JP2014511383A5 - - Google Patents
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- Publication number
- JP2014511383A5 JP2014511383A5 JP2013555616A JP2013555616A JP2014511383A5 JP 2014511383 A5 JP2014511383 A5 JP 2014511383A5 JP 2013555616 A JP2013555616 A JP 2013555616A JP 2013555616 A JP2013555616 A JP 2013555616A JP 2014511383 A5 JP2014511383 A5 JP 2014511383A5
- Authority
- JP
- Japan
- Prior art keywords
- hsa
- medicament
- erbb2
- f5b6h2
- effective amount
- 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
- 239000007864 aqueous solution Substances 0.000 claims description 30
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 27
- 229960004891 lapatinib Drugs 0.000 claims description 27
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 27
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 claims description 26
- 239000000328 estrogen antagonist Substances 0.000 claims description 24
- 238000002648 combination therapy Methods 0.000 claims description 17
- 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 16
- 229960000575 trastuzumab Drugs 0.000 claims description 16
- 201000011510 cancer Diseases 0.000 claims description 14
- 229940122815 Aromatase inhibitor Drugs 0.000 claims description 12
- 239000003886 aromatase inhibitor Substances 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 9
- 229960003881 letrozole Drugs 0.000 claims description 9
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical group C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 9
- 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 8
- 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 8
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical group OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 claims description 8
- 229960004117 capecitabine Drugs 0.000 claims description 8
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 8
- 229960004316 cisplatin Drugs 0.000 claims description 8
- 229960002258 fulvestrant Drugs 0.000 claims description 8
- 229960001603 tamoxifen Drugs 0.000 claims description 8
- 229940102550 Estrogen receptor antagonist Drugs 0.000 claims description 7
- 230000001988 toxicity Effects 0.000 claims description 6
- 231100000419 toxicity Toxicity 0.000 claims description 6
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims description 5
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims description 5
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 5
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 5
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 5
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 5
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims description 5
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims description 5
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims description 5
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims description 5
- 229960001686 afatinib Drugs 0.000 claims description 5
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims description 5
- 229960002448 dasatinib Drugs 0.000 claims description 5
- 229960001433 erlotinib Drugs 0.000 claims description 5
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 5
- 229960002584 gefitinib Drugs 0.000 claims description 5
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 5
- 229960002411 imatinib Drugs 0.000 claims description 5
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims description 5
- 229960001346 nilotinib Drugs 0.000 claims description 5
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims description 5
- 229960000639 pazopanib Drugs 0.000 claims description 5
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims description 5
- 229960003787 sorafenib Drugs 0.000 claims description 5
- 229960001796 sunitinib Drugs 0.000 claims description 5
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims description 5
- 229940046836 anti-estrogen Drugs 0.000 claims description 4
- 230000001833 anti-estrogenic effect Effects 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 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 3
- 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 3
- 229960003437 aminoglutethimide Drugs 0.000 claims description 3
- 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 3
- 229960002932 anastrozole Drugs 0.000 claims description 3
- 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 3
- 230000008406 drug-drug interaction Effects 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 3
- 229960000255 exemestane Drugs 0.000 claims description 3
- 229950011548 fadrozole Drugs 0.000 claims description 3
- 229960004421 formestane Drugs 0.000 claims description 3
- 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 3
- 150000002596 lactones Chemical class 0.000 claims description 3
- 229960001592 paclitaxel Drugs 0.000 claims description 3
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 3
- 238000012360 testing method Methods 0.000 claims description 3
- 229930012538 Paclitaxel Natural products 0.000 claims description 2
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 claims description 2
- 238000012986 modification Methods 0.000 claims description 2
- 230000004048 modification Effects 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 32
- 150000001413 amino acids Chemical group 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 206010013710 Drug interaction Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000002939 deleterious effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 1
- 238000000034 method Methods 0.000 description 35
- 210000004027 cell Anatomy 0.000 description 25
- 239000002609 medium Substances 0.000 description 9
- 125000003275 alpha amino acid group Chemical group 0.000 description 6
- 238000011260 co-administration Methods 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 6
- 238000004113 cell culture Methods 0.000 description 5
- 230000010261 cell growth Effects 0.000 description 5
- 230000001640 apoptogenic effect Effects 0.000 description 4
- 230000004663 cell proliferation Effects 0.000 description 4
- 239000003104 tissue culture media Substances 0.000 description 4
- 239000000654 additive Substances 0.000 description 3
- 230000000996 additive effect Effects 0.000 description 3
- 230000006907 apoptotic process Effects 0.000 description 2
- 230000012010 growth Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- 108010058566 130-nm albumin-bound paclitaxel Proteins 0.000 description 1
- 229940123237 Taxane Drugs 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940044683 chemotherapy drug Drugs 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161446326P | 2011-02-24 | 2011-02-24 | |
| US61/446,326 | 2011-02-24 | ||
| US201161470848P | 2011-04-01 | 2011-04-01 | |
| US61/470,848 | 2011-04-01 | ||
| PCT/US2012/026602 WO2012116317A2 (en) | 2011-02-24 | 2012-02-24 | Combination therapies comprising anti-erbb3 agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014511383A JP2014511383A (ja) | 2014-05-15 |
| JP2014511383A5 true JP2014511383A5 (enExample) | 2015-04-16 |
Family
ID=46721477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013555616A Pending JP2014511383A (ja) | 2011-02-24 | 2012-02-24 | 抗ＥｒｂＢ３剤を含む併用療法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20140056898A1 (enExample) |
| EP (1) | EP2678359A4 (enExample) |
| JP (1) | JP2014511383A (enExample) |
| KR (1) | KR20140053865A (enExample) |
| CN (1) | CN103547598A (enExample) |
| AU (1) | AU2012222094A1 (enExample) |
| BR (1) | BR112013021660A2 (enExample) |
| CA (1) | CA2828099A1 (enExample) |
| IL (1) | IL228095A0 (enExample) |
| MX (1) | MX2013009732A (enExample) |
| WO (1) | WO2012116317A2 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ579644A (en) | 2007-02-16 | 2012-05-25 | Merrimack Pharmaceuticals Inc | Antibodies against erbb3 and uses thereof |
| US8895001B2 (en) | 2010-03-11 | 2014-11-25 | Merrimack Pharmaceuticals, Inc. | Use of ErbB3 inhibitors in the treatment of triple negative and basal-like breast cancers |
| EP2815765A1 (en) * | 2011-03-15 | 2014-12-24 | Merrimack Pharmaceuticals, Inc. | Overcoming resistance to ERBB pathway inhibitors |
| WO2013170263A2 (en) * | 2012-05-11 | 2013-11-14 | Merrimack Pharmaceuticals, Inc. | Dosage and administration of bispecific scfv conjugates in combination with anti-cancer therapeutics |
| WO2015100459A2 (en) | 2013-12-27 | 2015-07-02 | Merrimack Pharmaceuticals, Inc. | Biomarker profiles for predicting outcomes of cancer therapy with erbb3 inhibitors and/or chemotherapies |
| DK3805268T3 (da) | 2014-02-28 | 2025-01-20 | Merus Nv | Antistof, der binder erbb-2 og erbb-3 |
| CA2941030C (en) | 2014-02-28 | 2025-05-13 | Merus N.V. | ANTIBODIES THAT BIND TO EGFR AND ERBB3 |
| US10184006B2 (en) | 2015-06-04 | 2019-01-22 | Merrimack Pharmaceuticals, Inc. | Biomarkers for predicting outcomes of cancer therapy with ErbB3 inhibitors |
| JP7296728B2 (ja) | 2015-10-23 | 2023-06-23 | メルス ナムローゼ フェンノートシャップ | 癌の成長を抑制する結合分子 |
| ES2971286T3 (es) * | 2016-12-01 | 2024-06-04 | Oxford BioDynamics PLC | Aplicación de interacciones cromosómicas epigenéticas en diagnóstico de cáncer |
| JP7737220B2 (ja) | 2017-03-31 | 2025-09-10 | メルス ナムローゼ フェンノートシャップ | ＮＲＧ１融合遺伝子を有する細胞の処置における使用のためのＥｒｂＢ－２及びＥｒｂＢ３結合二重特異性抗体 |
| EP3625264B9 (en) * | 2017-05-17 | 2023-10-25 | Merus N.V. | Combination of an erbb-2/erbb-3 bispecific antibody with endocrine therapy for breast cancer |
| RS66708B9 (sr) | 2017-08-09 | 2025-08-29 | Merus Nv | Antitela koja se vezuju za egfr i cmet |
| US20230121116A1 (en) * | 2020-01-29 | 2023-04-20 | Board Of Regents, The University Of Texas System | Use of quinazoline-based tyrosine kinase inhibitors for the treatment of cancers with nrg1 fusions |
| JP7767613B2 (ja) | 2021-11-15 | 2025-11-11 | システィミューン，インコーポレイテッド | 二重特異性抗体－カンプトテシン薬物複合体及びその製薬的使用 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102282168A (zh) * | 2008-11-18 | 2011-12-14 | 梅里麦克制药股份有限公司 | 人血清白蛋白接头以及其结合物 |
| AU2011341337A1 (en) * | 2010-12-10 | 2013-06-13 | Merrimack Pharmaceuticals, Inc. | Dosage and administration of bispecific scFv conjugates |
-
2012
- 2012-02-24 CA CA2828099A patent/CA2828099A1/en not_active Abandoned
- 2012-02-24 AU AU2012222094A patent/AU2012222094A1/en not_active Abandoned
- 2012-02-24 CN CN201280019977.7A patent/CN103547598A/zh active Pending
- 2012-02-24 KR KR1020137025188A patent/KR20140053865A/ko not_active Withdrawn
- 2012-02-24 US US14/001,448 patent/US20140056898A1/en not_active Abandoned
- 2012-02-24 BR BR112013021660A patent/BR112013021660A2/pt not_active IP Right Cessation
- 2012-02-24 WO PCT/US2012/026602 patent/WO2012116317A2/en not_active Ceased
- 2012-02-24 MX MX2013009732A patent/MX2013009732A/es not_active Application Discontinuation
- 2012-02-24 JP JP2013555616A patent/JP2014511383A/ja active Pending
- 2012-02-24 EP EP12749889.7A patent/EP2678359A4/en not_active Withdrawn
-
2013
- 2013-08-22 IL IL228095A patent/IL228095A0/en unknown
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