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

Authors Hatzimichael E, Tsolas E, Briasoulis E

Received 31 March 2014

Accepted for publication 24 May 2014

Published 19 August 2014 Volume 2014:5 Pages 143—152


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Eleftheria Hatzimichael, Evangelos Tsolas, Evangelos Briasoulis

Department of Haematology, University Hospital of Ioannina, Ioannina, Greece

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.

Keywords: pacritinib, SB-1518, JAK inhibitors, myeloproliferative neoplasms, acute myeloid leukemia, lymphoma, treatment

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