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Welchol (COLESEVELAM)
Welchol works by binding to bile acids in the gut, reducing their reabsorption and increasing their excretion, which in turn lowers cholesterol levels and improves blood sugar control.
Welchol (Colesevelam) is a bile acid sequestrant, a small molecule drug class, originally developed by Daiichi Sankyo and currently owned by Cosette. It is used to treat hypercholesterolemia and as an adjunct to control blood sugar levels in type 2 diabetes mellitus. Welchol is off-patent, with 15 generic manufacturers available. It is a commercial option for patients with these conditions. Key safety considerations include gastrointestinal side effects and potential interactions with other medications.
At a glance
| Generic name | COLESEVELAM |
|---|---|
| Sponsor | Cosette |
| Drug class | Bile Acid Sequestrant |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 2000 |
Mechanism of action
Primary Hyperlipidemia: Colesevelam hydrochloride, the active pharmaceutical ingredient, is non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7--hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, HMG-CoA reductase, and increasing the number of hepatic LDL receptors. These compensatory effects result in increased clearance of LDL-C from the blood, resulting in decreased serum LDL-C levels. Serum TG levels may increase or remain unchanged.. Type Diabetes Mellitus: The mechanism by which colesevelam hydrochloride improves glycemic control is unknown.
Approved indications
- Hypercholesterolemia
- Type 2 Diabetes Mellitus Treatment Adjunct
Common side effects
- Constipation
- Dyspepsia
- Nausea
- Accidental injury
- Asthenia
- Pharyngitis
- Flu syndrome
- Rhinitis
- Myalgia
- Nasopharyngitis
- Headache
- Fatigue
Key clinical trials
- Examining a Novel Gastrointestinal Intervention to Negate Environmental Toxicants (ENGINE) (PHASE1,PHASE2)
- A Study of Colesevelam for Lenalidomide-Associated Diarrhea (PHASE2)
- Prospective German Very High Cardiovascular Risk Patients Dyslipidemia Treatment Indication Registry
- Metabolic Effects of Endogenous Bile Acids After Gastric Bypass Surgery (EARLY_PHASE1)
- Three Antidiarrheal Strategies in HER2+/HR+ Early Breast Cancer Patients Treated With Extended Adjuvant Neratinib (PHASE2)
- Impact of Therapy Using Colesevelam Treatment Reducing Bile Acids in Patients With Fontan Circulation. (PHASE1,PHASE2)
- A Study of Colesevelam in Fecal Incontinence (PHASE3)
- Effect of the Sequestrant Colesevelam in Bile Acid Diarrhoea (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Welchol CI brief — competitive landscape report
- Welchol updates RSS · CI watch RSS
- Cosette portfolio CI