Identification
- Summary
Colesevelam is a bile acid sequestrant used to lower LDL-C in adults with hyperlipidemia and pediatric patients with heterozygous familial hypercholesterolemia, and to improve glycemic control in type 2 diabetes.
- Brand Names
- Cholestagel, Lodalis, Welchol
- Generic Name
- Colesevelam
- DrugBank Accession Number
- DB00930
- Background
Colesevelam is a bile acid sequestrant. Colesevelam is used with exercise and diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in the blood. It works by binding bile acids in the intestine. Bile acids are made when cholesterol is broken down in the body. Removing these bile acids helps to lower blood cholesterol.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Colesevelam
Pharmacology
- Indication
For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa).
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in management of Heterozygous familial hypercholesterolemia (hefh) •••••••••••• ••••••••••• ••••••••• Used in combination to treat Hyperlipidemia •••••••••••• Adjunct therapy in management of Type 2 diabetes mellitus •••••••••••• ••••• Adjunct therapy in management of Primary hyperlipidemia •••••••••••• ••••• - Contraindications & Blackbox Warnings
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Colesevelam is a high capacity bile-acid binding molecule. Colesevelam binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associated with LDL-C) are associated with an increased risk of atherosclerosis in humans. Similarly, decreased levels of high-density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the levels of total-C and LDL-C, and inversely with the level of HDL-C. The combination of colesevelam and an HMG-CoA reductase inhibitor is effective in further lowering serum total-C and LDL-C levels beyond that achieved by either agent alone.
- Mechanism of action
Colesevelam binds bile acids in the intestine and prevents their reabsorption. Colesevelam is not absorbed itself. The depletion of bile acid causes the upregulation of cholesterol 7-alpha-hydroxylase and conversion of cholesterol to bile acid. this increases the production and activity of hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase in the liver as well as an increase in the number of low density lipoprotein (LDL) receptors. This process clears LDL cholesterol from the blood.
Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol.
Target Actions Organism ABile acids binderHumans - Absorption
Not hydrolyzed by digestive enzymes and is not absorbed.
- Volume of distribution
Not Available
- Protein binding
Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
- Metabolism
Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
- Route of elimination
Excretion: In 16 healthy volunteers, an average of 0.05% of administered radioactivity from a single 14C-labeled colesevelam hydrochloride dose was excreted in the urine.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colesevelam is not absorbed, the risk of systemic toxicity is low. Doses in excess of 4.5 g per day have not been tested.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAceclofenac Colesevelam can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy. Acemetacin Colesevelam can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy. Acenocoumarol Colesevelam can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetazolamide Colesevelam can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetyl sulfisoxazole Colesevelam can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy. - Food Interactions
- Drink plenty of fluids.
- Take with food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Colesevelam hydrochloride P4SG24WI5Q 182815-44-7 VTAKZNRDSPNOAU-UHFFFAOYSA-M - Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cholestagel Tablet, film coated 625 mg Oral Cheplapharm Arzneimittel Gmb H 2016-09-08 Not applicable EU 
