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MODULATION OF SOME TYROZINKINASES
专利权人:
ИНК. (US);ТЕСАРО
发明人:
УИЛКОКСЕН Кейт М. (US)
申请号:
RU2014119150/15
公开号:
RU2014119150A
申请日:
2012.11.13
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. A method comprising the following step: administering a compound of formula I to a subject suffering from an ALK-related condition, wherein said subject exhibits one or more signs of resistance to an ALK inhibitor. 2. A method according to claim 1, wherein said one or more signs of resistance to an ALK inhibitor are selected from L1196M, R1275Q, F1174L, ELM4-ALK, NPM-ALK, and combinations thereof. A method according to claim 1 or 2, wherein said ALK inhibitor is krizotinib. A method according to claim 3, wherein the compound of formula I is administered in a dose selected from from about 50 mg to about 1200 mg. The method of claim 4, wherein the compound of formula I is administered one, two, three or four times a day. A method comprising the following step: administering to a subject suffering from or predisposed to a condition associated with ALK a compound of formula I in combination with an additional chemotherapeutic agent. The method of claim 6, wherein said additional chemotherapeutic agent is selected from the group consisting of docetaxel, pemetrexed, carboplatin, paclitaxel and cisplatin. A method according to claim 6 or 7, in which at least one of the compounds of formula I and the specified additional chemotherapeutic agent is administered at a dose less than if the only agent was administered. The method of claim 1 or 6, wherein said subject has a genetic marker associated with ALK selected from L1196M, R1275Q, F1174L, ELM4-ALK, NPM-ALK, and combinations thereof. The method of claim 9, wherein said genetic marker associated with ALK is detected by in situ fluorescence hybridization. The method of claim 6, wherein the subject has a marker associated with cryzotinib resistance. The method of claim 11, wherein said marker associated with mouth1. Способ, включающий следующую стадию:введение соединения формулы I субъекту, страдающему состоянием, связанным с ALK, где указанный субъект демонстрирует один или более признаков устойчивости к ингибитору ALK.2.
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