Delgocitinib: A Topical Janus Kinase Family Inhibitor
JTE-052 (delgocitinib)
topical Janus kinase (JAK) family inhibitor approved for atopic dermatitis in JP from scaffold hop from known JAK inhibitor J. Med. Chem., Jun. 8, 2020 Japan Tobacco, Osaka, JP
Other molecules you may be interested in
BMS-986251
BMS-986251 is an inverse agonist of RORgt, a hot target in inflammation for a significant period. Unfortunately it looks like development hit a wall in this space, and several publications of various company’s RORgt modulators have appeared in the last several months. Chemically, 251 is interesting with 5 stereocenters, none of which look [...]
AZD0284
The AstraZeneca oral RORgt inverse agonist, AZD0284 , is an inverse agonist of the nuclear receptor RORC2 (RORγt). Reviewer Chris Gampe says, “targeting the activation and function of Th17 cells has been successful for the treatment of autoimmune disease (cf. IL-17, IL-17R, IL-23 Abs). RORC2 is the transcription factor that controls Th17 [...]
BioCryst Kallikrein Inhibitor
The Biocryst oral plasma kallikrein inhibitor, berotralstat (BCX7353) , was recently approved as the first non-steroidal treatment for prevention of hereditary angioedema attacks. The molecule is given orally (150 mg QD) despite having two basic amines. Interestingly for a chronically administered drug, the molecule is noted to have QT [...]
remibrutinib
Remibrutinib (Novartis oral BTK-selective covalent kinase inhibitor clinical candidate)
BAY 1003803
BAY 1003803 is a potent topical agonist of the glucocorticoid receptor (GR) transrepression pathway, with less activity on the GR transactivation pathway mediated by GR dimers, which may lead to undesirable side effects. The fluoroaminoquinoline was the only heterocycle among analogs tested that was Ames-negative. The compound appears to have [...]