GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1]. PI3Kδ|1 nM (IC50)
GS-9901 (0.3/1/3 mg/kg, orally, twice daily for 7 days) demonstrates efficacy in a rat model of arthritis and is predicted to be suitable for q.d. dosing in humans[1]. Animal Model: Female Lewis rats with established collagen-induced arthritis (CIA)[1].
[1]. Patel L, et al. Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability. J Med Chem. 2016 Oct 13;59(19):9228-9242.