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Related Concept Videos

FDA Approved Drugs: Changes to Approved Drugs01:26

FDA Approved Drugs: Changes to Approved Drugs

Post-approval, manufacturers may modify an approved new or generic drug product. Such modifications can encompass alterations in the Active Pharmaceutical Ingredient (API), manufacturing process, formulation, batch size, manufacturing site, and container closure system (FDA Guidance for Industry, April 2004). Often, a drug product may undergo multiple changes.These modifications require careful evaluation to determine their potential impact on the drug product's identity, strength, quality,...
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...
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...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
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...

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Related Experiment Video

Updated: Jun 22, 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

Update on patented cholesterol absorption inhibitors.

M T Chhabria1, B M Mahajan

  • 1L. M. College of Pharmacy, Department of Pharmaceutical Chemistry, Navrangpura, Ahmedabad - 380 009, Gujarat, India. mahesh.chhabria@rediffmail.com

Expert Opinion on Therapeutic Patents
|June 26, 2009
PubMed
Summary

Ezetimibe, a cholesterol absorption inhibitor, combined with statins offers an effective approach for managing hypercholesterolemia. Newer analogues are also showing promise in clinical trials for cholesterol management.

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Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
09:15

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles

Published on: November 10, 2017

Related Experiment Videos

Last Updated: Jun 22, 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

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
09:15

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles

Published on: November 10, 2017

Area of Science:

  • Pharmacology
  • Cardiovascular Medicine

Background:

  • Atherosclerosis, a life-threatening disease, is linked to high cholesterol levels.
  • Cholesterol balance is maintained through synthesis and absorption; interventions targeting both are key.
  • Statins inhibit cholesterol biosynthesis, while ezetimibe blocks intestinal cholesterol absorption.

Purpose of the Study:

  • To review advancements in ezetimibe and novel cholesterol absorption inhibitors.
  • To critically analyze various targets involved in lipid absorption, including cholesterol esterase and bile acid transport.

Main Methods:

  • Literature review of ezetimibe and related cholesterol absorption inhibitors.
  • Analysis of patented compounds and their mechanisms of action.
  • Examination of therapeutic targets in lipid absorption.

Main Results:

  • Ezetimibe represents a new class of drugs for hypercholesterolemia management.
  • Combination therapy with statins provides an effective strategy for cholesterol control.
  • Several novel cholesterol absorption inhibitors are in clinical development.

Conclusions:

  • Ezetimibe in combination with statins offers a significant advancement in hypercholesterolemia treatment.
  • Emerging analogues like darapladib, FM-VP4, and A-002 show potential.
  • Targeting cholesterol absorption provides a valuable therapeutic avenue.