFROGAE-UHFFFAOYSA-N 4-[(4-bromophenyl)methyl-(1,2,4-triazol-4-yl)amino]benzonitrile Chemical compound C1=CC(Br)=CC=C1CN(N1C=NN=C1)C1=CC=C(C#N)C=C1 GGPPBTSXFROGAE-UHFFFAOYSA-N 0.000 claims description 4
229950006700 edatrexate Drugs 0.000 claims description 4
FSIRXIHZBIXHKT-MHTVFEQDSA-N edatrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CC(CC)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FSIRXIHZBIXHKT-MHTVFEQDSA-N 0.000 claims description 4
VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 4
229960005420 etoposide Drugs 0.000 claims description 4
SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 4
229960005277 gemcitabine Drugs 0.000 claims description 4
229960001101 ifosfamide Drugs 0.000 claims description 4
HOMGKSMUEGBAAB-UHFFFAOYSA-N ifosfamide Chemical compound ClCCNP1(=O)OCCCN1CCCl HOMGKSMUEGBAAB-UHFFFAOYSA-N 0.000 claims description 4
CTMCWCONSULRHO-UHQPFXKFSA-N nemorubicin Chemical compound C1CO[C@H](OC)CN1[C@@H]1[C@H](O)[C@H](C)O[C@@H](O[C@@H]2C3=C(O)C=4C(=O)C5=C(OC)C=CC=C5C(=O)C=4C(O)=C3C[C@](O)(C2)C(=O)CO)C1 CTMCWCONSULRHO-UHQPFXKFSA-N 0.000 claims description 4
229950010159 nemorubicin Drugs 0.000 claims description 4
YJGVMLPVUAXIQN-XVVDYKMHSA-N podophyllotoxin Chemical class COC1=C(OC)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YJGVMLPVUAXIQN-XVVDYKMHSA-N 0.000 claims description 4
229950009213 rubitecan Drugs 0.000 claims description 4
VHXNKPBCCMUMSW-FQEVSTJZSA-N rubitecan Chemical compound C1=CC([N+]([O-])=O)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VHXNKPBCCMUMSW-FQEVSTJZSA-N 0.000 claims description 4
NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims description 4
229960001278 teniposide Drugs 0.000 claims description 4
229940122255 Microtubule inhibitor Drugs 0.000 claims description 3
229940123237 Taxane Drugs 0.000 claims description 3
YJGVMLPVUAXIQN-UHFFFAOYSA-N epipodophyllotoxin Natural products COC1=C(OC)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YJGVMLPVUAXIQN-UHFFFAOYSA-N 0.000 claims description 3
238000004519 manufacturing process Methods 0.000 claims description 3
229960001237 podophyllotoxin Drugs 0.000 claims description 3
YVCVYCSAAZQOJI-UHFFFAOYSA-N podophyllotoxin Natural products COC1=C(O)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YVCVYCSAAZQOJI-UHFFFAOYSA-N 0.000 claims description 3
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 claims description 3
VMDWTZZCNDEKIO-CBNJBKGYSA-N [(2s,3s,4s,6r)-6-[[(1s,3s)-3-acetyl-3,5,12-trihydroxy-6,11-dioxo-2,4-dihydro-1h-tetracen-1-yl]oxy]-4-(aziridin-1-yl)-2-methyloxan-3-yl] methanesulfonate Chemical compound N1([C@H]2C[C@@H](O[C@H]([C@H]2OS(C)(=O)=O)C)O[C@@H]2C3=C(O)C=4C(=O)C5=CC=CC=C5C(=O)C=4C(O)=C3C[C@](O)(C2)C(C)=O)CC1 VMDWTZZCNDEKIO-CBNJBKGYSA-N 0.000 claims description 2
125000000217 alkyl group Chemical group 0.000 claims 1
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 21
229940011871 estrogen Drugs 0.000 description 15
239000000262 estrogen Substances 0.000 description 15
230000004044 response Effects 0.000 description 12
238000002512 chemotherapy Methods 0.000 description 11
229960001603 tamoxifen Drugs 0.000 description 10
238000009472 formulation Methods 0.000 description 9
238000001794 hormone therapy Methods 0.000 description 9
230000004614 tumor growth Effects 0.000 description 9
ARSRBNBHOADGJU-UHFFFAOYSA-N 7,12-dimethyltetraphene Chemical compound C1=CC2=CC=CC=C2C2=C1C(C)=C(C=CC=C1)C1=C2C ARSRBNBHOADGJU-UHFFFAOYSA-N 0.000 description 8
102000014654 Aromatase Human genes 0.000 description 8
108010078554 Aromatase Proteins 0.000 description 8
241000700159 Rattus Species 0.000 description 8
230000012010 growth Effects 0.000 description 7
229940127089 cytotoxic agent Drugs 0.000 description 6
201000010099 disease Diseases 0.000 description 6
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
102000015694 estrogen receptors Human genes 0.000 description 6
108010038795 estrogen receptors Proteins 0.000 description 6
239000002254 cytotoxic agent Substances 0.000 description 5
239000002671 adjuvant Substances 0.000 description 4
230000015572 biosynthetic process Effects 0.000 description 4
230000008859 change Effects 0.000 description 4
238000012937 correction Methods 0.000 description 4
