dalcetrapib

Dalcetrapib is an investigational small molecule drug that acts as a selective inhibitor and modulator of cholesteryl ester transfer protein (CETP). Its primary mechanism is to induce a conformational change in CETP, reducing its activity and thereby increasing high-density lipoprotein cholesterol (HDL-C) by approximately 25–30%, with little effect on low-density lipoprotein cholesterol (LDL-C)[2][5][6][8]. Unlike other CETP inhibitors, dalcetrapib does not fully block CETP function but modulates it, resulting in more modest HDL increases[5][8]. Dalcetrapib was originally developed by F. Hoffmann–La Roche and later licensed to DalCor Pharmaceuticals for further development as a precision medicine targeting patients with acute coronary syndrome (ACS) who have the AA genotype at variant rs1967309 in the ADCY9 gene[3]. Clinical trials have shown potential benefit in this genetically defined subgroup, although overall results for broader populations were less conclusive[2][3].

Other names

dalcetrapib