Cholestagel Tablet, film coated 625 mg Oral Cheplapharm Arzneimittel Gmb H 2016-09-08 Not applicable EU Cholestagel Tablet, film coated 625 mg Oral Cheplapharm Arzneimittel Gmb H 2016-09-08 Not applicable EU Cholestagel Tablet, film coated 625 mg Oral Cheplapharm Arzneimittel Gmb H 2016-09-08 Not applicable EU Colesevelam Hydrochloride Tablet, film coated 625 mg/1 Oral Cosette Pharmaceuticals, Inc. 2022-08-01 Not applicable US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-colesevelam Tablet 625 mg Oral Apotex Corporation 2020-07-23 Not applicable Canada 
Colesevelam Tablet, film coated 625 mg/1 Oral Zydus Pharmaceuticals USA Inc. 2019-10-11 Not applicable US Colesevelam Tablet 625 mg/1 Oral Zydus Lifesciences Limited 2019-10-11 Not applicable US Colesevelam HCL Tablet, film coated 625 mg/1 Oral A-S Medication Solutions 2018-10-06 Not applicable US Colesevelam HCL Tablet, film coated 625 mg/1 Oral Ascend Laboratories, LLC 2018-10-06 Not applicable US
Categories
- ATC Codes
- C10AC04 — Colesevelam
- Drug Categories
- Alkenes
- Allyl Compounds
- Allylamine
- Amines
- Anticholesteremic Agents
- Bile Acid Sequestrants
- Bile-acid Binding Activity
- Hydrocarbons, Acyclic
- Hypolipidemic Agents
- Hypolipidemic Agents Indicated for Hyperlipidemia
- Lipid Modifying Agents
- Lipid Modifying Agents, Plain
- Lipid Regulating Agents
- Non-statin Hypolipidemic Agents Indicated for Hyperlipidemia
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1XU104G55N
- CAS number
- 182815-43-6
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Not Available
- External Links
- PubChem Substance
- 46505437
- 141626
- PharmGKB
- PA449095
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Colesevelam
- FDA label
- Download (130 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Basic Science Bileacid Malabsorption 2 4 Completed Basic Science Type 2 Diabetes Mellitus 2 4 Completed Other Atherosclerosis / Carotid Artery Diseases / Coronary Artery Disease (CAD) 1 4 Completed Prevention Dyslipidemia / Hyperglycemia / Hyperlipidemias 1 4 Completed Treatment Bileacid Malabsorption / Chronic Diarrhea 1
Pharmacoeconomics
- Manufacturers
- Daiichi sankyo inc
- Packagers
- Daiichi Sankyo
- Patheon Inc.
- Physicians Total Care Inc.
- Quality Care
- Resource Optimization and Innovation LLC
- Southwood Pharmaceuticals
- Dosage Forms
Form Route Strength Powder, for suspension Oral 1.875 g/1 Powder, for suspension Oral 3.75 g/1 Tablet Oral 625 mg/1 Tablet, coated Oral 625 mg/1 Powder Oral Tablet, film coated Oral Powder, for suspension Oral 3.75 g / sachet Tablet Oral 625 mg Bar, chewable Oral 3.75 g/1 For suspension Oral 1.875 g/1 For suspension Oral 3.75 g/1 Tablet, film coated Oral 625 mg/1 Tablet, film coated Oral 625 mg - Prices
Unit description Cost Unit Welchol 625 mg tablet 1.96USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5679717 No 1997-10-21 2014-04-29 US US7229613 Yes 2007-06-12 2022-10-17 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Insoluble Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
References
- Levy P, Jellinger PS: The potential role of colesevelam in the management of prediabetes and type 2 diabetes mellitus. Postgrad Med. 2010 May;122(3Suppl):1-8. doi: 10.3810/pgm.2010.05.2168. [Article]
- Staels B: A review of bile acid sequestrants: potential mechanism(s) for glucose-lowering effects in type 2 diabetes mellitus. Postgrad Med. 2009 May;121(3 Suppl 1):25-30. doi: 10.3810/pgm.2009.05.suppl53.290. [Article]
- Corsini A, Windler E, Farnier M: Colesevelam hydrochloride: usefulness of a specifically engineered bile acid sequestrant for lowering LDL-cholesterol. Eur J Cardiovasc Prev Rehabil. 2009 Feb;16(1):1-9. doi: 10.1097/HJR.0b013e32831215db. [Article]
- Steinmetz KL, Schonder KS: Colesevelam: potential uses for the newest bile resin. Cardiovasc Drug Rev. 2005 Spring;23(1):15-30. [Article]
- Melian EB, Plosker GL: Colesevelam. Am J Cardiovasc Drugs. 2001;1(2):141-6; discussion 147-8. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54