Drug intelligence / Profile preview

BMS-986158 + ruxolitinib

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

Overview

**BMS-986158 + ruxolitinib** is an experimental combination therapy composed of **BMS-986158**, a selective, orally bioavailable small-molecule bromodomain and extra-terminal (BET) inhibitor, and **ruxolitinib**, a Janus kinase (JAK) 1/2 inhibitor. BMS-986158 modulates gene expression through epigenetic inhibition of BET proteins (such as BRD2, BRD3, BRD4), which play vital roles in cell proliferation, inflammation, and oncogenic signaling, while ruxolitinib inhibits aberrant JAK-STAT pathway signaling by blocking JAK1 and JAK2 kinases. The combination is under clinical investigation, particularly for its enhanced efficacy in patients with intermediate- or high-risk myelofibrosis (a bone marrow cancer), by targeting two complementary pathogenic pathways—epigenetic regulation (BET) and cytokine signaling (JAK-STAT)—to improve clinical responses and disease control[1][3][5][7].

Brand names
Jakafi
Other names
BMS-986158 combined with ruxolitinibBMS986158 combined with ruxolitinibBMS 986158 combined with ruxolitinib
02

Targets

TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)BRD4 (Bromodomain-containing protein 4)JAK3 (Janus kinase 3)BRDT (Bromodomain testis-specific protein)JAK1 (Janus kinase 1)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)

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