Новое поколение ингибиторов тирозинкиназы: афатиниб

Новое поколение ингибиторов тирозинкиназы: афатиниб

Автор: Большакова С.А., Бычков Ю.М.

Журнал: Вестник Российского научного центра рентгенорадиологии Минздрава России @vestnik-rncrr

Рубрика: Обзоры

Статья в выпуске: 3 т.18, 2018 года.

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Резюме Препараты первого поколения обратимых ингибиторов тирозинкиназы (ТК) рецепторов эпидермального фактора роста (EGFR) - эрлотиниб и гефитиниб являются важной вехой в лечении немелкоклеточного рака легкого (НМРЛ) при наличии активирующих EGFR мутаций. У пациентов возможно развитие резистентности к этим препаратам. Существует гипотеза, что появление второго поколения ингибиторов с большим блокирующим спектром может удлинить время клинической эффективности и преодолеть возникшую резистентность к ингибиторам ТК первого поколения. Афатиниб относится ко второму поколению ингибиторов ТК и является необратимым блокатором семейства ErbB. Он связывается со всеми гомодимерами и гетеродимерами, образованными EGFR, рецепторами человеческого эпидерамального фактора роста (HER-2), HER-3 и HER-4 29 рецепторами. Афатиниб продемонстрировал клиническую активность у пациентов с НМРЛ, у которых было выявлено прогрессирование заболевания при приеме эрлотиниба/гефитиниба, особенно в комбинации с цетуксимабом, а также в комбинации с паклитакселом при сравнении с группой химиотерапии. Эффективность афатиниба, как в первой линии лечения, так и при возникновении рецидива/рефрактерности может быть связана с его способностью необратимо блокировать все формы, относящиеся к семейству ErbB. Афатиниб имеет удовлетворительный профиль токсичности, характерными побочными проявлениями являются гастроинтестинальная и кожная токсичность.

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Немелкоклеточный рак легкого, рецептор эпидермального фактора роста, ингибитор тирозинкиназы

Короткий адрес: https://sciup.org/149132070

IDR: 149132070

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