Obicetrapib: Reversing the Tide of CETP Inhibitor Disappointments

John J. P. Kastelein, Andrew Hsieh, Mary R. Dicklin, Marc Ditmarsch, Michael H. Davidson

Research output: Contribution to journalReview articleAcademicpeer-review

5 Citations (Scopus)


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. Summary: 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.
Original languageEnglish
JournalCurrent Atherosclerosis Reports
Early online date2023
Publication statusE-pub ahead of print - 2023


  • Atherosclerotic cardiovascular disease (ASCVD)
  • Cardiovascular outcomes trial
  • Cholesteryl ester transfer protein (CETP) inhibitor
  • High-density lipoprotein cholesterol (HDL-C)
  • Low-density lipoprotein cholesterol (LDL-C)
  • Obicetrapib

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