Drug intelligence / Profile preview

colesevelam + atorvastatin

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Colesevelam + atorvastatin is a combination therapy used primarily for the management of hypercholesterolemia (high cholesterol). Colesevelam is a bile acid sequestrant that works by binding bile acids in the intestine, preventing their reabsorption and promoting their excretion. This process depletes the bile acid pool, leading to increased conversion of cholesterol to bile acids in the liver and upregulation of LDL receptors, which enhances clearance of LDL cholesterol from the blood[1][6][8]. Atorvastatin is an HMG-CoA reductase inhibitor (statin) that reduces cholesterol synthesis in the liver and also increases hepatic uptake of LDL cholesterol. The combination has been shown to be more effective at lowering LDL-C than either agent alone[5]. Colesevelam may also improve glycemic control in type 2 diabetes mellitus. The primary indication for this combination is hypercholesterolemia, especially when monotherapy with statins or colesevelam alone does not achieve target lipid levels.

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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