cholestyramine
Trade name: questran
Approved
Aug 3, 1973
Colestyramine (INN) or cholestyramine (USAN) is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. It is a strong ion exchange resin, which means it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer. — Wikipedia
Clinical trial activity
29 trials · 48 clinical orgs · 19 marketing orgs
Earliest trial started Nov 1, 1971 (NCT00000594)
Timeline
1970s
- Jan 1, 1971
Earliest Phase 3 Sponsor(trial)
- Aug 3, 1973
Bristol-Myers — Earliest FDA Approval
- Aug 3, 1973
Bristol-Myers Squibb — NDA Secondary Org
- Aug 3, 1973
Bristol-Myers — NDA Organization
1980s
- Jan 1, 1986
Earliest Phase 2 Sponsor(trial)
1990s
- Feb 22, 1996
Upsher-Smith Laboratories — Marketing Organization
- Aug 15, 1996
Epic Pharma Llc — Marketing Organization
- Aug 15, 1996
Invatech — Marketing Organization
- Aug 15, 1996
Allied Pharmaceutical Services — Marketing Organization
- Aug 15, 1996
Sandoz — Marketing Organization
- Aug 15, 1996
Chartwell Pharmaceuticals — Marketing Organization
- Oct 2, 1996
Ani Pharmaceuticals — Marketing Organization
- Sep 30, 1998
Teva — Marketing Organization
2000s
- Aug 26, 2005
Endo Pharmaceuticals — Marketing Organization
- Aug 26, 2005
Par Pharmaceuticals — Marketing Organization
2010s
- Jan 1, 2010
Earliest Phase 1 Sponsor(trial)
- Apr 25, 2017
Zydus Discovery DMCC — Marketing Organization
2020s
- Apr 6, 2020
Ajanta Pharma Ltd — Marketing Organization
- Nov 12, 2020
Precision Dose — Marketing Organization
- Oct 19, 2021
Alkem Labs Ltd — Marketing Organization
- Oct 31, 2024
Macleods Pharmaceuticals, Ltd — Marketing Organization
Indications
Approved for
Studied for
- Alagille Syndrome · Phase 1
- Bile Acids and Salts · Phase 2
- Cardiovascular Diseases · Phase 3
- Cholestasis · Phase 1
- Coronary Disease · Phase 3
- Diabetes Mellitus · Phase 4
- Diabetic Neuropathies · Phase 4
- Diabetic Retinopathy · Phase 4
- Graft vs Host Disease · Phase 1
- Graves Disease · Phase 3
- Healthy Volunteers · Phase 4
- Heart Diseases · Phase 3
- Hemodialysis, Home · Phase 4
- Hypercholesterolemia · Phase 3
- Hyperlipoproteinemia Type II · Phase 3
- Hyperphosphatemia · Phase 4
- Hyperthyroidism · Phase 3
- Kidney Failure, Chronic · Phase 1
- Liver Cirrhosis, Biliary · Phase 1
- Liver Diseases · Phase 1
- Multiple Myeloma · Phase 2
- Multiple Sclerosis · Phase 3
- Myocardial Infarction · Phase 3
- Myocardial Ischemia · Phase 3
- Neoplasms · Phase 1
- Non-alcoholic Fatty Liver Disease · Phase 2
- Pancreatic Neoplasms · Phase 1
- Renal Insufficiency, Chronic · Phase 4
- Short Bowel Syndrome · Phase 2
Mechanism of action
- Bile acidsSEQUESTERING AGENT
Bile acids sequestering agent
Colestyramine is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. It is a strong ion exchange resin, which means it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. It forms insoluble complexes with bile acids in the intestine, which are then excreted in the feces. As a result of this loss of bile acids, more plasma cholesterol is converted to bile acids in the liver to normalise levels. This conversion of cholesterol into bile acids lowers plasma cholesterol levels.
The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer.
