RU2015137596A - The combination of an EGFR inhibitor T790M and an EGFR inhibitor for the treatment of non-small cell lung cancer - Google Patents

The combination of an EGFR inhibitor T790M and an EGFR inhibitor for the treatment of non-small cell lung cancer Download PDF

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RU2015137596A
RU2015137596A RU2015137596A RU2015137596A RU2015137596A RU 2015137596 A RU2015137596 A RU 2015137596A RU 2015137596 A RU2015137596 A RU 2015137596A RU 2015137596 A RU2015137596 A RU 2015137596A RU 2015137596 A RU2015137596 A RU 2015137596A
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egfr
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Зеланна Айрис ГОЛДБЕРГ
Джон Чарльз Кэт
Стивен Пол ЛЕТРЕНТ
Скотт Лоуренс ВАЙНРИХ
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Claims (30)

1. Способ лечения немелкоклеточного рака легкого, включающий введение пациенту, нуждающемуся в этом, эффективного количества необратимого ингибитора EGFR Т790М (рецептор эпидермального фактора роста с мутацией Т790М) в комбинации с эффективным количеством ингибитора EGFR.1. A method of treating non-small cell lung cancer, comprising administering to a patient in need thereof an effective amount of an irreversible EGFR T790M inhibitor (epidermal growth factor receptor with a T790M mutation) in combination with an effective amount of an EGFR inhibitor. 2. Способ по п. 1, где необратимый ингибитор EGFR Т790М представляет собой 1-{(3R,4R)-3-[({5-хлор-2-[(1-метил-1H-пиразол-4-ил)амино]-7H-пирроло[2,3-d]пиримидин-4-ил}окси)метил]-4-метоксипирролидин-1-ил}проп-2-ен-1-он или его фармацевтически приемлемую соль.2. The method according to claim 1, where the irreversible EGFR T790M inhibitor is 1 - {(3R, 4R) -3 - [({5-chloro-2 - [(1-methyl-1H-pyrazol-4-yl) amino ] -7H-pyrrolo [2,3-d] pyrimidin-4-yl} oxy) methyl] -4-methoxypyrrolidin-1-yl} prop-2-en-1-one or a pharmaceutically acceptable salt thereof. 3. Способ по п. 1 или 2, где ингибитор EGFR выбран из группы, состоящей из гефитиниба, эрлотиниба, икотиниба, вандетаниба, лапатиниба, нератиниба, афатиниба, пелитиниба, дакомитиниба, канертиниба, цетуксимаба и панитумумаба или их фармацевтически приемлемой соли.3. The method according to claim 1 or 2, wherein the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, icotinib, vandetanib, lapatinib, neratinib, afatinib, pelitinib, dacomitinib, canertinib, cetuximab and panitumumab, or a pharmaceutically acceptable salt thereof. 4. Способ по п. 1 или 2, где ингибитор EGFR выбран из группы, состоящей из гефитиниба, эрлотиниба, афатиниба и дакомитиниба или их фармацевтически приемлемой соли.4. The method of claim 1 or 2, wherein the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, afatinib, and dacomitinib, or a pharmaceutically acceptable salt thereof. 5. Способ по п. 1 или 2, где ингибитор EGFR представляет собой эрлотиниб или его фармацевтически приемлемую соль.5. The method of claim 1 or 2, wherein the EGFR inhibitor is erlotinib or a pharmaceutically acceptable salt thereof. 6. Способ по п. 1 или 2, где ингибитор EGFR представляет собой дакомитиниб или его фармацевтически приемлемую соль.6. The method of claim 1 or 2, wherein the EGFR inhibitor is dacomitinib or a pharmaceutically acceptable salt thereof. 7. Способ лечения немелкоклеточного рака легкого, включающий введение пациенту, нуждающемуся в этом, эффективного количества ингибитора EGFR Т790М в комбинации с ингибитором panHER (панингибитор рецепторов эпидермального фактора роста человека), где ингибитор panHER вводят в соответствии с нестандартным клиническим режимом дозирования.7. A method of treating non-small cell lung cancer, comprising administering to a patient in need thereof, an effective amount of an EGFR T790M inhibitor in combination with a panHER inhibitor (pan-human epidermal growth factor receptor panhibitor), wherein the panHER inhibitor is administered in accordance with a non-standard clinical dosage regimen. 