Drug intelligence / Profile preview

fedratinib + efavirenz

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

**fedratinib + efavirenz** is a combination of two drugs: **fedratinib**, an orally administered, selective inhibitor of Janus kinase 2 (JAK2) used primarily to treat adult patients with intermediate-2 or high-risk primary or secondary myelofibrosis; and **efavirenz**, a non-nucleoside reverse transcriptase inhibitor (NNRTI) commonly used as part of antiretroviral therapy for HIV infection. The combination of these two drugs is not used as a marketed therapy but may occur as a result of co-administration for patients who require both treatments. When efavirenz is co-administered with fedratinib, efavirenz induces CYP3A4, resulting in a significant reduction (about 47–50%) in fedratinib exposure, potentially reducing its efficacy. This interaction is considered clinically significant, and co-administration should generally be avoided.

Other names
RZA-CHW-FedratinibDMP 266DMP266DMP-266
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseJAK1 (Janus kinase 1)JAK2 (Janus kinase 2)JAK2 JH2 (Janus kinase 2 (JAK2) JH2 pseudokinase domain)JAK3 (Janus kinase 3)TYK2 (Tyrosine kinase 2)

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