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BMS-986158 + fedratinib

Development stage: Unknown
Lead developer: Bristol Myers Squibb
Modality: Small Molecules
Administration: Oral

Overview

BMS-986158 + fedratinib is an investigational **combination therapy** being studied for intermediate- or high-risk myelofibrosis. BMS-986158 is an orally bioavailable, potent, and selective small-molecule BET (bromodomain and extra-terminal domain) inhibitor that modulates gene expression via epigenetic mechanisms. Fedratinib is an oral, selective Janus kinase 2 (JAK2) inhibitor approved for myelofibrosis. The combination targets two distinct pathways—BET-regulated transcription and JAK-STAT signaling—to enhance disease modification. Trials show acceptable safety and preliminary efficacy in patients refractory, relapsed, or intolerant to prior ruxolitinib (another JAK inhibitor), with endpoints including spleen volume reduction and modulation of JAK2 variant allele frequency[1][3][5][7].

Brand names: Inrebic (fedratinib)
Other names: BMS-986158 + fedratinib

Targets

BRD (Bromodomain-containing protein family)JAK2 (Janus kinase 2)

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