Drug intelligence / Profile preview

fedratinib

Development stage
Approved
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Fedratinib is an oral small molecule kinase inhibitor used to treat adults with intermediate-2 or high-risk primary or secondary myelofibrosis, including post-polycythemia vera and post-essential thrombocythemia myelofibrosis. It works by selectively inhibiting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3), which are involved in abnormal signaling pathways that drive the proliferation of malignant cells in myeloproliferative neoplasms. By blocking these kinases, fedratinib reduces phosphorylation of STAT3/5 proteins, inhibits cell proliferation, induces apoptosis in mutated JAK2 and FLT3 cell lines, and helps control symptoms such as splenomegaly and constitutional symptoms associated with myelofibrosis. Fedratinib was originally discovered at TargeGen; its development continued through Sanofi-Aventis, Impact Biomedicines, Celgene Corporation, and now Bristol Myers Squibb[1][5][6][7][8].

Brand names
Inrebic
Other names
fedratinib hydrochloride
02

Targets

TYK2 (Tyrosine kinase 2)KCNH2 (Voltage-gated potassium channel subfamily H member 2)JAK2 (Janus kinase 2)JAK1 (Janus kinase 1)JAK3 (Janus kinase 3)FLT3 (Fms related receptor tyrosine kinase 3)

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