Bile acid sequestrants (colesevelam): how it works, status and trials
Approved (generic)PillLowering LDL cholesterol
Bile acid sequestrants bind bile acids in the gut and stop them from returning to the liver. The liver then uses more cholesterol to make new bile acids and adds LDL receptors. They can raise triglycerides.
In technical terms: Bind bile acids and stop their return to the liver; the liver converts more cholesterol to bile acids and up-regulates LDL receptors. Can raise TG.
The highlighted badge marks where Bile acid sequestrants (colesevelam) acts. Open the full map or compare every therapy.
At a glance
- Acts on
- Bile acids · gut lumen
- How it is given
- Oral resin · daily
- What the main trial found
- LDL-C ≈ −15% to −20% (colesevelam −16.7 pp vs placebo)
- Status (curated October 25, 2026)
- Approved (generic)
Where it fits in the body
Cholesterol synthesis and absorption
When the liver has less cholesterol, whether because synthesis is blocked (statins, bempedoic acid) or less arrives from the gut (ezetimibe, bile acid sequestrants), SREBP-2 switches on the LDL-receptor gene and the liver pulls more LDL out of the blood. SREBP-2 also raises PCSK9, which is one reason PCSK9 inhibitors add well to statins.
Evidence
- Colesevelam RCT (PubMed 18458145)
Common questions
How does Bile acid sequestrants (colesevelam) work?
Bile acid sequestrants bind bile acids in the gut and stop them from returning to the liver. The liver then uses more cholesterol to make new bile acids and adds LDL receptors. They can raise triglycerides. In technical terms: Bind bile acids and stop their return to the liver; the liver converts more cholesterol to bile acids and up-regulates LDL receptors. Can raise TG. It acts on Bile acids · gut lumen.
How much does Bile acid sequestrants (colesevelam) lower cholesterol or other lipids?
LDL-C ≈ −15% to −20% (colesevelam −16.7 pp vs placebo). Individual results differ, and a clinician can say what to expect for one person.
Is Bile acid sequestrants (colesevelam) approved, and what is the status?
Approved (generic) (curated October 25, 2026).
How is Bile acid sequestrants (colesevelam) taken?
Oral resin · daily.
Related therapies
- Statins: Approved (generic)
- Bempedoic acid (Nexletol, Nexlizet): Approved 2020
- Ezetimibe (Zetia): Approved (generic)
- Evolocumab (Repatha) and alirocumab (Praluent): Approved 2015
Educational, not medical advice. Mechanism and status text curated October 25, 2026; registry data refreshed October 27, 2026. Registries can lag company announcements. Effects are placebo-adjusted results from the main published trial, not head-to-head comparisons. Investigational agents are available only in clinical trials. Preval Health does not practice medicine; licensed clinicians in a partner network provide care. If you have chest pain or signs of a stroke, call 911.