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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

Mechanism

HDAC3 inhibitors(Histone deacetylase 3 inhibitors), HDAC6 inhibitors(Histone deacetylase 6 inhibitors), JAK1 inhibitors(Tyrosine-protein kinase JAK1 inhibitors)

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Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

China Pharmaceutical University

Active Organization

China Pharmaceutical University

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Psoriasis is a common, chronic, recurrent, and inflammatory skin disease, which causes physical and psychological problems in patients and lacks effective and economic therapeutics. Herein, we designed Janus kinase (JAK) and histone deacetylase (HDAC) dual inhibitors as a new strategy for the treatment of psoriasis. In particular, compound 11i was identified with excellent inhibitory activity toward JAKs (JAK2 IC₅₀ = 0.49 nM) and HDACs (HDAC6 IC₅₀ = 12 nM). Moreover, it exhibited potent activities in inhibiting the proliferation of TNF-α-induced HaCAT cells and the production of nitric oxide. Importantly, compound 11i significantly ameliorated psoriasis-like skin lesions in an imiquimod-induced murine model with low toxicity, which was superior to JAK inhibitor momelotinib, HDAC inhibitor vorinostat, and their combination. This work provided a proof-of-concept for JAK/HDAC dual inhibitors as a promising strategy for the treatment of psoriasis.

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