Obicetrapib is an investigational, oral, once-daily, small-molecule medication that acts as a potent and selective cholesteryl ester transfer protein (CETP) inhibitor.
It is being developed primarily to lower high levels of low-density lipoprotein cholesterol (LDL-C) and reduce cardiovascular risk.
In clinical trials, a 10 mg daily dose has shown a reduction in LDL-C levels by approximately 30% to 45% when added to existing statin therapy.
It also reduces other atherogenic biomarkers like Apolipoprotein B (ApoB), non-HDL-C, and Lipoprotein(a).
Unlike some earlier CETP inhibitors, it significantly increases high-density lipoprotein cholesterol (HDL-C) levels, with some studies reporting increases of over 150%.
It is also being studied in combination with ezetimibe to achieve even greater LDL-C lowering.
Trials demonstrated efficacy and safety in patients with atherosclerotic cardiovascular disease (ASCVD) and heterozygous familial hypercholesterolemia (HeFH).