# Obicetrapib: Reversing the Tide of CETP Inhibitor Disappointments

Review · Kastelein JJP, Hsieh A, Dicklin MR, Ditmarsch M, Davidson MH

- Archive id: doi:10.1007/s11883-023-01184-1
- Published: 2023-12-22
- Venue: Current atherosclerosis reports
- DOI: https://doi.org/10.1007/s11883-023-01184-1
- PMID: 38133847
- PMCID: PMC10838241
- Citations: 54
- Source URL: https://doi.org/10.1007/s11883-023-01184-1
- PDF: https://europepmc.org/articles/PMC10838241/pdf
- Provenance: europepmc

## 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.

_Abstract reproduced under CC-BY (article license as recorded by Europe PMC; abstract reproduced unmodified apart from markup removal)._

Topics: [Cardiovascular Therapeutics](https://space-kitty.com/topics/cardiovascular-innovation)

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