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"cholestagel®" (Colesevelam)

University Hospital, Gentofte, Copenhagen · FDA-approved active Small molecule

Colesevelam is a bile acid sequestrant that binds bile acids in the intestine, preventing their reabsorption and increasing their fecal excretion.

Colesevelam is a bile acid sequestrant that binds bile acids in the intestine, preventing their reabsorption and increasing their fecal excretion. Used for Hypercholesterolemia (elevated LDL cholesterol), Type 2 diabetes mellitus (as adjunctive therapy).

At a glance

Generic name"cholestagel®" (Colesevelam)
SponsorUniversity Hospital, Gentofte, Copenhagen
Drug classBile acid sequestrant
TargetBile acids
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved

Mechanism of action

By binding bile acids in the gastrointestinal tract, colesevelam reduces the enterohepatic circulation of bile acids. This triggers increased hepatic conversion of cholesterol to bile acids to replenish the bile acid pool, thereby lowering serum LDL cholesterol levels. The drug may also improve glycemic control through mechanisms involving altered bile acid signaling and gut microbiota changes.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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