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Drugs Today (Barc) ; 50(2): 113-20, 2014 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-24619588

RESUMEN

Idelalisib is a novel, highly selective, small-molecule, tyrosine kinase inhibitor with potent activity against phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kδ). Given the highly selective inhibition of this compound, studies have shown that idelalisib is able to achieve significantly increased apoptotic activity in B-cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL) cell lines, without significant increase in apoptosis among normal T and natural killer cells. Recent studies have suggested potential clinical benefit with idelalisib as either a single agent or in combination with established chemotherapeutic compounds including bendamustine and rituximab in relapsed/refractory CLL. This review will focus on the preclinical pharmacology, pharmacokinetics and clinical utility of idelalisib in the treatment of various indolent forms of non-Hodgkin's lymphoma.


Asunto(s)
Fosfatidilinositol 3-Quinasa Clase Ia/uso terapéutico , Linfoma no Hodgkin/tratamiento farmacológico , Purinas/uso terapéutico , Quinazolinonas/uso terapéutico , Animales , Fosfatidilinositol 3-Quinasa Clase Ia/farmacocinética , Fosfatidilinositol 3-Quinasa Clase Ia/farmacología , Ensayos Clínicos Fase I como Asunto , Ensayos Clínicos Fase II como Asunto , Ensayos Clínicos Fase III como Asunto , Humanos , Purinas/metabolismo , Purinas/farmacocinética , Purinas/farmacología , Quinazolinonas/metabolismo , Quinazolinonas/farmacocinética , Quinazolinonas/farmacología
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