206010061289 metastatic neoplasm Diseases 0.000 description 4
WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
230000009471 action Effects 0.000 description 3
201000011510 cancer Diseases 0.000 description 3
230000002401 inhibitory effect Effects 0.000 description 3
230000036961 partial effect Effects 0.000 description 3
238000009097 single-agent therapy Methods 0.000 description 3
230000004083 survival effect Effects 0.000 description 3
238000002560 therapeutic procedure Methods 0.000 description 3
206010055113 Breast cancer metastatic Diseases 0.000 description 2
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
241000124008 Mammalia Species 0.000 description 2
206010067572 Oestrogenic effect Diseases 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
238000013459 approach Methods 0.000 description 2
238000011260 co-administration Methods 0.000 description 2
231100000433 cytotoxic Toxicity 0.000 description 2
230000001472 cytotoxic effect Effects 0.000 description 2
230000001419 dependent effect Effects 0.000 description 2
239000000328 estrogen antagonist Substances 0.000 description 2
230000001076 estrogenic effect Effects 0.000 description 2
238000002474 experimental method Methods 0.000 description 2
229940088597 hormone Drugs 0.000 description 2
239000005556 hormone Substances 0.000 description 2
239000003112 inhibitor Substances 0.000 description 2
230000005764 inhibitory process Effects 0.000 description 2
230000002452 interceptive effect Effects 0.000 description 2
230000001394 metastastic effect Effects 0.000 description 2
230000002829 reductive effect Effects 0.000 description 2
102220240796 rs553605556 Human genes 0.000 description 2
239000008159 sesame oil Substances 0.000 description 2
235000011803 sesame oil Nutrition 0.000 description 2
230000000638 stimulation Effects 0.000 description 2
238000003786 synthesis reaction Methods 0.000 description 2
238000009121 systemic therapy Methods 0.000 description 2
231100000331 toxic Toxicity 0.000 description 2
230000002588 toxic effect Effects 0.000 description 2
238000013519 translation Methods 0.000 description 2
DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 description 1
VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
206010057654 Breast cancer female Diseases 0.000 description 1
KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 description 1
208000005623 Carcinogenesis Diseases 0.000 description 1
206010014733 Endometrial cancer Diseases 0.000 description 1
206010014759 Endometrial neoplasm Diseases 0.000 description 1
DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 description 1
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
206010053759 Growth retardation Diseases 0.000 description 1
206010027476 Metastases Diseases 0.000 description 1
101000783705 Myxoma virus (strain Uriarra) Envelope protein A28 homolog Proteins 0.000 description 1
101710162501 Ovarian aromatase Proteins 0.000 description 1
108091027981 Response element Proteins 0.000 description 1
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
102000040945 Transcription factor Human genes 0.000 description 1
108091023040 Transcription factor Proteins 0.000 description 1
210000000577 adipose tissue Anatomy 0.000 description 1
230000008484 agonism Effects 0.000 description 1
230000001270 agonistic effect Effects 0.000 description 1
230000001195 anabolic effect Effects 0.000 description 1
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 1
229960005471 androstenedione Drugs 0.000 description 1
AEMFNILZOJDQLW-UHFFFAOYSA-N androstenedione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 AEMFNILZOJDQLW-UHFFFAOYSA-N 0.000 description 1
150000004056 anthraquinones Chemical class 0.000 description 1
229940046836 anti-estrogen Drugs 0.000 description 1
230000001833 anti-estrogenic effect Effects 0.000 description 1
230000003388 anti-hormonal effect Effects 0.000 description 1
229940041181 antineoplastic drug Drugs 0.000 description 1
230000002238 attenuated effect Effects 0.000 description 1
230000008901 benefit Effects 0.000 description 1
235000019445 benzyl alcohol Nutrition 0.000 description 1
230000004071 biological effect Effects 0.000 description 1
210000000481 breast Anatomy 0.000 description 1
