Related Experiment Video

Updated: May 27, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
07:13

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader

Published on: May 24, 2024

Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction

D E Gutstein1, R Krishna, D Johns

  • 1Merck Sharp & Dohme Corp., Rahway, New Jersey, USA. david_gutstein@merck.com

Clinical Pharmacology and Therapeutics
|December 2, 2011
PubMed

Insights

Cholesteryl ester transfer protein (CETP) inhibition, using drugs like anacetrapib, shows promise for increasing HDL-C and lowering cardiovascular risk. This review details anacetrapib

Area of Science:

  • Cardiovascular Medicine
  • Pharmacology
  • Lipid Metabolism

Background:

  • Cholesteryl ester transfer protein (CETP) plays a key role in lipoprotein metabolism.
  • Elevated high-density lipoprotein cholesterol (HDL-C) is associated with reduced cardiovascular risk.
  • Targeting CETP is an experimental strategy to modulate HDL-C levels.

Purpose of the Study:

  • To review the preclinical and clinical data for the CETP inhibitor anacetrapib.
  • To discuss the mechanisms of CETP inhibition and its impact on lipid biology.
  • To provide an overview of other CETP inhibitors in development.

Main Methods:

  • Literature review of preclinical studies.
  • Analysis of clinical trial data for anacetrapib.
  • Discussion of lipid metabolism and CETP function.

Main Results:

  • Anacetrapib is a highly selective and potent CETP inhibitor.
  • CETP inhibition effectively raises HDL-C levels.
  • Anacetrapib has demonstrated a favorable safety and efficacy profile in studies.

Conclusions:

  • Anacetrapib represents a promising therapeutic approach for cardiovascular risk reduction.
  • Further research into CETP inhibition strategies is warranted.
  • Anacetrapib and other CETP inhibitors offer potential new avenues for managing dyslipidemia.

Related Concept Videos

Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Lipid-Lowering Drugs: Statins and Miscellaneous Agents01:20

Lipid-Lowering Drugs: Statins and Miscellaneous Agents

Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
Atherosclerosis III: Management01:26

Atherosclerosis III: Management

Management of atherosclerosis involves an integrated strategy encompassing pharmacological treatment, surgical interventions, lifestyle changes, and nutrition therapy to address the multifactorial nature of the disease.Pharmacological TherapyA cornerstone of atherosclerosis management is the use of pharmacological agents. Statins, such as atorvastatin, are pivotal in inhibiting HMG-CoA reductase, an enzyme that catalyzes an initial step in cholesterol synthesis in the liver. This reduction in...
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Lipid Absorption01:24

Lipid Absorption

Dietary triglycerides from chyme in the duodenum are mixed with bile salts produced by the liver to emulsify fats. As a result, large droplets are broken down into smaller ones, increasing the surface area for enzymatic action. Once emulsified, pancreatic lipases hydrolyze the triglycerides into free fatty acids and monoglycerides.
These breakdown products bind with bile salts and lecithin to form micelles, which quickly pass between microvilli to come in close contact with the apical...