Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00721)
Name
Vardenafil
Synonyms    Click to Show/Hide the Synonyms of This API
Levitra; 224785-90-4; Vivanza; UNII-UCE6F4125H; Levitra (TN); BAY 38-9456; BAY38-9456; CHEMBL1520; UCE6F4125H; 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE; CHEBI:46295; 224789-15-5; 2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one; Vardenafil ODT; 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one; 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propyl-1H,4H-imidazo[4,3-f][1,2,4]triazin-4-one; HSDB 7304; SR-05000001442; NCGC00167533-01; Vardenafil [USAN:INN:BAN]; Vardenafil (Vivanza); 2-(2-Ethoxy-5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl)-5-methyl-7-propyl-3H-imidazo(5,1-f)(1,2,4)triazin-4-one; Vardenafil (USAN/INN); EC 607-088-5; SCHEMBL5772; BSPBio_002392; 1-((3-(3,4-Dihydro-5-methyl-4-oxo-7-propylimidazo(5,1-f)-as-triazin-2-yl)-4-ethoxyphenyl)sulfonyl)-4-ethylpiperazine; GTPL7320; IMI044; DTXSID3048318; BDBM14776; HMS2089K04; HMS3715F19; BCP02961; EX-A2806; HY-B0442; STK642629; ZINC18324776; AKOS005574038; AKOS015994765; AKOS022186043; AT-4121; BAY-389456; CCG-221149; CID 110634; DB00862; GS-6519; KS-5073; MCULE-5211071344; SB17349; NCGC00167533-03; 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4-ol; Piperazine, 1-((3-(1,4-dihydro-5-methyl-4-oxo-7-propylimidazo(5,1-f)(1,2,4)triazin-2-yl)-4-ethoxyphenyl)sulfonyl)-4-ethyl-; BCP0726000254; SBI-0206836.P001; FT-0631204; FT-0675783; 85V904; D08668; AB00698215-08; AB01274740-01; AB01274740_02; AB01274740_03; AB01275440-01; Q424161; J-014730; SR-05000001442-1; SR-05000001442-2; BRD-K13926615-003-01-7; BRD-K13926615-003-02-5; Z2790753946; 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo(5,1-f)triazin-4(3H)-one; 2-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl)-5-methyl-7-propylimidazo[1,5-f][1,2,4]triazin-4(1H)-one; 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one; 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazine-4-one; 2-[2-ethoxy-5-(4-ethylpiperazine-1-sulfonyl)phenyl]-5-methyl-7-propyl-1H,4H-imidazo[4,3-f][1,2,4]triazin-4-one; 2-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propyl-imidazo[5,1-f][1,2,4]triazin-4-one; 2-{2-ethoxy-5-[(4-ethylpiperazine-1-)sulfonyl]phenyl}-5-methyl-7-propyl-3H,4H-imidazo[1,5-a][1,2,4]triazin-4-one; citric acid;2-[2-ethoxy-5-(4-ethylpiperazino)sulfonyl-phenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one; Imidazo[5,1-f][1,2,4]triazin-4(1H)-one, 2-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propyl-
Clinical Status
Approved
Disease Indication Erectile dysfunction ICD-11: HA01 [1]
PubChem CID
135400189
Formula
C23H32N6O4S
Canonical SMILES
CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C
InChI
1S/C23H32N6O4S/c1-5-8-20-24-16(4)21-23(30)25-22(26-29(20)21)18-15-17(9-10-19(18)33-7-3)34(31,32)28-13-11-27(6-2)12-14-28/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,30)
InChIKey
SECKRCOLJRRGGV-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=135400189"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 488.6 Topological Polar Surface Area 118
XlogP 2.5 Complexity 854
Heavy Atom Count 34 Rotatable Bond Count 8
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Vardenafil 10 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
Aspartame; Magnesium stearate; Mannitol; Sorbitol; Crospovidone; Silicon dioxide
                   Dosage Form Disintegrating 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]
Aspartame DIG Info Pregnane X receptor (Ki = 13 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Crospovidone 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
Aspartame; Magnesium stearate; Mannitol; Sorbitol; Silicon dioxide; Crospovidone (15 mpa.s at 5%)
                   Dosage Form Disintegrating Oral Tablet
                   Company GlaxoSmithKline
                   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]
Aspartame DIG Info Pregnane X receptor (Ki = 13 uM) [3]
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; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; PD-Rx Pharmaceuticals; 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]
Crospovidone 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
Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   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]
          Vardenafil 20 mg tablet Click to Show/Hide the Full List of Formulation(s):          3 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; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Kaiser Foundation Hospitals; 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]
Crospovidone 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; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack; PD-Rx 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]
Crospovidone 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; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   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]
          Vardenafil 5 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene 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
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Crospovidone 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; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   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]
          Vardenafil 2.5 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
Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   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]
References
1 FDA label for approved vardenafil 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 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 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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