{"id":"doi:10.1007/s11883-023-01184-1","kind":"review","title":"Obicetrapib: Reversing the Tide of CETP Inhibitor Disappointments","authors":["Kastelein JJP","Hsieh A","Dicklin MR","Ditmarsch M","Davidson MH"],"author_count":5,"year":2024,"published":"2023-12-22","venue":"Current atherosclerosis reports","cited_by":54,"doi":"10.1007/s11883-023-01184-1","arxiv_id":null,"nct_id":null,"source_url":"https://doi.org/10.1007/s11883-023-01184-1","archive_url":"https://space-kitty.com/papers/doi:10.1007/s11883-023-01184-1","updated":null,"pmid":"38133847","pmcid":"PMC10838241","openalex_id":null,"pdf_url":"https://europepmc.org/articles/PMC10838241/pdf","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_license":"CC-BY (article license as recorded by Europe PMC; abstract reproduced unmodified apart from markup removal)","license":"CC-BY","is_open_access":true,"retracted":false,"peer_reviewed":null,"categories":[],"details":null,"provenance":"europepmc","attribution":"Abstract of \"Obicetrapib: Reversing the Tide of CETP Inhibitor Disappointments\" by Kastelein JJP, Hsieh A, Dicklin MR et al., https://doi.org/10.1007/s11883-023-01184-1, used under its Creative Commons Attribution license (CC-BY); markup removed, otherwise unmodified.","topics":[{"slug":"cardiovascular-innovation","name":"Cardiovascular Therapeutics","domain_slug":"medicine"}],"cited_in_dossiers":[]}