Colestipol is a bile acid sequestrant used as an adjunct to diet and exercise to reduce LDL-C cholesterol levels in patients with primary hypercholesterolemia. Bile acid sequestrants like colestipol have been in use since the 1970s.
- Mechanism
- Curator reviewed
Colestipol is a lipid-lowering polymer that binds with bile acids in the intestine forming a complex that is excreted in the feces. This non-systemic action results in a continuous, partial removal of bile acids from the enterohepatic circulation preventing their reabsorption. This increased fecal loss of bile acids due to colestipol hydrochloride administration leads to increased oxidation of cholesterol to bile acids. This results in an increase in the number of hepatic low-density lipoprotein (LDL) receptors, and consequently an increased uptake of LDL and a decrease in serum/plasma beta lipoprotein or total and LDL cholesterol levels. Although hydrochloride produces an increase in the hepatic synthesis of cholesterol in man, serum cholesterol levels fall.
- Primary indication
- Colestipol is indicated as adjunctive therapy to diet for the reduction of elevated serum total and low-density lipoprotein cholesterol (LDL-C) in patients with primary hypercholesterolemia (a condition that features elevated LDL-C) who do not respond...Curator reviewed · 1 structured indication
- First approval
- Canada, 2003 · United States, 1977
- Also known as
- Epichlorohydrin-tetraethylenepentamine polymer
- Code names
- U 26597 A
- Brand names
Resolves to
What you can answer from here — as of July 17, 2026
Which other approved drugs treat the same conditions as Colestipol, and which companies have late-stage candidates in those indications?
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