İmatinib: etki mekanizması ve direnç geliştirme mekanizmaları

Abstract

Keywords

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İmatinib: Etki Mekanizması ve Direnç Geliștirme Mekanizmaları

Abstract

İmatinib, kronik miyelojen lösemi (KML) tedavisinde kullanıma girmiș spesifik bir ilaç olarak tıpta adeta bir devrim yaratmıștır. İmatinib mesylate (Glivec), 2-phenylaminopyrimidine’in bir türevidir. KML tedavisinde kullanılması için 2001 yılında FDA tarafından onay almıștır. Türkiye’de ise KML ve gastrointestinal stromal tümörler (GİSTs) tedavisinde kullanılması için 2003 yılında onay almıștır. İmatinib abl, c-kit ve PDGF-R bağlı spesifik bir tirozin kinaz kinaz inhibitörü olarak geliștirilmiștir. Erken faz KML hastalarda imatinib çok yüksek bașarı göstermesine rağmen, ileri faz KML hastalarda imatinibe karșı gelișen direnç nedeniyle bașarı oranı azalmıștır. Bcr-abl kinaz bölgesinde mutasyonlar, gelișen direncin en önemli nedeni olarak görülmektedir. İmatinibin terapötik etkisini arttırmak ve gelișen direnci kırmak amacıyla birçok çalıșma yapılmaktadır, zira imatinib gelecekte birçok hastalığın tedavisi için umut vericidir.

Keywords

• imatinib, tirozin kinaz, abl, c-kit, PDGF-R

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