RAP-0001

RAP-0001 is a first-in-class, highly potent and selective inhibitor of Equilibrative Nucleoside Transporter 1 (ENT1), developed by Rapafusyn Pharmaceuticals. It acts as a non-degrading molecular glue that uniquely binds to both the intracellular chaperone protein FKBP12 and ENT1, forming a ternary complex. This mechanism blocks cellular uptake of adenosine via ENT1, thereby preserving elevated extracellular adenosine levels during ischemic stress. The increased availability of adenosine allows activation of its protective receptors, reducing metabolic stress and mitigating ischemia/reperfusion injury—a major driver of acute kidney injury (AKI) in patients undergoing cardiac surgery. RAP-0001 has demonstrated preclinical efficacy in preventing renal damage associated with ischemia/reperfusion injury and is being advanced for the prevention of AKI in high-risk clinical settings[1][3][5].

Brand names

RAP-0001RAP0001RAP 0001

Other names

ENT1 inhibitorENT-1 inhibitorENT 1 inhibitorSLC29A1 inhibitorSLC-29A1 inhibitorSLC 29A1 inhibitor