Drug intelligence / Profile preview

EP31670 + momelotinib

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

EP31670 + momelotinib is an investigational combination therapy being evaluated for the treatment of myelofibrosis. Momelotinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/JAK2) and activin A receptor type 1 (ACVR1/ALK2), which is already approved for the treatment of myelofibrosis patients with anemia. EP31670 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) proteins, which are epigenetic readers that regulate the expression of genes involved in inflammation and cell proliferation. The combination aims to provide synergistic effects by simultaneously targeting the JAK/STAT signaling pathway and the epigenetic regulation of pro-inflammatory and pro-fibrotic genes, potentially addressing the underlying disease drivers and improving clinical outcomes such as spleen volume reduction and symptom control in patients with myelofibrosis.

Other names
EP31670 + momelotinibmomelotinib + EP31670
02

Targets

ACVR1 (Activin receptor type I)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)JAK3 (Janus kinase 3)TYK2 (Tyrosine kinase 2)BRD4 (Bromodomain-containing protein 4)

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