COLESTIPOL

First approved in 1977

Description
Sources: http://www.google.com/patents/WO1993000915A1?cl=enhttp://www.huntsman.com/performance_products/Media%20Library/a_MC348531CFA3EA9A2E040EBCD2B6B7B06/Products_MC348531D0B9FA9A2E040EBCD2B6B7B06/Amines_MC348531D0BECA9A2E040EBCD2B6B7B06/Ethyleneamines_MC348531D0CD3A9A2E040EBCD2B6B7B06/files/tetraethylenepentamine_tepa.pdf
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26581493 | http://pubs.acs.org/doi/abs/10.1021/ic50099a028?journalCode=inocaj | http://pubs.acs.org/doi/abs/10.1021/ic50048a017?journalCode=inocaj | https://clinicaltrials.gov/ct2/show/NCT01484470 | https://www.ncbi.nlm.nih.gov/pubmed/18209724 | https://www.ncbi.nlm.nih.gov/pubmed/16219531

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.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Oxidative Stress 160 Target ID: WP408 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18047399	Inhibitor 8297
Copper 16 Target ID: CHEMBL2363057 Sources: http://pubs.acs.org/doi/abs/10.1021/ic50099a028?journalCode=inocaj	Chelating Agent 142
Bile acids 3 Target ID: CHEMBL2364175 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017563s023,020222s005lbl.pdf	Binding Agent 1064

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hematologic malignancies 19 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18209724 http://www.bloodjournal.org/content/122/21/295?sso-checked=true https://clinicaltrials.gov/ct2/show/NCT01484470	Primary		Phase II 1132	StemEx Approved Use Unknown
Primary hypercholesterolemia 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017563s023,020222s005lbl.pdf	Palliative		Approved 8429	COLESTID Approved Use COLESTID Granules and FLAVORED COLESTID Granules are indicated as adjunctive therapy to diet for the reduction of elevated serum total and low-density lipoprotein (LDL) cholesterol in patients with primary hypercholesterolemia (elevated low density lipoproteins [LDL] cholesterol) who do not respond adequately to diet. Generally, COLESTID and FLAVORED COLESTID have no clinically significant effect on serum triglycerides, but with its use triglyceride levels may be raised in some patients. Launch Date 1977

