JP2014533272A5 - - Google Patents
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- JP2014533272A5 JP2014533272A5 JP2014541283A JP2014541283A JP2014533272A5 JP 2014533272 A5 JP2014533272 A5 JP 2014533272A5 JP 2014541283 A JP2014541283 A JP 2014541283A JP 2014541283 A JP2014541283 A JP 2014541283A JP 2014533272 A5 JP2014533272 A5 JP 2014533272A5
- Authority
- JP
- Japan
- Prior art keywords
- mutation
- formula
- braf
- treatment
- agent
- 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.)
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- 102100004328 BRAF Human genes 0.000 claims description 11
- 101700004551 BRAF Proteins 0.000 claims description 11
- 230000035772 mutation Effects 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 8
- 230000002062 proliferating Effects 0.000 claims description 8
- 239000003112 inhibitor Substances 0.000 claims description 7
- 230000002401 inhibitory effect Effects 0.000 claims description 7
- 206010025650 Malignant melanoma Diseases 0.000 claims description 4
- 201000011231 colorectal cancer Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 229940079593 drugs Drugs 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
Description
結果を図1に示す。耐性は、式IIの化合物を連続投与されたすべてのマウスにおいて出現したが、間欠的投薬計画の対象になったマウスにおいて耐性の証拠はない。
本発明は以下の態様を包含し得る。
[1] BRAFキナーゼの突然変異を特徴とする増殖性疾患を治療する方法であって、間欠的投薬計画に従って式II
のBRAF阻害剤を投与することによって、式IIのBRAF阻害剤による治療に対する耐性を抑制するステップを含む、方法。
[2] BRAF突然変異がV600突然変異である、請求項1に記載の方法。
[3] 増殖性疾患が、V600突然変異を特徴とする黒色腫、またはV600突然変異を特徴とする結腸直腸癌である、請求項1に記載の方法。
[4] 増殖性疾患が、BRAFV600Eを特徴とする黒色腫、またはBRAFV600Eを特徴とする結腸直腸癌である、請求項1に記載の方法。
[5] 式II
のBRAF阻害剤の使用であって、前記BRAF阻害剤を間欠的投薬計画に従って投与することによる増殖性疾患の治療のための薬剤を調製するための、使用。
本発明は以下の態様を包含し得る。
[1] BRAFキナーゼの突然変異を特徴とする増殖性疾患を治療する方法であって、間欠的投薬計画に従って式II
[2] BRAF突然変異がV600突然変異である、請求項1に記載の方法。
[3] 増殖性疾患が、V600突然変異を特徴とする黒色腫、またはV600突然変異を特徴とする結腸直腸癌である、請求項1に記載の方法。
[4] 増殖性疾患が、BRAFV600Eを特徴とする黒色腫、またはBRAFV600Eを特徴とする結腸直腸癌である、請求項1に記載の方法。
[5] 式II
Claims (5)
- BRAF突然変異がV600突然変異である、請求項1に記載の薬剤。
- 増殖性疾患が、V600突然変異を特徴とする黒色腫、またはV600突然変異を特徴とする結腸直腸癌である、請求項1に記載の薬剤。
- 増殖性疾患が、BRAFV600Eを特徴とする黒色腫、またはBRAFV600Eを特徴とする結腸直腸癌である、請求項1に記載の薬剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161558619P | 2011-11-11 | 2011-11-11 | |
US61/558,619 | 2011-11-11 | ||
PCT/US2012/064269 WO2013070996A1 (en) | 2011-11-11 | 2012-11-09 | Method of treating a proliferative disease |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2014533272A JP2014533272A (ja) | 2014-12-11 |
JP2014533272A5 true JP2014533272A5 (ja) | 2015-12-24 |
JP6150813B2 JP6150813B2 (ja) | 2017-06-21 |
Family
ID=47279036
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2014541283A Active JP6150813B2 (ja) | 2011-11-11 | 2012-11-09 | 増殖性疾患の治療方法 |
Country Status (11)
Country | Link |
---|---|
US (1) | US11007194B2 (ja) |
EP (1) | EP2776037B1 (ja) |
JP (1) | JP6150813B2 (ja) |
CN (2) | CN108542906A (ja) |
AU (1) | AU2012335663B2 (ja) |
BR (1) | BR112014011223A8 (ja) |
CA (1) | CA2855243C (ja) |
HK (1) | HK1198920A1 (ja) |
MX (1) | MX354725B (ja) |
RU (1) | RU2622015C2 (ja) |
WO (1) | WO2013070996A1 (ja) |
Families Citing this family (7)
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AR092045A1 (es) * | 2012-08-07 | 2015-03-18 | Novartis Ag | Combinaciones farmaceuticas |
CN109890386B (zh) * | 2016-06-03 | 2022-05-24 | 阵列生物制药公司 | 药物组合 |
US11590133B2 (en) * | 2016-12-11 | 2023-02-28 | Memorial Sloan Kettering Cancer Center | Methods and compositions for treatment of BRAF mutant cancers |
US12076320B2 (en) | 2018-07-12 | 2024-09-03 | Shenzhen Targetrx, Inc. | Diarylpyrazole compound, composition comprising same, and use thereof |
TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療braf相關的疾病和失調症之化合物 |
WO2023230554A1 (en) | 2022-05-25 | 2023-11-30 | Pfizer Inc. | Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer |
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-
2012
- 2012-11-09 CN CN201810135736.8A patent/CN108542906A/zh active Pending
- 2012-11-09 EP EP12795175.4A patent/EP2776037B1/en active Active
- 2012-11-09 BR BR112014011223A patent/BR112014011223A8/pt not_active Application Discontinuation
- 2012-11-09 CN CN201280054663.0A patent/CN103917236A/zh active Pending
- 2012-11-09 MX MX2014005726A patent/MX354725B/es active IP Right Grant
- 2012-11-09 CA CA2855243A patent/CA2855243C/en active Active
- 2012-11-09 US US14/355,903 patent/US11007194B2/en active Active
- 2012-11-09 RU RU2014117707A patent/RU2622015C2/ru active
- 2012-11-09 JP JP2014541283A patent/JP6150813B2/ja active Active
- 2012-11-09 AU AU2012335663A patent/AU2012335663B2/en active Active
- 2012-11-09 WO PCT/US2012/064269 patent/WO2013070996A1/en active Application Filing
-
2014
- 2014-12-10 HK HK14112437.0A patent/HK1198920A1/xx unknown
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