Valganciclovir

Category	Cytomegalovirus (CMV)
CAS	175865-60-8
Description	In cell culture model systems using Caco-2 cells for PEPT1 and SKPT cells for PEPT2, valganciclovir inhibited glycylsarcosine transport mediated by PEPT1 and PEPT2 with K(i) values (inhibition constant) of 1.68+/-0.30 and 0.043+/- 0.005 mM, respectively. The inhibition by valganciclovir was competitive in both cases. 37 patients were enrolled; 19 patients received treatment with VGV and 18 patients received treatment with GCV. The VGV was not inferior in efficacy to GCV as pre-emptive therapy, with rates of viral clearance at 28 days of 89.5% and 83%, respectively (P-value for non-inferiority = 0.030). Toxicities were similar between the 2 arms. No patients developed CMV disease. Patients being treated with an alemtuzumab-containing regimen received prophylaxis with either valaciclovir 500 mg orally daily orvalganciclovir 450 mg orally twice daily. None of the 20 patients randomized to valganciclovir experienced CMV reactivation (P = .004).

Quotation Now

Product Information

Synonyms	Valganciclovir
IUPAC Name	[2-[(2-amino-6-oxo-1H-purin-9-yl)methoxy]-3-hydroxypropyl] (2S)-2-amino-3-methylbutanoate
Molecular Weight	354.36
Molecular Formula	C14H22N6O5
Canonical SMILES	CC(C)C(C(=O)OCC(CO)OCN1C=NC2=C1NC(=NC2=O)N)N
InChI	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
Boiling Point	607.8ºC at 760 mmHg
Melting Point	194-197ºC
Flash Point	321.4ºC
Purity	>98%
Density	1.7±0.1 g/cm3
Solubility	In vitro: 10 mM in DMSO
Appearance	Solid powder
Storage	Store at -20°C
Complexity	528
Exact Mass	354.16516782
Index Of Refraction	1.692
In Vitro	In cell culture model systems using Caco-2 cells for PEPT1 and SKPT cells for PEPT2, valganciclovir inhibited glycylsarcosine transport mediated by PEPT1 and PEPT2 with K(i) values (inhibition constant) of 1.68+/-0.30 and 0.043+/- 0.005 mM, respectively. The inhibition by valganciclovir was competitive in both cases .
In Vivo	37 patients were enrolled; 19 patients received treatment with VGV and 18 patients received treatment with GCV. The VGV was not inferior in efficacy to GCV as pre-emptive therapy, with rates of viral clearance at 28 days of 89.5% and 83%, respectively (P-value for non-inferiority = 0.030). Toxicities were similar between the 2 arms. No patients developed CMV disease . Patients being treated with an alemtuzumab-containing regimen received prophylaxis with either valaciclovir 500 mg orally daily orvalganciclovir 450 mg orally twice daily. None of the 20 patients randomized to valganciclovir experienced CMV reactivation (P = .004) .
PSA	145.35000
Target	CMV
XLogP3-AA	-1.5