8. Способ по п. 7, где нестандартный клинический режим дозирования представляет собой нестандартную клиническую дозу или нестандартную схему дозирования.8. The method of claim 7, wherein the non-standard clinical dosage regimen is a non-standard clinical dose or a non-standard dosage regimen. 9. Способ по п. 7, где нестандартный клинический режим дозирования представляет собой низкую дозу ингибитора panHER.9. The method of claim 7, wherein the non-standard clinical dosage regimen is a low dose panHER inhibitor. 10. Способ по п. 7, где нестандартный клинический режим дозирования представляет собой прерывистый режим дозирования.10. The method of claim 7, wherein the non-standard clinical dosage regimen is an intermittent dosage regimen. 11. Способ по любому из пп. 7-10, где ингибитор EGFR Т790М выбран из группы, состоящей из Go6976, PKC412, АР26113, НМ61713, WZ4002, СО-1686 и TAS-2913 или их фармацевтически приемлемой соли.11. The method according to any one of paragraphs. 7-10, where the EGFR T790M inhibitor is selected from the group consisting of Go6976, PKC412, AP26113, HM61713, WZ4002, CO-1686 and TAS-2913 or a pharmaceutically acceptable salt thereof. 12. Способ по любому из пп. 7-10, где ингибитор EGFR Т790М представляет собой 1-{(3R,4R)-3-[({5-хлор-2-[(1-метил-1Н-пиразол-4-ил)амино]-7Н-пирроло[2,3-d]пиримидин-4-ил}окси)метил]-4-метоксипирролидин-1-ил}проп-2-ен-1-он или его фармацевтически приемлемую соль.12. The method according to any one of paragraphs. 7-10, where the EGFR T790M inhibitor is 1 - {(3R, 4R) -3 - [({5-chloro-2 - [(1-methyl-1H-pyrazol-4-yl) amino] -7H-pyrrolo [2,3-d] pyrimidin-4-yl} oxy) methyl] -4-methoxypyrrolidin-1-yl} prop-2-en-1-one or a pharmaceutically acceptable salt thereof. 13. Способ по любому из пп. 7-10, где ингибитор panHER выбран из группы, состоящей из лапатиниба, нератиниба, афатиниба, пелитиниба, дакомитиниба и канертиниба или его фармацевтически приемлемой соли.13. The method according to any one of paragraphs. 7-10, where the panHER inhibitor is selected from the group consisting of lapatinib, neratinib, afatinib, pelitinib, dacomitinib and canterinib, or a pharmaceutically acceptable salt thereof. 14. Способ по любому из пп. 7-10, где ингибитор panHER представляет собой афатиниб или его фармацевтически приемлемую соль.14. The method according to any one of paragraphs. 7-10, where the panHER inhibitor is afatinib or a pharmaceutically acceptable salt thereof. 15. Способ по любому из пп. 7-10, где ингибитор panHER представляет собой дакомитиниб или его фармацевтически приемлемую соль.15. The method according to any one of paragraphs. 7-10, wherein the panHER inhibitor is dacomitinib or a pharmaceutically acceptable salt thereof. 16. Способ лечения немелкоклеточного рака легкого, включающий введение пациенту, нуждающемуся в этом, синергического количества ингибитора EGFR Т790М в комбинации с ингибитором EGFR.16. A method of treating non-small cell lung cancer, comprising administering to a patient in need thereof a synergistic amount of an EGFR T790M inhibitor in combination with an EGFR inhibitor. 17. Способ по п. 16, где ингибитор EGFR Т790М выбран из группы, состоящей из Go6976, PKC412, АР26113, НМ61713, WZ4002, СО-1686 и TAS-2913 или их фармацевтически приемлемой соли.17. The method of claim 16, wherein the EGFR T790M inhibitor is selected from the group consisting of Go6976, PKC412, AP26113, HM61713, WZ4002, CO-1686 and TAS-2913 or a pharmaceutically acceptable salt thereof. 18. Способ по п. 16, где ингибитор EGFR Т790М представляет собой 1-{(3R,4R)-3-[({5-хлор-2-[(1-метил-1H-пиразол-4-ил)амино]-7Н-пирроло[2,3-d]пиримидин-4-ил}окси)метил]-4-метоксипирролидин-1-ил}проп-2-ен-1-он или его фармацевтически приемлемую соль.18. The method according to p. 16, where the EGFR T790M inhibitor is 1 - {(3R, 4R) -3 - [({5-chloro-2 - [(1-methyl-1H-pyrazol-4-yl) amino] -7H-pyrrolo [2,3-d] pyrimidin-4-yl} oxy) methyl] -4-methoxypyrrolidin-1-yl} prop-2-en-1-one or a pharmaceutically acceptable salt thereof. 