molecules of the month

The Celgene/BMS PKCθ kinase inhibitor, CC-90005, highlighted by Julien Lefranc, is a clinical candidate in Ph. I for psoriasis, with some dosing being conducted in healthy volunteers. The safety profile is impressive given how fraught with selectivity issues previous PKC inhibitors have been. The molecule is >550-fold selective for PKCθ over PKCδ, and has relatively high sp3 character for a kinase inhibitor. The advancement of a PKC kinase inhibitor into healthy volunteers and with an intended chronic inflammation indication is testament to how far kinase inhibition has come in 20 years with respect to achievable selectivity and safety.