PubMed

Title	Date	PubMed
Treatment of heterozygous familial hypercholesterolemia with lipid-lowering drugs.	1989 Jan-Feb	2492189
Inhibitors of hydroxymethylglutaryl coenzyme A reductase for treating hypercholesterolaemia.	1990 Sep 29	2224231
Currently available hypolipidaemic drugs and future therapeutic developments.	1995 Oct	8593127
Common hepatic lipase gene promoter variant determines clinical response to intensive lipid-lowering treatment.	2001 Feb 13	11171785
Application of capillary electrophoresis for organic acid analysis in herbal studies.	2001 Jul	11504059
Determinants of variable response to statin treatment in patients with refractory familial hypercholesterolemia.	2001 May	11348882
Effects of prolonged intensive lipid-lowering therapy on the characteristics of carotid atherosclerotic plaques in vivo by MRI: a case-control study.	2001 Oct	11597936
Effect of concomitant colestipol hydrochloride administration on the bioavailability of diltiazem from immediate- and sustained-release formulations.	2002 Dec	12469330
Cellular copper content modulates differentiation and self-renewal in cultures of cord blood-derived CD34+ cells.	2002 Mar	11849228
Low- and high-density lipoprotein cholesterol and ischemic cerebrovascular disease: the bezafibrate infarction prevention registry.	2002 May 13	11996608
2-D soft ferromagnet based on [Wv(CN)8]3- and CuII with a Tc of 34 K.	2002 May 21	12122703
Lipid-lowering therapy after coronary artery bypass grafting: time for more aggressive intervention.	2002 Nov 1	12434726
Aluminum accumulation and membrane fluidity alteration in synaptosomes isolated from rat brain cortex following aluminum ingestion: effect of cholesterol.	2002 Oct	12354633
Treatment of children with familial hypercholesterolemia with colestilan, a newly developed bile acid-binding resin.	2002 Oct	12204812
Differential effects of lipid-lowering therapies on stroke prevention: a meta-analysis of randomized trials.	2003 Mar 24	12639199
Statin use and cancer risk in the General Practice Research Database.	2004 Feb 9	14760377
Effectiveness and tolerability of ezetimibe add-on therapy to a bile acid resin-based regimen for hypercholesterolemia.	2004 Sep 15	15374793
Effect of time of administration on cholesterol-lowering by psyllium: a randomized cross-over study in normocholesterolemic or slightly hypercholesterolemic subjects.	2004 Sep 28	15453909
Sodium monofluoroacetate (Compound 1080) poisoning in dogs.	2005 Aug	16119418
A highly efficient preparative-scale generic immunoaffinity chromatography method for the purification of antibodies to hydrophobic haptens: purification procedure and monitoring tests.	2005 Dec 5	16202669
A bitter tale.	2005 Jan 6	15635787
Mitochondrial membrane potential is reduced in copper-deficient C2C12 cells in the absence of apoptosis.	2005 Jul	16037610
[Charge control and IR analysis of amine on diarylide yellow pigment PY14].	2005 Oct	16395888
Complementary therapy to target LDL cholesterol: the role of the ezetimibe/simvastatin combination.	2006	17319467
Genetically determined apo B levels and peak LDL density predict angiographic response to intensive lipid-lowering therapy.	2006 Apr	16594908
Prediction of estrogen receptor agonists and characterization of associated molecular descriptors by statistical learning methods.	2006 Nov	16497524
Synthesis of a quaternary amine anion exchange resin and study [of] its adsorption behaviour for chromate oxyanions.	2006 Sep 21	16682117
Is the fixed-dose combination of telmisartan and hydrochlorothiazide a good approach to treat hypertension?	2007	17703634
Bile acid sequestrants and the treatment of type 2 diabetes mellitus.	2007	17600387
Profiling recombinant major birch pollen allergen Bet v 1a and carbamylated variants with CZE and CIEF.	2007 Jul	17538926
In situ ligand reactions under hydrothermal conditions afford a novel zinc-substituted polyoxovanadate dimer.	2007 Oct 29	17915859
Pathogenesis and treatment of pruritus in cholestasis.	2008	18840005
Efficient CO2 capturer derived from as-synthesized MCM-41 modified with amine.	2008	18283702
Colesevelam HCl improves glycemic control and reduces LDL cholesterol in patients with inadequately controlled type 2 diabetes on sulfonylurea-based therapy.	2008 Aug	18458145
Thermodynamic and spectroscopic studies of lanthanides(III) complexation with polyamines in dimethyl sulfoxide.	2008 Feb 4	18166040
Transplantation of ex vivo expanded cord blood cells using the copper chelator tetraethylenepentamine: a phase I/II clinical trial.	2008 May	18209724
Preparation of polyurea capsules using electrocapillary emulsification.	2008 Oct 15	18768303
Primary biliary cirrhosis.	2009 Sep	19603170

Patents

Sample Use Guides

In Vivo Use Guide

The recommended daily adult dose is 5-30 g (granules) or 2-16 g (tablets) given once or in divided doses.

Route of Administration: Oral

In Vitro Use Guide

In vitro binding capacity is 1 mequiv cholic acid/g.

Substance Class	Polymer Created by `admin` on `Sat Dec 16 13:14:41 GMT 2023` Edited by `admin` on `Sat Dec 16 13:14:41 GMT 2023`
Record UNII	K50N755924
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

COLESTIPOL

Official Name

English

POLY(EPICHLOROHYDRIN-CO-TETRAETHYLENEPENTAMINE)

Common Name

English

COPOLYMER OF DIETHYLENETRIAMINE AND 1-CHLORO-2,3-EPOXYPROPANE

Common Name

English

colestipol [INN]

Common Name

English

COLESTIPOL [VANDF]

Common Name

English

NSC-147003

Code

English

COLESTIPOL [MI]

Common Name

English

Colestipol [WHO-DD]

Common Name

English

Classification Tree Code System Code

LIVERTOX

NBK548432