19. Способ по любому из пп. 16-18, где ингибитор EGFR выбран из группы, состоящей из гефитиниба, эрлотиниба, икотиниба, вандетаниба, лапатиниба, нератиниба, афатиниба, пелитиниба, дакомитиниба, канертиниба, цетуксимаба и панитумумаба или их фармацевтически приемлемой соли.19. The method according to any one of paragraphs. 16-18, where the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, icotinib, vandetanib, lapatinib, neratinib, afatinib, pelitinib, dacomitinib, canertinib, cetuximab and panitumumab or a pharmaceutically acceptable salt thereof. 20. Способ по любому из пп. 16-18, где ингибитор EGFR выбран из группы, состоящей из гефитиниба, эрлотиниба, афатиниба и дакомитиниба или его фармацевтически приемлемой соли.20. The method according to any one of paragraphs. 16-18, where the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, afatinib, and dacomitinib, or a pharmaceutically acceptable salt thereof. 21. Способ по любому из пп. 16-18, где ингибитор EGFR представляет собой эрлотиниб или его фармацевтически приемлемую соль.21. The method according to any one of paragraphs. 16-18, where the EGFR inhibitor is erlotinib or a pharmaceutically acceptable salt thereof. 22. Синергическая комбинация22. Synergistic combination а) ингибитора EGFR Т790М; иa) an EGFR T790M inhibitor; and б) ингибитора EGFR,b) an EGFR inhibitor, где компонент (а) и компонент (б) являются синергическими.where component (a) and component (b) are synergistic. 23. Комбинация по п. 22, где ингибитор EGFR Т790М выбран из группы, состоящей из Go6976, PKC412, АР26113, НМ61713, WZ4002, СО-1686 и TAS-2913 или их фармацевтически приемлемой соли.23. The combination of claim 22, wherein the EGFR T790M inhibitor is selected from the group consisting of Go6976, PKC412, AP26113, HM61713, WZ4002, CO-1686, and TAS-2913 or a pharmaceutically acceptable salt thereof. 24. Комбинация по п. 22, где ингибитор EGFR Т790М представляет собой 1-{(3R,4R)-3-[({5-хлор-2-[(1-метил-1H-пиразол-4-ил)амино]-7H-пироло[2,3-d]пиримидин-4-ил}окси)метил]-4-метоксипирролидин-1-ил}проп-2-ен-1-он или его фармацевтически приемлемую соль.24. The combination of claim 22, wherein the EGFR T790M inhibitor is 1 - {(3R, 4R) -3 - [({5-chloro-2 - [(1-methyl-1H-pyrazol-4-yl) amino] -7H-pyrolo [2,3-d] pyrimidin-4-yl} oxy) methyl] -4-methoxypyrrolidin-1-yl} prop-2-en-1-one or a pharmaceutically acceptable salt thereof. 25. Комбинация по любому из пп. 22-24, где ингибитор EGFR выбран из группы, состоящей из гефитиниба, эрлотиниба, икотиниба, вандетаниба, лапатиниба, нератиниба, афатиниба, пелитиниба, дакомитиниба, канертиниба, цетуксимаба и панитумумаба или их фармацевтически приемлемой соли.25. The combination according to any one of paragraphs. 22-24, wherein the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, icotinib, vandetanib, lapatinib, neratinib, afatinib, pelitinib, dacomitinib, canertinib, cetuximab and panitumumab or a pharmaceutically acceptable salt thereof. 26. Комбинация по любому из пп. 22-24, где ингибитор EGFR выбран из группы, состоящей из гефитиниба, эрлотиниба, афатиниба и дакомитиниба или их фармацевтически приемлемой соли.26. The combination according to any one of paragraphs. 22-24, where the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, afatinib and dacomitinib, or a pharmaceutically acceptable salt thereof. 27. Комбинация по любому из пп. 22-24, где ингибитор EGFR представляет собой эрлотиниб или его фармацевтически приемлемую соль.27. The combination according to any one of paragraphs. 22-24, wherein the EGFR inhibitor is erlotinib or a pharmaceutically acceptable salt thereof.
RU2015137596A 2013-03-14 2014-03-03 The combination of an EGFR inhibitor T790M and an EGFR inhibitor for the treatment of non-small cell lung cancer RU2015137596A (en)

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