Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00155)
Name
Crofelemer
Clinical Status
Approved
Disease Indication Human immunodeficiency virus infection ICD-11: 1C60 [1]
Full List of Drug Formulations (DFMs) Containing This API
          Crofelemer 125 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
Methylparaben; Ethyl acrylate; Magnesium stearate; Propylparaben; Talc; Titanium dioxide; Triethyl citrate; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Xanthan gum
                   Dosage Form Delayed Release Oral Tablet
                   Company Napo Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
methylparaben DIG Info Carbonic anhydrase VII (Ki = 780 nM) [2]
Ethyl acrylate DIG Info NFE2-related factor 2 (EC50 = 5110 nM) [3]
Propyl 4-hydroxybenzoate DIG Info Estrogen receptor alpha (IC50 = 11 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Crofelemer 125mg Delayed Release 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
Colloidal Silicon Dioxide; Croscarmellose Sodium; Magnesium Stearate; Microcrystalline Cellulose; Ethylacrylate; Methylacrylate Copolymer Dispersion; Talc; Triethyl Citrate; Xanthan Gum; Titanium Dioxide; Propyl Paraben; Methyl Paraben
                   Dosage Form Delayed Release Tablet
                   Company Napo Pharms
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
methylparaben DIG Info Carbonic anhydrase VII (Ki = 780 nM) [2]
Ethyl acrylate DIG Info NFE2-related factor 2 (EC50 = 5110 nM) [3]
Propyl 4-hydroxybenzoate DIG Info Estrogen receptor alpha (IC50 = 11 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [5]
References
1 FDA label for approved crofelemer from the official website of the U.S. Food and Drug Administration.
2 Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV. Bioorg Med Chem. 2013 Mar 15; 21(6):1564-9.
3 A novel chalcone derivative as Nrf2 activator attenuates learning and memory impairment in a scopolamine-induced mouse model. Eur J Med Chem. 2020 Jan 1; 185:111777.
4 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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