Drug intelligence / Profile preview

zasocitinib

Development stage
Phase 3
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Zasocitinib (TAK-279) is an investigational, oral, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2). Unlike traditional Janus kinase (JAK) inhibitors that target the orthosteric ATP-binding site, zasocitinib binds to the regulatory pseudokinase domain of TYK2. This allosteric mechanism provides exceptional selectivity for TYK2 over the closely related JAK1, JAK2, and JAK3 kinases, potentially minimizing off-target toxicities such as hematological abnormalities or lipid changes. By inhibiting TYK2, the drug modulates signaling pathways for key cytokines including interleukin-12 (IL-12), interleukin-23 (IL-23), and Type 1 interferons, which are central to the pathogenesis of various autoimmune and inflammatory conditions. Originally developed by Nimbus Therapeutics as NDI-034858, the asset was acquired by Takeda in 2023 and is currently being evaluated in late-stage clinical trials for plaque psoriasis and psoriatic arthritis, as well as Phase 2 studies for inflammatory bowel disease and systemic lupus erythematosus.

Other names
TAK-279TAK279TAK 279NDI-034858NDI034858NDI 034858
02

Targets

TYK2 (Tyrosine kinase 2)

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