Ligand id: 8315

Name: peficitinib

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 4
Rotatable bonds 3
Topological polar surface area 104.03
Molecular weight 326.17
XLogP 1.83
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Peficitinib is being assessed in Phase III clinical trial as a potential treatment for rheumatoid arthritis (RA). A Phase IIa trial in patients with moderate to severe psoriasis has produced encouraging results [3].
Mechanism Of Action and Pharmacodynamic Effects
The Janus kinase (JAK) enzymes play a key role in cytokine signalling, which is involved in the pathological symptoms of immune-mediated disorders such as rheumatoid arthritis (RA). Peficitinib has been reported to inhinit all four JAKs at low nanomolar concentrations, although this data is not yet published in a peer reviewed article (see ASP015K: A Novel JAK Inhibitor Demonstrated Potent Efficacy in Adjuvant-Induced Arthritis Model in Rats, an abstract from the proceedings of the American College of Rheumatology/Association of Rheumatology Health Professionals, Annual Scientific Meeting, Washington DC, November 9-14, 2012).