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Related Concept Videos

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...
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...
Cholesterol: Significance and Regulation01:29

Cholesterol: Significance and Regulation

Although not a source of energy, cholesterol plays a significant role as a foundational structure for bile salts, steroid hormones, and vitamin D, as well as being a crucial component of plasma membranes. Approximately 15% of blood cholesterol is derived from our diet, with the remainder synthesized from acetyl CoA by the liver and intestines. Cholesterol is eliminated from the body through its conversion into bile salts, which are eventually discarded in the feces.
Considering cholesterol and...
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
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...
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...

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Related Experiment Video

Updated: May 21, 2026

LDL Cholesterol Uptake Assay Using Live Cell Imaging Analysis with Cell Health Monitoring
08:45

LDL Cholesterol Uptake Assay Using Live Cell Imaging Analysis with Cell Health Monitoring

Published on: November 17, 2018

Dalcetrapib , a cholesteryl ester transfer protein modulator.

Amanda J Hooper1, John R Burnett

  • 1Royal Perth Hospital, Department of Core Clinical Pathology & Biochemistry, PathWest Laboratory Medicine WA, Perth, Western Australia.

Expert Opinion on Investigational Drugs
|June 26, 2012
PubMed
Summary
This summary is machine-generated.

Dalcetrapib, a cholesteryl ester transfer protein (CETP) inhibitor, effectively raised HDL-cholesterol but failed to demonstrate significant clinical benefit in Phase III trials, halting further development.

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Cholesterol Efflux Assay
07:54

Cholesterol Efflux Assay

Published on: March 6, 2012

Related Experiment Videos

Last Updated: May 21, 2026

LDL Cholesterol Uptake Assay Using Live Cell Imaging Analysis with Cell Health Monitoring
08:45

LDL Cholesterol Uptake Assay Using Live Cell Imaging Analysis with Cell Health Monitoring

Published on: November 17, 2018

Cholesterol Efflux Assay
07:54

Cholesterol Efflux Assay

Published on: March 6, 2012

Area of Science:

  • Pharmacology
  • Cardiovascular Medicine
  • Lipid Metabolism

Background:

  • Cholesteryl ester transfer protein (CETP) facilitates cholesterol transfer, impacting HDL-cholesterol levels.
  • Inhibiting CETP is a strategy to increase HDL-cholesterol and potentially mitigate atherosclerosis.
  • Dalcetrapib is an oral CETP inhibitor investigated for hyperlipidaemia treatment.

Purpose of the Study:

  • To review the mode of action, preclinical, and clinical development of dalcetrapib.
  • To analyze the pharmacokinetic and pharmacodynamic properties of dalcetrapib.
  • To assess the clinical efficacy and safety of dalcetrapib in managing lipid disorders.

Main Methods:

  • Review of preclinical data and clinical trial outcomes for dalcetrapib.
  • Pharmacokinetic and pharmacodynamic assessments.
  • Analysis of efficacy and safety data from clinical studies, including effects on blood pressure and the renin-angiotensin-aldosterone system.

Main Results:

  • Dalcetrapib significantly increased HDL-cholesterol levels, alone or with statins.
  • No adverse effects on blood pressure or the renin-angiotensin-aldosterone system were observed.
  • Dalcetrapib did not impede the formation of pre-β HDL, potentially important for reverse cholesterol transport.

Conclusions:

  • Dalcetrapib is well-tolerated with a favorable safety profile.
  • Despite increasing HDL-cholesterol, interim Phase III results indicated a lack of clinically meaningful benefit.
  • Further investigation of dalcetrapib has been discontinued due to insufficient efficacy.