Profile of pacritinib and its potential in the treatment of hematologic disorders.

Abstract

Pacritinib (previously known as SB-1518) is an innovative selective inhibitor of Janus kinase 2 and FMS-related tyrosine kinase 3 providing potential in the treatment of hematological malignancies such as myeloproliferative neoplasias, acute myeloid leukemia, and various lymphomas. Pacritinib has potent antiproliferative activity in Janus kinase 2 and/or FMS-related tyrosine kinase 3 activity-dependent cell lines and an ability to promote apoptosis and inhibit the signal transducers and activators of transcription (STAT) pathway. Pharmacokinetic studies have indicated a good per os bioavailability and favorable kinetic parameters. To date, promising results have been produced in five completed early-phase clinical trials in which pacritinib has been studied. Pacritinib displayed interesting activity and an acceptable safety profile, with mild to moderate gastrointestinal disorders being its most common adverse effects.

• Authors: Eleftheria Hatzimichael, Evangelos Tsolas, Evangelos Briasoulis
• Journal: Journal of blood medicine (J Blood Med) Vol. 5 Pg. 143-52 ( 2014) ISSN: 1179-2736 [Print] New Zealand
• PMID: 25170285 (Publication Type: Journal Article, Review)