Drug intelligence / Profile preview

zunsemetinib

Development stage
Phase 2
Lead developer
Aclaris Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Zunsemetinib is an orally bioavailable small molecule inhibitor of mitogen‐activated protein kinase‐activated protein kinase 2 (MK2). It was originally developed by Confluence Life Sciences and further developed by Aclaris Therapeutics and Washington University School of Medicine. Zunsemetinib selectively targets the p38α-MK2 pathway, leading to inhibition of multiple pro-inflammatory cytokines and chemokines such as TNFα, IL1α, IL1β, IL6, IL8 and IL17. This mechanism is intended to mitigate inflammatory responses in diseases like rheumatoid arthritis and other immuno-inflammatory conditions. The drug has been investigated for several indications including rheumatoid arthritis, hidradenitis suppurativa, psoriatic arthritis, COVID‑19 infection, cryopyrin-associated periodic syndromes (CAPS), psoriasis and metastatic HER‑negative breast cancer with bone metastasis[1][3][5][6].

Other names
zunsemetinib [INN]zunsemetinib [USAN](1(2H),4'-bipyridin)-2-one, 3-chloro-4-((3,5-difluoro-2-pyridinyl)methoxy)-2'-(2-(1-hydroxy-1-methylethyl)-4-pyrimidinyl)-5',6-dimethyl-, (-)-(p)-3-chloro-4-((3,5-difluoropyridin-2 yl)methoxy)-2'-(2-(2-hydroxypropan 2 yl)pyrimidin 4 yl)-5',6-dimethyl 2h (1,4'-bipyridin) 2 oneUNII: AX2VWG0ZCR
02

Targets

MK2 (Mitogen-activated protein kinase-activated protein kinase 2)

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