Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00018)
Name
Alfuzosin
Synonyms    Click to Show/Hide the Synonyms of This API
alfuzosin; 81403-80-7; Alfuzosina; Alfuzosine; Alfuzosinum; Uroxatral; SL 77499; ALFLUZOCIN; ALFLUZOSIN; CHEMBL709; CHEBI:51141; Alfuzosine [French]; Alfuzosinum [Latin]; Alfusosine; Alfuzosina [Spanish]; Alfuzosin [INN:BAN]; SL 77499-10; Alfuzosin (INN); SMR000466340; Xatral (TN); HSDB 7290; SL 77-499; SL-7749910; SL-77499-10; Alfuzosin/; N-(3-((4-amino-6,7-dimethoxyquinazolin-2-yl); SR-01000759345; Prestwick0_000322; Prestwick1_000322; Prestwick2_000322; Prestwick3_000322; Spectrum2_000505; Spectrum3_001063; Spectrum4_001208; Spectrum5_000817; SCHEMBL34477; BSPBio_000323; BSPBio_002646; KBioGR_001616; MLS000759449; MLS001424027; MLS006011887; SPECTRUM1505263; SPBio_000429; SPBio_002244; BPBio1_000357; GTPL7109; DTXSID6048549; KBio3_001866; HMS1922P11; HMS2051I10; HMS2093O06; HMS2235O22; HMS3369K03; HMS3393I10; HMS3749I05; HMS3886O22; Pharmakon1600-01505263; ACT03219; HY-B0192; ABP000595; BDBM50033110; CCG-39585; MFCD00865792; NSC760065; STK643675; AKOS005574697; CCG-100859; DB00346; MCULE-9094645643; NC00109; NSC-760065; SDCCGSBI-0206735.P002; VA10203; NCGC00095152-01; NCGC00095152-02; NCGC00095152-03; NCGC00095152-04; NCGC00095152-05; NCGC00095152-07; NCGC00095152-19; SBI-0206735.P001; AB0014226; DB-056523; AB00514667; FT-0630891; D07124; AB00514667-07; AB00514667-09; AB00514667-10; AB00514667_11; AB00514667_12; (methyl)amino)propyl)tetrahydrofuran-2-carboxamide; 403A807; A840122; L001317; Q2736873; SR-01000759345-4; BRD-A09056319-001-02-2; BRD-A09056319-001-05-5; BRD-A09056319-003-03-6; 1100050-87-0
Clinical Status
Approved
Disease Indication Prostatic hyperplasia ICD-11: GA90 [1]
PubChem CID
2092
Formula
C19H27N5O4
Canonical SMILES
CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC
InChI
1S/C19H27N5O4/c1-24(8-5-7-21-18(25)14-6-4-9-28-14)19-22-13-11-16(27-3)15(26-2)10-12(13)17(20)23-19/h10-11,14H,4-9H2,1-3H3,(H,21,25)(H2,20,22,23)
InChIKey
WNMJYKCGWZFFKR-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=2092"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 389.4 Topological Polar Surface Area 112
XlogP 1.7 Complexity 511
Heavy Atom Count 28 Rotatable Bond Count 8
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Alfuzosin 10 mg tablet Click to Show/Hide the Full List of Formulation(s):        15 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; Mannitol; Ferric oxide yellow; Povidone; Silicon dioxide; Cellulose, microcrystalline; Ethylcellulose (100 mpa.s); Hydrogenated castor oil; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Physicians Total Care
                   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]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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; Mannitol; Ferric oxide yellow; Silicon dioxide; Cellulose, microcrystalline; Ethylcellulose (100 mpa.s); Hydrogenated castor oil; Hypromelloses; Povidones
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Concordia Pharmaceuticals; Covis Pharmaceuticals; Sanofi-Aventis
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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; Anhydrous dibasic calcium phosphate; Propylene glycol; Titanium dioxide; Povidone k30; Silicon dioxide; Carbomer homopolymer type b (allyl sucrose crosslinked); Hydrogenated cottonseed oil; Hypromellose 2208 (100 mpa.s); Hypromellose 2910 (5 mpa.s)
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Aurobindo Pharma; Citron Pharma
                   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 %) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Lactose monohydrate; Magnesium stearate; Ferric oxide yellow; Talc; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromellose 2910 (15 mpa.s)
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Wockhardt
                   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) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Anhydrous lactose; Magnesium stearate; Talc; Povidone; Colloidal silicon dioxide; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Torrent Pharmaceuticals
                   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) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Lactose monohydrate; Magnesium stearate; Silicon dioxide; Hypromellose 2208 (100000 mpa.s); Hypromellose 2910 (5 mpa.s); Povidone k29/32
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Unichem Pharmaceuticals
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Magnesium stearate; Talc; Silicon dioxide; Dimethylaminoethyl methacrylate - butyl methacrylate - methyl methacrylate copolymer; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Bryant Ranch Prepack; DirectRX; Sun Pharmaceutical Industries
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Magnesium stearate; Talc; Silicon dioxide; Dimethylaminoethyl methacrylate - butyl methacrylate - methyl methacrylate copolymer; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Aidarex Pharmaceuticals
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Magnesium stearate; Silicon dioxide; Cellulose, microcrystalline; Guar gum; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Avera McKennan Hospital; Camber Pharmaceuticals; Cipla
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Ferric oxide yellow; Hypromellose 2208 (4000 mpa.s); Polyvinyl acetate phthalate
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Physicians Total Care
                   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) [4]
             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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Ferric oxide yellow; Hypromellose 2208 (4000 mpa.s); Polyvinyl acetate phthalate
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Apotex
                   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) [4]
             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
Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Ferric oxide yellow; Hypromellose 2208 (4000 mpa.s); Polyvinyl acetate phthalate
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Golden State Medical Supply
                   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) [4]
             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
Lactose monohydrate; Magnesium stearate; Hypromelloses; Povidones
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Mylan Pharamceuticals
                   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) [4]
             Drug Formulation 14 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; Cellulose, microcrystalline; Colloidal silicon dioxide; Guar gum; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Exelan Pharmaceuticals
                   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) [4]
             Drug Formulation 15 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; Cellulose, microcrystalline; Guar gum; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Liberty Pharmaceuticals
                   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) [4]
References
1 FDA label for approved alfuzosin 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 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 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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