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Updated: Jun 16, 2025

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
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Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

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Obicetrapib-the Rebirth of CETP Inhibitors?

Bliss Chang1, Luke J Laffin2,3, Ashish Sarraju2,3

  • 1Department of Cardiovascular Medicine, Cleveland Clinic Foundation, Cleveland, OH, USA.

Current Atherosclerosis Reports
|August 16, 2024
PubMed
Abstract

Insights

Obicetrapib, a cholesterylester transfer protein (CETP) inhibitor, shows promise in lowering LDL-C and other lipids. Ongoing trials will determine its role in treating dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).

Area of Science:

  • Cardiology
  • Pharmacology
  • Lipidology

Background:

  • Dyslipidemia and atherosclerotic cardiovascular disease (ASCVD) remain significant health concerns.
  • Cholesterylester transfer protein (CETP) inhibitors represent a therapeutic target for lipid modification.
  • Obicetrapib is a third-generation CETP inhibitor under investigation.

Purpose of the Study:

  • To review the development status of obicetrapib.
  • To discuss the potential role of obicetrapib in managing dyslipidemia and ASCVD.
  • To provide perspective on emerging clinical trial data.

Main Methods:

  • Review of Phase II clinical trial data (ROSE and ROSE2 trials).
  • Analysis of obicetrapib's effects on lipid biomarkers.
  • Overview of ongoing Phase III clinical trials, including a cardiovascular outcomes trial.

Main Results:

  • Obicetrapib significantly reduced low-density lipoprotein cholesterol (LDL-C), Apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C).
  • Obicetrapib demonstrated an increase in high-density lipoprotein cholesterol (HDL-C).
  • Preliminary safety data from early studies showed no significant safety concerns.

Conclusions:

  • Obicetrapib exhibits favorable effects on key dyslipidemia biomarkers.
  • The drug has the potential to reduce ASCVD events.
  • Further evaluation in Phase III trials is warranted to confirm efficacy and safety.
Keywords:
CETPCholesterylester transfer protein inhibitorLipid loweringLow-density lipoproteinObicetrapib

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