229940127093 camptothecin Drugs 0.000 description 1
VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 description 1
230000036952 cancer formation Effects 0.000 description 1
231100000504 carcinogenesis Toxicity 0.000 description 1
238000006243 chemical reaction Methods 0.000 description 1
230000000973 chemotherapeutic effect Effects 0.000 description 1
238000009096 combination chemotherapy Methods 0.000 description 1
238000011284 combination treatment Methods 0.000 description 1
230000002301 combined effect Effects 0.000 description 1
230000001276 controlling effect Effects 0.000 description 1
231100000599 cytotoxic agent Toxicity 0.000 description 1
238000011393 cytotoxic chemotherapy Methods 0.000 description 1
230000003467 diminishing effect Effects 0.000 description 1
230000008034 disappearance Effects 0.000 description 1
VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 description 1
239000000890 drug combination Substances 0.000 description 1
238000013399 early diagnosis Methods 0.000 description 1
230000008030 elimination Effects 0.000 description 1
238000003379 elimination reaction Methods 0.000 description 1
229960005309 estradiol Drugs 0.000 description 1
229930182833 estradiol Natural products 0.000 description 1
229960003399 estrone Drugs 0.000 description 1
238000011156 evaluation Methods 0.000 description 1
239000008103 glucose Substances 0.000 description 1
230000003054 hormonal effect Effects 0.000 description 1
238000001727 in vivo Methods 0.000 description 1
238000007918 intramuscular administration Methods 0.000 description 1
230000002601 intratumoral effect Effects 0.000 description 1
230000001404 mediated effect Effects 0.000 description 1
239000002207 metabolite Substances 0.000 description 1
239000002547 new drug Substances 0.000 description 1
108091008589 nuclear estrogen receptors Proteins 0.000 description 1
238000009806 oophorectomy Methods 0.000 description 1
230000002611 ovarian Effects 0.000 description 1
230000002085 persistent effect Effects 0.000 description 1
239000008177 pharmaceutical agent Substances 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
239000002831 pharmacologic agent Substances 0.000 description 1
230000000144 pharmacologic effect Effects 0.000 description 1
238000010837 poor prognosis Methods 0.000 description 1
230000002265 prevention Effects 0.000 description 1
108090000623 proteins and genes Proteins 0.000 description 1
102000005962 receptors Human genes 0.000 description 1
108020003175 receptors Proteins 0.000 description 1
230000009467 reduction Effects 0.000 description 1
230000001105 regulatory effect Effects 0.000 description 1
238000011160 research Methods 0.000 description 1
238000011519 second-line treatment Methods 0.000 description 1
230000035945 sensitivity Effects 0.000 description 1
150000003431 steroids Chemical class 0.000 description 1
239000000758 substrate Substances 0.000 description 1
238000011477 surgical intervention Methods 0.000 description 1
208000024891 symptom Diseases 0.000 description 1
229960003604 testosterone Drugs 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
210000001519 tissue Anatomy 0.000 description 1
231100000419 toxicity Toxicity 0.000 description 1
230000001988 toxicity Effects 0.000 description 1
238000013518 transcription Methods 0.000 description 1
230000035897 transcription Effects 0.000 description 1
210000004881 tumor cell Anatomy 0.000 description 1
230000009278 visceral effect Effects 0.000 description 1
229960001771 vorozole Drugs 0.000 description 1
XLMPPFTZALNBFS-INIZCTEOSA-N vorozole Chemical compound C1([C@@H](C2=CC=C3N=NN(C3=C2)C)N2N=CN=C2)=CC=C(Cl)C=C1 XLMPPFTZALNBFS-INIZCTEOSA-N 0.000 description 1
230000003442 weekly effect Effects 0.000 description 1
230000004584 weight gain Effects 0.000 description 1
235000019786 weight gain Nutrition 0.000 description 1
230000004580 weight loss 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
- A61K31/33—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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Chemical & Material Sciences (AREA)
Epidemiology (AREA)
Organic Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Molecular Biology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

