Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00716)
Name
Valganciclovir
Synonyms    Click to Show/Hide the Synonyms of This API
175865-60-8; Cymeval; Valcyte; L-Valine, ester with ganciclovir; CHEBI:63635; L-Valine, 2-((2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy)-3-hydroxypropyl ester; Valganciclovir [INN:BAN]; 2-[(2-amino-6-oxo-6,9-dihydro-3H-purin-9-yl)methoxy]-3-hydroxypropyl (2S)-2-amino-3-methylbutanoate; Valganciclovir (INN); C14H22N6O5; NCGC00168779-01; HSDB 8085; L-Valine, 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester; 5-Amino-3-[1-(hydroxymethyl)-2-(L-valyloxy)ethoxymethyl]-6,7-dihydro-3H-imidazo[4,5-d]pyrimidin-7-one; RS 79070; RO1079070/194; SCHEMBL28996; GTPL4716; CHEMBL1201314; DTXSID8048288; SCHEMBL12672612; SCHEMBL22357189; (2S)-2-((2-Amino-6-oxo-1H-purin-9(6H)-yl)methoxy)-3-hydroxypropyl 2-amino-3-methylbutanoate; HY-A0032; AKOS015896083; AKOS015966553; CS-0950; DB01610; 2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy]-3-hydroxypropyl L-valinate; NCGC00387997-02; NCGC00387997-04; AM807983; Ro-1079070/194; D02495; W-5321; AB01563009_01; 865V608; Q423384; BRD-A50922295-003-01-9; (2S)-2-amino-3-methyl-butyric acid [2-[(2-amino-6-keto-3H-purin-9-yl)methoxy]-3-hydroxy-propyl] ester; [2-[(2-amino-6-oxo-1H-purin-9-yl)methoxy]-3-hydroxy-propyl] (2S)-2-amino-3-methyl-butanoate
Clinical Status
Approved
Disease Indication Cytomegalovirus infection ICD-11: 1D82 [1]
PubChem CID
135413535
Formula
C14H22N6O5
Canonical SMILES
CC(C)[C@@H](C(=O)OCC(CO)OCN1C=NC2=C1N=C(NC2=O)N)N
InChI
1S/C14H22N6O5/c1-7(2)9(15)13(23)24-4-8(3-21)25-6-20-5-17-10-11(20)18-14(16)19-12(10)22/h5,7-9,21H,3-4,6,15H2,1-2H3,(H3,16,18,19,22)/t8?,9-/m0/s1
InChIKey
WPVFJKSGQUFQAP-GKAPJAKFSA-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=135413535"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 354.36 Topological Polar Surface Area 167
XlogP -1.5 Complexity 528
Heavy Atom Count 25 Rotatable Bond Count 9
Hydrogen Bond Donor Count 4 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Valganciclovir 450 mg tablet Click to Show/Hide the Full List of Formulation(s):          9 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
Stearic acid; Ferric oxide red; Talc; Titanium dioxide; Crospovidone; Polyethylene glycol 4000; Polyvinyl alcohol; Povidone k30; Silicon dioxide; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company AvKARE
                   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) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [5]
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
Stearic acid; Ferric oxide red; Talc; Titanium dioxide; Crospovidone; Polyethylene glycol 4000; Povidone k30; Silicon dioxide; Cellulose, microcrystalline; Polyvinyl alcohol, unspecified
                   Dosage Form Oral Tablet
                   Company Qualitest Pharmaceuticals
                   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) [2]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [5]
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
Stearic acid; Ferric oxide red; Titanium dioxide; Crospovidone; Polysorbate 80; Povidone; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company AvPAK; Camber Pharmaceuticals
                   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) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Crospovidone 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
Stearic acid; Ferric oxide red; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Povidone k30; Crospovidone (15 mpa.s at 5%); Hypromellose 2910 (6 mpa.s); Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Genentech
                   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) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [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
Magnesium stearate; Ferric oxide red; Titanium dioxide; Crospovidone; Polyethylene glycol 400; Polysorbate 80; Povidone k30; Cellulose, microcrystalline; Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s)
                   Dosage Form Oral Tablet
                   Company Aurobindo Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             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
Magnesium stearate; Ferric oxide red; Titanium dioxide; Crospovidone; Polysorbate 80; Povidone k30; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   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
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
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 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; Ferric oxide red; Titanium dioxide; Crospovidone; Polyethylene glycol 400; Polysorbate 80; Povidone k30; Cellulose, microcrystalline; Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s)
                   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
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             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; Ferric oxide red; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Povidone k30; Crospovidone (15 mpa.s at 5%); Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s); Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company McKesson
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             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; Ferric oxide red; Titanium dioxide; Polysorbate 20; Crospovidone (15 mpa.s at 5%); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 20 DIG Info Cytochrome P450 2E1 (IC50 = 64.1 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved valganciclovir from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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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