colestipol
Trade name: colestid
Approved
Apr 4, 1977
Tetraethylenepentamine (TEPA) is a low-molecular-weight linear polyamine exerting metal-chelating properties. TEPA is widely used in industrial applications. The principal hazards that arise in working with TEPA are those associated with similar organic amines; namely, a corrosive action on skin and eyes. TEPA biological activity was attributed to its effect on cellular Cu levels as (a) treatment with TEPA resulted in reduction of cellular Cu, and (b) excess of Cu reversed TEPA's activity and accelerated differentiation. TEPA was shown to attenuate the differentiation of ex vivo cultured hematopoietic cells resulting in preferential expansion of early progenitors. A phase I/II trial was performed to test the feasibility and safety of transplantation of CD133+ cord blood (CB) hematopoietic progenitors cultured in media containing stem cell factor, FLT-3 ligand, interleukin-6, thrombopoietin and TEPA. Transplanting a population of CD133+ CB cells which were expanded ex vivo for 21 days using SCF, FLT3, IL-6, TPO and the copper chelator TEPA (StemEx) was feasible. The expanded cells were well tolerated, with no infusion-related adverse events observed. — NCATS
Clinical trial activity
6 trials · 10 clinical orgs · 8 marketing orgs
Earliest trial started Jun 1, 1980 (NCT00000599)
Timeline
1970s
- Apr 4, 1977
Pharmacia & Upjohn — Earliest FDA Approval
- Apr 4, 1977
Pfizer — Marketing Organization
- Apr 4, 1977
Pharmacia & Upjohn — NDA Secondary Org
- Apr 4, 1977
Pharmacia & Upjohn — NDA Organization
- Apr 4, 1977
Pfizer — NDA Secondary Org
1980s
- Jan 1, 1980
Earliest Phase 3 Sponsor(trial)
2000s
- May 2, 2006
Impax Laboratories — Marketing Organization
2020s
- Mar 10, 2022
Zydus Discovery DMCC — Marketing Organization
- Mar 10, 2023
Ani Pharmaceuticals — Marketing Organization
- Aug 16, 2024
Edenbridge Pharms — Marketing Organization
- Dec 3, 2024
RiconPharma — Marketing Organization
- Sep 15, 2025
PHARMOBEDIENT — Marketing Organization
Indications
Approved for
Studied for
- Arterial Occlusive Diseases · Phase 3
- Atherosclerosis · Phase 3
- Breast Neoplasms · Phase 2
- Cardiovascular Diseases · Phase 3
- Carotid Artery Diseases · Phase 3
- Cerebrovascular Disorders · Phase 3
- Coronary Artery Disease · Phase 3
- Coronary Disease · Phase 3
- Drugs, Investigational · Phase 1
- Healthy Volunteers · Phase 1
- Heart Diseases · Phase 3
- Hematologic Neoplasms · Phase 2
- Hypercholesterolemia · Phase 4
- Hyperlipidemias · Phase 4
- Intracranial Arteriosclerosis · Phase 3
- Myocardial Ischemia · Phase 3
- Protoporphyria, Erythropoietic · Phase 2/Phase 3
Mechanism of action
- Bile acidsSEQUESTERING AGENT
Bile acids sequestering agent
Approval history
- approvedPriority reviewApr 4, 1977
Chemistry & pharmacology
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaColestipol ↗
- NCATSK50N755924 ↗
- ChEMBLCHEMBL1909303 ↗
- ChEMBLCHEMBL1201474 ↗
Also known as
- cholestabyl
- cholestipol
- colestid
- colestid
- colestid
- colestid flavored colestid
- colestid orange
- colestipol
- colestipol
- colestipol
- colestipol
- colestipol
- colestipol
- colestipol
- colestipol
- colestipol
- colestipol hcl
- colestipol hcl
- colestipol hcl
- colestipol hydrochloride
- colestipol hydrochloride
- colestipol hydrochloride
- colestipol hydrochloride
- colestipolum
- colestipolum
- copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
- copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
- epichlorohydrin-tetraethylenepentamine polymer
- epichlorohydrin-tetraethylenepentamine polymer
- flavored colestid
- flavored colestid
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02400476 | Phase 2 | Feb 1, 2015 | Puma Biotechnology, Inc. |
| NCT02263547 | Phase 1 | Jan 1, 2015 | Genzyme, University of South Florida |
| NCT01422915 | Phase 2/Phase 3 (Phase 3) | May 1, 2011 | Harvard University |
| NCT00203476 | Phase 4 | May 1, 2005 | American Society of Health-System Pharmacists Research and Education Foundation, Department of Veteran Affairs, Tuscaloosa Research & Education Advancement Corporation (TREAC) |
| NCT00000512 | Phase 3 | Jan 1, 1984 | National Heart, Lung, and Blood Institute (NHLBI), University of Washington |
| NCT00000599 | Phase 3 | Jun 1, 1980 | National Heart, Lung, and Blood Institute (NHLBI), University of Southern California |
Organizations
Research & Development (10)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Heart, Lung, and Blood Institute (NHLBI) | Government | 2 | 1 | 1 | 1980 |
| American Society of Health-System Pharmacists Research and Education Foundation | Academic/Hospital | 1 | 0 | 1 | 2005 |
| Department of Veteran Affairs | Government | 1 | 0 | 1 | 2005 |
| Genzyme | For profit | 1 | 0 | 1 | 2015 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Puma Biotechnology, Inc. | For profit | 1 | 1 | 1 | 2015 |
| Tuscaloosa Research & Education Advancement Corporation (TREAC) | Academic/Hospital | 1 | 1 | 1 | 2005 |
| University of Southern California | Academic/Hospital | 1 | 0 | 1 | 1980 |
| University of South Florida | Academic/Hospital | 1 | 1 | 1 | 2015 |
| University of Washington | Academic/Hospital | 1 | 1 | 1 | 1984 |
Marketing (10)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Ani Pharmaceuticals | For profit | MKTG | Mar 10, 2023 |
| Edenbridge Pharms | For profit | MKTG | Aug 16, 2024 |
| Impax Laboratories | For profit | MKTG | May 2, 2006 |
| PHARMOBEDIENT | For profit | MKTG | Sep 15, 2025 |
| Pfizer | For profit | MKTG | Apr 4, 1977 |
| Pfizer | For profit | NDA2 | Apr 4, 1977 |
| Pharmacia & Upjohn | For profit | NDA2 | Apr 4, 1977 |
| Pharmacia & Upjohn | For profit | NDA | Apr 4, 1977 |
| RiconPharma | For profit | MKTG | Dec 3, 2024 |
| Zydus Discovery DMCC | For profit | MKTG | Mar 10, 2022 |