Investigational Drug Details
| Drug ID: | D074 |
| Drug Name: | Cholestyramine |
| Synonyms: | Cholestyramine resin; Colestyramine |
| Type: | Chemical drug |
| DrugBank ID: | DB01432 |
| DrugBank Description: | Cholestyramine or colestyramine is a bile acid sequestrant. Bile acid sequestrants are polymeric compounds which serve as ion exchange resins. Cholestyramine resin is quite hydrophilic, but insoluble in water. |
| PubChem ID: | 70695641 |
| CasNo: | 11041-12-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | [N+](c1ccc(CCC(c2ccc(cc2)CC)C)cc1)(C)(C)C |
| Structure: |
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| InChiKey: | HGMSJMJPXGGEBP-UHFFFAOYSA-N |
| Molecular Weight: | 296.478 |
| DrugBank Targets: | Bile acids binder |
| DrugBank MoA: | Cholestyramine forms a resin that acts as a bile acid sequestrant to limit the reabsorption of bile acids in the gastrointestinal tract. Cholestyramine resin is a strong anion exchange resin, allowing it to exchange its chloride anions with anionic bile acids present in the gastrointestinal tract and form a strong resin matrix. Cholestyramine consists of a functional group, which is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer, in the anion exchange resin. |
| DrugBank Pharmacology: | Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum. Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption. |
| DrugBank Indication: | Indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein cholesterol) who do not respond adequately to diet. Also for the relief of pruritus associated with partial biliary obstruction. |
| Targets: | -- |
| Therapeutic Category: | Hypolipidemic drug |
| Clinical Trial Progress: | Phase 2 completed (NCT04235205: Elobixibat resolved constipation in the short-term, and was well tolerated with both short-term and long-term treatment. The evidence supports the use of this novel approach to increase intracolonic concentrations of endogenous bile acid for the treatment of chronic constipation.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0034 | NCT04235205 | Phase 2 | Completed | No Results Available | January 29, 2020 | November 16, 2021 | Details |
| L0440 | JPRN-JapicCTI-205120 | Phase 2 | Not Recruiting | No Results Available | 21/01/2020 | 27 December 2021 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A06377 | 32907904 | BMJ Open | Rationale and design of a randomised, double-blind, placebo-controlled, parallel-group, investigator-initiated phase 2a study to investigate the efficacy and safety of elobixibat in combination with cholestyramine for non-alcoholic fatty liver disease. | Details |
| A08697 | 32019572 | J Med Case Rep | Thrombotic microangiopathy and liver toxicity due to a combination therapy of leflunomide and methotrexate: a case report. | Details |
| A16342 | 28446519 | Diabetes | Cationic Polystyrene Resolves Nonalcoholic Steatohepatitis, Obesity, and Metabolic Disorders by Promoting Eubiosis of Gut Microbiota and Decreasing Endotoxemia. | Details |
| A16516 | 28345673 | Sci Rep | Sex-dependent effects on gut microbiota regulate hepatic carcinogenic outcomes. | Details |
| A18226 | 27273788 | Int J Cancer | Dysregulated hepatic bile acids collaboratively promote liver carcinogenesis. | Details |
| A22658 | 24378273 | Ann Hepatol | Effects of bile acid sequestration on hepatic steatosis in obese mice. | Details |
| A27469 | 18330098 | Acta Gastroenterol Belg | Statins in hepatobiliary diseases: effects, indications and risks. | Details |
| A40857 | 6572892 | Postgrad Med | Gemfibrozil in combination with other drugs for severe hyperlipidemia. Preliminary study comprising four cases. | Details |
| A52347 | 28275691 | Cell Mol Gastroenterol Hepatol | Targeting the Enterohepatic Bile Acid Signaling Induces Hepatic Autophagy via a CYP7A1-AKT-mTOR Axis in Mice. | Details |
| A52878 | 20197195 | Metabolism | Impact of dietary fat type within the context of altered cholesterol homeostasis on cholesterol and lipoprotein metabolism in the F1B hamster. | Details |
| A53194 | 4892101 | Am J Dig Dis | Steatorrhea associated with disordered bile acid metabolism. Micellar phase defects. | Details |