JP2000617927A 1999-05-18 2000-04-14 アロマターゼ阻害剤と更なる生理活性化合物とを含む併用治療法 Withdrawn JP2003512301A (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GBGB9911582.6A GB9911582D0 (en)	1999-05-18	1999-05-18	Combined method of treatment comprising an aromatase inhibitor and a further biologically active compound
GB9911582.6		1999-05-18
PCT/EP2000/003407 WO2000069467A1 (en)	1999-05-18	2000-04-14	Combined method of treatment comprising an aromatase inhibitor and a further biologically active compound

Publications (1)

Publication Number	Publication Date
JP2003512301A true JP2003512301A (ja)	2003-04-02

Family

ID=10853700

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2000617927A Withdrawn JP2003512301A (ja)	1999-05-18	2000-04-14	アロマターゼ阻害剤と更なる生理活性化合物とを含む併用治療法

Country Status (6)

Country	Link
EP (1)	EP1178831A1 (es)
JP (1)	JP2003512301A (es)
AR (1)	AR029451A1 (es)
AU (1)	AU3820700A (es)
GB (1)	GB9911582D0 (es)
WO (1)	WO2000069467A1 (es)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP2009511609A (ja) *	2005-10-19	2009-03-19	チャバフピーティーワイエルティーディー	乳癌の治療に使用されるアロマターゼ阻害薬による副作用の低減
JP2015145411A (ja) *	2001-02-19	2015-08-13	ノバルティスアーゲー	癌の処置

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2002020020A1 (en) *	2000-09-08	2002-03-14	Pharmacia Italia S.P.A.	Exemestane as chemopreventing agent
NZ525720A (en) *	2000-11-16	2006-12-22	Upjohn Co	The use of triptorelin and exemestane in the manner of a medicament for treating a sex steroid dependent cancer
WO2002092091A1 (en) *	2001-05-16	2002-11-21	Novartis Ag	Combination comprising n-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent
JP6091431B2 (ja)	2011-01-31	2017-03-15	ルコラス−エム．ディー．リミテッド	医薬的使用
US10064874B2 (en)	2014-10-22	2018-09-04	Havah Therapeutics Pty Ltd.	Methods of reducing mammographic breast density and/or breast cancer risk
AU2016343297A1 (en)	2015-10-22	2018-05-10	Havah Therapeutics Pty Ltd	Methods of reducing mammographic breast density and/or breast cancer risk
CN119970752A (zh)	2019-06-03	2025-05-13	哈瓦赫治疗有限公司	用于递送雄激素剂和芳香酶抑制剂的药物制剂

1999
- 1999-05-18 GB GBGB9911582.6A patent/GB9911582D0/en not_active Ceased
2000
- 2000-04-14 EP EP00917084A patent/EP1178831A1/en not_active Withdrawn
- 2000-04-14 WO PCT/EP2000/003407 patent/WO2000069467A1/en not_active Ceased
- 2000-04-14 JP JP2000617927A patent/JP2003512301A/ja not_active Withdrawn
- 2000-04-14 AU AU38207/00A patent/AU3820700A/en not_active Abandoned
- 2000-05-17 AR ARP000102365A patent/AR029451A1/es unknown

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP2015145411A (ja) *	2001-02-19	2015-08-13	ノバルティスアーゲー	癌の処置
JP2009511609A (ja) *	2005-10-19	2009-03-19	チャバフピーティーワイエルティーディー	乳癌の治療に使用されるアロマターゼ阻害薬による副作用の低減
JP2013091656A (ja) *	2005-10-19	2013-05-16	Chavah Pty Ltd	乳癌の治療に使用されるアロマターゼ阻害薬による副作用の低減
US9168302B2 (en)	2005-10-19	2015-10-27	Chavah Pty Ltd	Reduction of side effects from aromatase inhibitors used for treating breast cancer
US9616072B2 (en)	2005-10-19	2017-04-11	Chavah Pty Ltd.	Reduction of side effects from aromatase inhibitors used for treating breast cancer
US10765684B2 (en)	2005-10-19	2020-09-08	Havah Therapeutics Pty Ltd.	Reduction of side effects from aromatase inhibitors used for treating breast cancer

