Colesevelam

Identification

Name
Colesevelam
Accession Number
DB00930
Description

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).

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

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.

TargetActionsOrganism
ABile acids
binder
Humans
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
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

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.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AceclofenacColesevelam can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcemetacinColesevelam can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcenocoumarolColesevelam can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetazolamideColesevelam can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetyl sulfisoxazoleColesevelam can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetyldigitoxinColesevelam can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylsalicylic acidColesevelam can cause a decrease in the absorption of Acetylsalicylic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlclofenacColesevelam can cause a decrease in the absorption of Alclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlfacalcidolThe serum concentration of Alfacalcidol can be decreased when it is combined with Colesevelam.
AminophenazoneColesevelam can cause a decrease in the absorption of Aminophenazone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Additional Data Available
  • Extended Description
    Extended Description
    Available for Purchase

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity
    Available for Purchase

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level
    Available for Purchase

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action
    Available for Purchase

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
  • Drink plenty of fluids.
  • Take with food.

Products

Purchasing individual compounds or compound libraries for your research?
Learn More
Product Ingredients
IngredientUNIICASInChI Key
Colesevelam hydrochlorideP4SG24WI5Q182815-44-7VTAKZNRDSPNOAU-UHFFFAOYSA-M
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CholestagelTablet, film coated625 mgOralGenzyme Europe Bv2004-03-10Not applicableEU flag
CholestagelTablet, film coated625 mgOralGenzyme Europe Bv2004-03-10Not applicableEU flag
CholestagelTablet, film coated625 mgOralGenzyme Europe Bv2004-03-10Not applicableEU flag
CholestagelTablet, film coated625 mgOralGenzyme Europe Bv2004-03-10Not applicableEU flag
Colesevelam hydrochlorideTablet, film coated625 mg/1OralOhm Laboratories, Inc.2018-05-23Not applicableUS flag
Colesevelam hydrochloridePowder, for suspension3.75 g/1OralOhm Laboratories, Inc.2018-07-17Not applicableUS flag
LodalisPowder, for suspensionOralValeant Canada Lp Valeant Canada S.E.C.2015-04-02Not applicableCanada flag
LodalisTabletOralValeant Canada Lp Valeant Canada S.E.C.2012-02-06Not applicableCanada flag
WelcholTablet, film coated625 mg/1OralMed Pharma Co., Ltd.2011-07-152012-08-01US flag
WelcholFor suspension3.75 g/1OralRebel Distributors2010-01-01Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-colesevelamTabletOralApotex Corporation2020-07-23Not applicableCanada flag
ColesevelamTablet625 mg/1OralCadila Healthcare Limited2019-10-11Not applicableUS flag
ColesevelamTablet, film coated625 mg/1OralZydus Pharmaceuticals (USA) Inc.2019-10-11Not applicableUS flag
ColesevelamTablet180 1/1OralTris Pharma Inc2020-10-19Not applicableUS flag
Colesevelam HCLTablet, film coated625 mg/1OralA-S Medication Solutions2018-10-06Not applicableUS flag
Colesevelam HCLTablet, film coated625 mg/1OralAscend Laboratories, LLC2018-10-06Not applicableUS flag
Colesevelam HydrochlorideTablet, film coated625 mg/1OralBionpharma Inc.2019-12-02Not applicableUS flag
Colesevelam HydrochloridePowder, for suspension3.75 g/1OralGlenmark Pharmaceuticals Inc.,Usa2018-07-16Not applicableUS flag
Colesevelam HydrochlorideTablet, coated625 mg/1OralAvKARE, Inc.2018-06-18Not applicableUS flag
Colesevelam HydrochlorideTablet, film coated625 mg/1OralGlenmark Pharmaceuticals Inc., USA2018-05-18Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more

Categories

ATC Codes
C10AC04 — Colesevelam
Drug Categories
Classification
Not classified

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
PubChem Substance
46505437
RxNav
141626
PharmGKB
PA449095
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Colesevelam
AHFS Codes
  • 24:06.04 — Bile Acid Sequestrants
FDA label
Download (130 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingOtherAtherosclerosis / Carotid Artery Diseases / Coronary Artery Disease (CAD)1
4CompletedBasic ScienceBileacid Malabsorption1
4CompletedBasic ScienceType 2 Diabetes Mellitus2
4CompletedPreventionDyslipidemia / Hyperglycemia / Hyperlipidemias1
4CompletedTreatmentDiarrhoea Predominant Irritable Bowel Syndrome1
4CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa)1
4CompletedTreatmentDyslipidemia / Hyperlipidemias1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHigh Cholesterol5
4CompletedTreatmentHigh Cholesterol / Hyperlipidemia, Familial Combined1

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
FormRouteStrength
Tablet, film coatedOral625 mg
TabletOral180 1/1
Powder, for suspensionOral1.875 g/1
Powder, for suspensionOral3.75 g/1
TabletOral625 mg/1
Tablet, coatedOral625 mg/1
PowderOral1875 mg
PowderOral3750 mg
Tablet, coatedOral625 mg
Powder, for suspensionOral
TabletOral
Bar, chewableOral3.75 g/1
For suspensionOral1.875 g/1
For suspensionOral3.75 g/1
Tablet, film coatedOral625 mg/1
Prices
Unit descriptionCostUnit
Welchol 625 mg tablet1.96USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5679717No1997-10-212014-04-29US flag
US7229613Yes2007-06-122022-10-17US flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

1. Bile acids
Kind
Group
Organism
Humans
Pharmacological action
Yes
Actions
Binder
References
  1. 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. [PubMed:20581432]
  2. 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. [PubMed:19494475]
  3. 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. [PubMed:19237992]
  4. Steinmetz KL, Schonder KS: Colesevelam: potential uses for the newest bile resin. Cardiovasc Drug Rev. 2005 Spring;23(1):15-30. [PubMed:15867945]
  5. Melian EB, Plosker GL: Colesevelam. Am J Cardiovasc Drugs. 2001;1(2):141-6; discussion 147-8. [PubMed:14728043]

Drug created on June 13, 2005 07:24 / Updated on November 23, 2020 09:08

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates