Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00151)
Name
Colestid
Synonyms    Click to Show/Hide the Synonyms of This API
Colestid; Cholestabyl; Colestipol HCl; 37296-80-3; Colestipol hydrochloride [USAN:USP]; Flavored Colestid; Lestid; N'-[2-[2-(2-aminoethylamino)ethylamino]ethyl]ethane-1,2-diamine;hydrochloride; U-26597A; UNII-X7D10K905G; tetraethylenepentamine HCl; C11H28ClN5O.HCl; Copolymer of diethylenetriamine and 1-chloro-2,3-epoxypropane, hydrochloride (with approximately 1 out of 5 amine nitrogens protonated); SCHEMBL284758; DTXSID40190737; X7D10K905G; FT-0749664
Clinical Status
Approved
Disease Indication Hypertriglyceridaemia ICD-11: 5C80 [1]
PubChem CID
3084661
Formula
C8H24ClN5
Canonical SMILES
C(CNCCNCCNCCN)N.Cl
InChI
1S/C8H23N5.ClH/c9-1-3-11-5-7-13-8-6-12-4-2-10;/h11-13H,1-10H2;1H
InChIKey
GACQNVJDWUAPFY-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=3084661"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 225.76 Topological Polar Surface Area 88.1
XlogP N.A. Complexity 78.6
Heavy Atom Count 14 Rotatable Bond Count 10
Hydrogen Bond Donor Count 6 Hydrogen Bond Acceptor Count 5
Full List of Drug Formulations (DFMs) Containing This API
          Colestid 1000 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Triacetin; Povidone; Silicon dioxide; Carnauba wax; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Triacetin; Silicon dioxide; Carnauba wax; Hypromellose, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Greenstone; Pharmacia and Upjohn Company
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Magnesium stearate; Triacetin; Silicon dioxide; Carnauba wax; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company Avera McKennan Hospital; Carilion Materials Management
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Dibutyl sebacate; Polyethylene glycol 6000; Silicon dioxide; Cellacefate; Cellulose, microcrystalline; Copovidone k25-31; Hypromellose 2910 (6 mpa.s)
                   Dosage Form Oral Tablet
                   Company Impax Generics
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved colestid from the official website of the U.S. Food and Drug Administration.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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