Also Published As

Publication number	Publication date
WO2000069467A1 (en)	2000-11-23
AR029451A1 (es)	2003-07-02
EP1178831A1 (en)	2002-02-13
AU3820700A (en)	2000-12-05
GB9911582D0 (en)	1999-07-21

Publication	Publication Date	Title
EP2783686B1 (en)	2017-06-21	Combination of a rapamycin derivative and letrozole for treating breast cancer
KR102871380B1 (ko)	2025-10-14	암을 치료하는 방법
KR101634138B1 (ko)	2016-06-28	암 치료 방법 및 조성물
AU2008254273B2 (en)	2013-03-28	Methods for using vasopressin antagonists with anthracycline chemotherapy agents to reduce cardiotoxicity and/or improve survival
JP2002543112A (ja)	2002-12-17	アントラサイクリン誘導体を含有する配合製剤
CN1929863A (zh)	2007-03-14	Cci－779和利妥昔单抗的抗肿瘤组合
US20130273178A1 (en)	2013-10-17	Methods and compositions for promoting activity of anti-cancer therapies
JP2002507571A (ja)	2002-03-12	アントラサイクリン誘導体とカンプトテシン誘導体の相乗組合せを含有する抗腫瘍組成物
JP2003512301A (ja)	2003-04-02	アロマターゼ阻害剤と更なる生理活性化合物とを含む併用治療法
ZA200409137B (en)	2005-08-31	Combinations comprising epothilones and pharmaceutical uses thereof
US7879868B2 (en)	2011-02-01	Use of imatinib (glivec,sti-571) to inhibit breast cancer resistance protein (BCRP)-mediated resistance to therapeutic agents
JP2003525233A (ja)	2003-08-26	乳癌のホルモン療法
KR20230144571A (ko)	2023-10-16	Serd 투여 요법의 조합을 사용하여 암을 치료하는 방법
WO2020254299A1 (en)	2020-12-24	Combination of a mcl-1 inhibitor and a standard of care treatment for breast cancer, uses and pharmaceutical compositions thereof
US20030158168A1 (en)	2003-08-21	Composition for combined use of aromatase inhibitors
WO2013037129A1 (zh)	2013-03-21	一种双活性组分抗肿瘤药物组合物及其用途
Rowinsky et al.	1997	Phase I study of paclitaxel on a 3-hour schedule followed by carboplatin in untreated patients with stage IV non-small cell lung cancer
KR20010102402A (ko)	2001-11-15	상승작용성 항종양 조성물
CN120420332A (zh)	2025-08-05	一种含mTOR抑制剂的组合物及其用途
EP3854411A1 (en)	2021-07-28	Pharmaceutical compositions and use thereof for relieving resistance due to cancer chemotherapy and enhancing effect of cancer chemotherapy
JP2005520806A (ja)	2005-07-14	がん治療を改善する併用療法におけるキナゾリノン化合物
HK1198946B (en)	2018-03-16	Combination of a rapamycin derivative and letrozole for treating breast cancer
HK1146247B (en)	2015-10-09	Treatment of breast tumors with a rapamycin derivative in combination with exemestane
HK1232469B (en)	2019-09-06	Rapamycin derivative for the treatment of lung cancer
HK1146245B (en)	2017-04-21	Treatment of solid kidney tumours with a rapamycin derivative

Legal Events

Date	Code	Title	Description
2007-07-03	A300	Application deemed to be withdrawn because no request for examination was validly filed	Free format text: JAPANESE INTERMEDIATE CODE: A300 Effective date: 20070703

Date

Code

Title

Description

2007-07-03

A300

Application deemed to be withdrawn because no request for examination was validly filed

Free format text: JAPANESE INTERMEDIATE CODE: A300

Effective date: 20070703