CE-224535

CE-224535 is a small molecule drug developed as a selective and potent antagonist of the human P2X7 receptor. It was investigated primarily as a disease-modifying antirheumatic drug (DMARD) for conditions such as rheumatoid arthritis and osteoarthritis. By antagonizing the P2X7 receptor—a ligand-gated ion channel involved in inflammation—CE-224535 reduces leukocyte secretion of pro-inflammatory cytokines IL-1 and IL-18. This mechanism offers a novel approach to modulating inflammatory responses in autoimmune diseases. The compound is orally bioavailable but has limited central nervous system penetration. Clinical trials showed that while it was safe and well tolerated at tested doses (up to 1600 mg single dose or up to 600 mg every 12 hours for two weeks), it failed to demonstrate efficacy in studies for knee pain due to osteoarthritis or rheumatoid arthritis[1][2][4][5][7].

Other names

724424-43-5UNII-T8B02RAU3CUNII-T-8B02RAU3CUNII-T 8B02RAU3CT8B02RAU3CT-8B02RAU3CT 8B02RAU3Ccompound 3 [PMID: 21782426]CP-23575CP23575CP 23575