Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00621)
Name
Sevelamer
Synonyms    Click to Show/Hide the Synonyms of This API
Sevelamer; 52757-95-6; 2-(chloromethyl)oxirane;prop-2-en-1-amine; Sevelamer [INN:BAN]; UNII-941N5DUU5C; HSDB 7608; Sevelamer (INN); Allylamine-epichlorohydrin copolymer; SCHEMBL726092; 2-Propen-1-amine, polymer with (chloromethyl)oxirane; 941N5DUU5C; 3-(Trifluoromethoxy)cinnamicacid; CHEMBL1201798; DB00658; NCGC00522026-01; D08512; 2-Propen-1-amine - 2-(chloromethyl)oxirane (1:1); Oxirane, (chloromethyl)-, polymer with 2-propen-1-amine; 2-Propen-1-amine Hydrochloride polymer with 2-(Chloromethyl)oxirane
Clinical Status
Approved
Disease Indication Chronic kidney disease ICD-11: GB61 [1]
PubChem CID
3085017
Formula
C6H12ClNO
Canonical SMILES
C=CCN.C1C(O1)CCl
InChI
1S/C3H5ClO.C3H7N/c4-1-3-2-5-3;1-2-3-4/h3H,1-2H2;2H,1,3-4H2
InChIKey
ZNSIZMQNQCNRBW-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=3085017"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 149.62 Topological Polar Surface Area 38.6
XlogP N.A. Complexity 55.1
Heavy Atom Count 9 Rotatable Bond Count 2
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Sevelamer 800 mg tablet Click to Show/Hide the Full List of Formulation(s):        13 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
Mannitol; Zinc stearate; Ammonia; Ferrosoferric oxide; Propylene glycol; Talc; Crospovidone; Lecithin, soybean; Polyvinyl alcohol; Silicon dioxide; Hydroxypropyl cellulose (type h); Shellac; Xanthan gum
                   Dosage Form Oral Tablet
                   Company Dr Reddy's Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [4]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Mannitol; Zinc stearate; Ammonia; Ferrosoferric oxide; Propylene glycol; Talc; Lecithin, soybean; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hydroxypropyl cellulose (1200000 mw); Polyvinyl alcohol, unspecified; Shellac; Xanthan gum
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Stearic acid; Isopropyl alcohol; Ferrosoferric oxide; Propylene glycol; Water; Silicon dioxide; Hypromellose 2910 (15 mpa.s); Hypromellose 2910 (5 mpa.s)
                   Dosage Form Oral Tablet
                   Company Department Of Health Central Pharmacy
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [6]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Glyceryl dibehenate; Mannitol; Ammonia; Ferrosoferric oxide; Propylene glycol; Talc; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Diacetylated monoglycerides; Hydroxypropyl cellulose (120000 mw); Hypromellose, unspecified; Shellac
                   Dosage Form Oral Tablet
                   Company American Health Packaging; Aurobindo Pharma; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             Drug Formulation 5 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
Stearic acid; Isopropyl alcohol; Ferrosoferric oxide; Propylene glycol; Water; Colloidal silicon dioxide; Hypromellose 2910 (15 mpa.s); Hypromellose 2910 (5 mpa.s)
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [6]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
             Drug Formulation 6 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
Stearic acid; Talc; Titanium dioxide; Polyethylene glycol 3350; Silicon dioxide; Cellulose, microcrystalline; Polyvinyl alcohol, unspecified
                   Dosage Form Oral Tablet
                   Company AvKARE; Impax Generics
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [6]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             Drug Formulation 7 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
Isopropyl alcohol; Ferrosoferric oxide; Propylene glycol
                   Dosage Form Oral Tablet
                   Company Atlantic Biologicals; Cardinal Health; Genzyme Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
             Drug Formulation 8 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
Isopropyl alcohol; Ferrosoferric oxide; Propylene glycol
                   Dosage Form Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
             Drug Formulation 9 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
Sodium stearyl fumarate; Talc; Silicon dioxide; Cellulose, microcrystalline; Crospovidone, unspecified; Diacetylated monoglycerides; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified
                   Dosage Form Oral Tablet
                   Company Cipla; Exelan Pharmaceuticals; InvaGen Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [8]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             Drug Formulation 10 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
Sodium stearyl fumarate; Talc; Silicon dioxide; Cellulose, microcrystalline; Crospovidone, unspecified; Diacetylated monoglycerides; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [8]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             Drug Formulation 11 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
Zinc stearate; Ammonia; Ferrosoferric oxide; Propylene glycol; Silicon dioxide; Cellulose, microcrystalline; Diacetylated monoglycerides; Hypromelloses; Shellac
                   Dosage Form Oral Tablet
                   Company Amneal Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             Drug Formulation 12 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
Zinc stearate; Ferrosoferric oxide; Sodium chloride; Diacetylated monoglycerides; Hypromellose, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Kaiser Foundation Hospitals; Winthrop
             Drug Formulation 13 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
Zinc stearate; Ferrosoferric oxide; Sodium chloride; Cellulose, microcrystalline; Diacetylated monoglycerides; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Global Pharmaceuticals
          Sevelamer 400 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Isopropyl alcohol; Ferrosoferric oxide; Propylene glycol
                   Dosage Form Oral Tablet
                   Company Cardinal Health; Genzyme Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
References
1 FDA label for approved sevelamer from the official website of the U.S. Food and Drug Administration.
2 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
4 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
7 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.
8 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.

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