Obicetrapib
Reversing the tide of CETP inhibitor disappointments: a review of obicetrapib and its ROSE2 data ahead of pivotal phase 3 outcomes trials (Curr Atheroscler Rep 2024)
Original title: Obicetrapib: Reversing the Tide of CETP Inhibitor Disappointments
A review by trial investigators tracing the history of CETP inhibitor cardiovascular outcomes trials and describing obicetrapib, a next-generation, oral, once-daily, low-dose CETP inhibitor then in late-stage development. In the ROSE2 phase 2 trial, obicetrapib 10 mg monotherapy and combined with ezetimibe 10 mg, both on top of high-intensity statins, significantly reduced LDL-C, non-HDL-C, apoB, total and small LDL particles, small dense LDL-C and Lp(a), while raising HDL-C. Phase 3 pivotal registration trials, including a cardiovascular outcomes trial, were underway at the time of writing. The authors describe an excellent safety and tolerability profile, framing obicetrapib as a promising ASCVD treatment ahead of confirmatory phase 3 data.
Original abstract
Purpose Of Review: To discuss the history of cardiovascular outcomes trials of cholesteryl ester transfer protein (CETP) inhibitors and to describe obicetrapib, a next-generation, oral, once-daily, low-dose CETP inhibitor in late-stage development for dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).
Recent Findings: Phase 1 and 2 trials have evaluated the safety and lipid/lipoprotein effects of obicetrapib as monotherapy, in conjunction with statins, on top of high-intensity statins (HIS), and with ezetimibe on top of HIS. In ROSE2, 10 mg obicetrapib monotherapy and combined with 10 mg ezetimibe, each on top of HIS, significantly reduced low-density lipoprotein cholesterol (LDL-C), non-high-density lipoprotein cholesterol (non-HDL-C), apolipoprotein B, total LDL particles, small LDL particles, small, dense LDL-C, and lipoprotein (a), and increased HDL-C. Phase 3 pivotal registration trials including a cardiovascular outcomes trial are underway. Obicetrapib has an excellent safety and tolerability profile and robustly lowers atherogenic lipoproteins and raises HDL-C. As such, obicetrapib may be a promising agent for the treatment of ASCVD.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.