fbpx

molecules of the month

PF-06826647

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.


request a trial

Drug Hunter is commited to helping industry innovators make informed decisions. Premium members have access to our library of the latest stories in science, written by scientists.

Request a trial to access insights powering the pros in our industry.


already a member? log in: