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Valganciclovir

Names

[ CAS No. ]:
175865-60-8

[ Name ]:
Valganciclovir

[Synonym ]:
L-Valine 2-[(2-Amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl Ester
2-((2-Amino-6-oxo-1,6-dihydro-9H-purin-9-yl)methoxy)-3-hydroxypropyl L-Valinate
Valcyte
Cymeval
valganciclovir
2-[(2-Amino-6-oxo-1,6-dihydro-9H-purin-9-yl)methoxy]-3-hydroxypropyl L-valinate
L-Valine, 2-[(2-amino-3,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester
valgancyclovir

Biological Activity

[Description]:

Valganciclovir, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir. Valganciclovir is an antiviral medication used to treat cytomegalovirus infections.IC50 Value: Target: CMVin 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 [1].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 [2]. 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) [3].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> CMV
Research Areas >> Infection

[References]

[1]. Sugawara M, et al. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9.

[2]. Chawla JS, et al. Oral valganciclovir versus ganciclovir as delayed pre-emptive therapy for patients after allogeneic hematopoietic stem cell transplant: a pilot trial (04-0274) and review of the literature. Transpl Infect Dis. 2012 Jun;14(3):259-67.

[3]. O'Brien S, et al. Valganciclovir prevents cytomegalovirus reactivation in patients receiving alemtuzumab-based therapy. Blood. 2008 Feb 15;111(4):1816-9.


[Related Small Molecules]

Letermovir | Maribavir | Brivudine | B220 | Tomeglovir

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
629.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C14H22N6O5

[ Molecular Weight ]:
354.362

[ Flash Point ]:
334.3±34.3 °C

[ Exact Mass ]:
354.165161

[ PSA ]:
171.37000

[ LogP ]:
-1.28

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.678

Safety Information

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%


Related Compounds