İmatinib: etki mekanizması ve direnç geliştirme mekanizmaları

Year 2012, Volume: 65 Issue: 2, 77 - 82, 01.02.2012

M. Merve Tuğlu Mehmet Melli

https://doi.org/10.1501/Tipfak_0000000813

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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