BMS-753426

BMS-753426 is a potent and orally bioavailable small molecule antagonist of the CC chemokine receptor 2 (CCR2), developed to improve upon the metabolic stability and pharmacokinetic properties of earlier CCR2 antagonists. It demonstrates significant improvements in oral bioavailability and lower clearance compared to previous candidates, with additional affinity for CCR5. In preclinical models, BMS-753426 showed efficacy in inhibiting monocyte migration and demonstrated activity in multiple sclerosis models using hCCR2 knock-in mice. The compound was discovered through structure–activity relationship studies within a trisubstituted cyclohexylamine series by Bristol Myers Squibb[2][5][6].