molecules of the month


TYK2-selective kinase inhibitor (JH1 domain)

in Ph. II for inflamm. conditions (oral, QD)

from structure-based design

J. Med. Chem., Aug. 5, 2020

Pfizer, Cambridge, MA / Groton, CT

Structure of Ropsacitinib (PF-06826647)
1 min read

PF-06826647 is a TYK2-selective kinase inhibitor which binds to the catalytically active JH1 kinase domain, in contrast to BMS-986165, a TYK2 inhibitor in Ph. III for psoriasis that binds to the JH2 pseudokinase domain. TYK2-selective inhibitors are expected to have anti-inflammatory activity with reduced side effects such as anemia due to inhibition of other JAK-family members. Interestingly, PF-07826647 interacts with the hinge region of TYK2’s JH1 domain through a polarized aryl C-H—O hydrogen bond. PF-06826647 is currently in clinical development as a once-daily oral treatment for a number of inflammatory conditions including psoriasis and ulcerative colitis.

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