Approval history
- approvedAug 3, 1973
Chemistry & pharmacology
SMILES
CCc1ccc(cc1)C(C)CCc2ccc(cc2)[N+](C)(C)C- Mol. weight
- 296.48 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2110633 ↗
- WikipediaColestyramine ↗
- NCATS4B33BGI082 ↗
- ChEMBLCHEMBL2104535 ↗
- ChEMBLCHEMBL1201625 ↗
- WikipediaTang ↗
Also known as
- a3384
- a3384
- cholestyramine
- cholestyramine
- cholestyramine
- cholestyramine
- cholestyramine
- cholestyramine
- cholestyramine
- cholestyramine
- cholestyramine chloride
- cholestyramine resin
- cholestyramine resin
- cholestyramine resin
- cholestyramine resin chloride
- cholybar
- colestyramin
- colestyramine
- colestyramine
- colestyramine
- colestyramine
- duolite ap143 resin
- questran
- questran
- questran
- questran light
- tang
- tang
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06454383 | Phase 1 | May 13, 2024 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT05966727 | N/A | Dec 31, 2023 | University of Nice Sophia Antipolis |
| NCT06141473 | Phase 3 | Dec 13, 2023 | Sanofi |
| NCT05894928 | Phase 1 | Jun 7, 2023 | Eli Lilly, Loxo Oncology |
| NCT05577507 | Phase 4 | Mar 30, 2023 | Ain Shams University |
| NCT05443425 | Phase 1 | Dec 10, 2022 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT05014646 | Phase 2 | Nov 15, 2021 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT04335526 | N/A | May 1, 2020 | Seoul National University |
| NCT04235205 | Phase 2 | Feb 1, 2020 | EA Pharma Co., Ltd., Yokohama City University |
| NCT04046328 | Phase 2 | Sep 30, 2019 | Multispecialty Hospital Stanley Dudrick, Pharmasciences, Pirogov Russian National Research Medical University, Solumed Centrum Medyczne |
| NCT03510715 | Phase 3 | Sep 3, 2018 | Regeneron, Sanofi |
| NCT03510884 | Phase 3 | May 31, 2018 | Regeneron, Sanofi |
| NCT03303053 | Phase 3 | May 11, 2017 | Clinical Research Centre, Malaysia, Government of Malaysia, University Putra Malaysia |
| NCT02890992 | Phase 2 | Sep 1, 2016 | Regeneron, Sanofi |
| NCT02249897 | Phase 4 | Jan 1, 2015 | Clinica Alemana de Santiago, University of Chile |
| NCT02046629 | Phase 1 | May 1, 2014 | Sanofi |
| NCT02078856 | Phase 2 | Mar 1, 2014 | Albireo |
| NCT01863888 | Phase 3 | Oct 1, 2013 | Sanofi |
| NCT02963077 | Phase 1 | Jul 1, 2013 | Albireo |
| NCT02942602 | N/A | Jun 1, 2013 | Yonsei University |
Organizations
Research & Development (48)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Sanofi | For profit | 7 | 7 | 3 | 2010 |
| National Heart, Lung, and Blood Institute (NHLBI) | Government | 4 | 4 | 2 | 1971 |
| City of Hope National Medical Center | Academic/Hospital | 3 | 3 | 2 | 2021 |
| National Cancer Institute (NCI) | Government | 3 | 0 | 2 | 2021 |
| Regeneron | For profit | 3 | 0 | 2 | 2016 |
| Albireo | For profit | 2 | 2 | 2 | 2013 |
| Daiichi Sankyo | For profit | 2 | 0 | 1 | 2010 |
| L-Marc Research Center | Academic/Hospital | 2 | 2 | 1 | 2010 |
| Provident Clinical Research | For profit | 2 | 0 | 1 | 2010 |
| Ain Shams University | Academic/Hospital | 1 | 1 | 1 | 2023 |
| Baylor University | Academic/Hospital | 1 | 0 | 1 | 1973 |
| Biomedical Foundation for Cardiovascular Research of Padova | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Bio-Science Laboratories | For profit | 1 | 0 | 1 | 1973 |
| Centers for Disease Control and Prevention (CDC) | Government | 1 | 0 | 1 | 1973 |
| Clinica Alemana de Santiago | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Clinical Research Centre, Malaysia | Academic/Hospital | 1 | 1 | 1 | 2017 |
| EA Pharma Co., Ltd. | For profit | 1 | 0 | 1 | 2020 |
| Eli Lilly | For profit | 1 | 1 | 1 | 2023 |
| George Washington University | Academic/Hospital | 1 | 0 | 1 | 1973 |
| Government of Malaysia | Government | 1 | 0 | 1 | 2017 |
Marketing (23)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Ajanta Pharma Ltd | For profit | MKTG | Apr 6, 2020 |
| Alkem Labs Ltd | For profit | MKTG | Oct 19, 2021 |
| Allied Pharmaceutical Services | For profit | MKTG | Aug 15, 1996 |
| Ani Pharmaceuticals | For profit | MKTG | Oct 2, 1996 |
| Ani Pharmaceuticals | For profit | SYN | Oct 2, 1996 |
| Apothecon | For profit | MKTG | — |
| Bristol-Myers | For profit | NDA | Aug 3, 1973 |
| Bristol-Myers Squibb | For profit | NDA2 | Aug 3, 1973 |
| Chartwell Pharmaceuticals | For profit | MKTG | Aug 15, 1996 |
| Endo Pharmaceuticals | For profit | MKTG | Aug 26, 2005 |
| Epic Pharma Llc | For profit | MKTG | Aug 15, 1996 |
| Epic Pharma Llc | For profit | SYN | Aug 15, 1996 |
| Invatech | For profit | MKTG | Aug 15, 1996 |
| Macleods Pharmaceuticals, Ltd | For profit | MKTG | Oct 31, 2024 |
| Par Pharmaceuticals | For profit | MKTG | Aug 26, 2005 |
| Parke-Davis | For profit | MKTG | — |
| Precision Dose | For profit | MKTG | Nov 12, 2020 |
| Sandoz | For profit | MKTG | Aug 15, 1996 |
| Teva | For profit | SYN | Jul 9, 1997 |
| Teva | For profit | SYN | May 28, 1998 |
| Teva | For profit | MKTG | Sep 30, 1998 |
| Upsher-Smith Laboratories | For profit | MKTG | Feb 22, 1996 |
| Zydus Discovery DMCC | For profit | MKTG | Apr 25, 2017 |