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Valganciclovir hydrochloride

Valganciclovir hydrochloride structure

CAS No:
175865-59-5
Formula:
C14H22N6O5.ClH
Chemical Name:
Valganciclovir hydrochloride
Synonyms:
L-Valine,2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester,hydrochloride (1:1);L-Valine,2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester,monohydrochloride;RS 079070-194;Valganciclovir hydrochloride;Ro 107-9070/194;Valcyte
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Valganciclovir (hydrochloride), 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 b

Valganciclovir hydrochloride Basic Attributes

Molecular Weight：

390.825

Exact Mass：

390.141846

Characteristics

PSA：

167

Melting Point：

143 °C

Boiling Point：

629.1°C at 760 mmHg

Safety Information

Transport codes：

NONH for all modes of transport

Precautionary statement(s)：

P201, P202, P260, P264, P270, P281, P308+P313, P314, P405, P501

Hazard Statements：

H340

Drug Function and Efficacy

Valganciclovir is the L-valyl ester (prodrug) of ganciclovir, which is rapidly converted to ganciclovir by esterases in the small intestine and liver after oral administration. Ganciclovir is a synthetic 2'-deoxyguanosine analog that inhibits the replication of herpes viruses in vitro and in vivo. Sensitive human viruses include human cytomegalovirus (HCMV), herpes simplex virus-1 and herpes simplex virus-2 (HSV-1, HSV-2), human herpes virus-6, 7, 8 (HHV-6, 7, 8), Epstein-Barr virus, varicella-zoster virus (VZV) and hepatitis B virus. In cells infected with cytomegalovirus (CMV), ganciclovir is first phosphorylated to ganciclovir monophosphate by the viral protein kinase UL97. It is further phosphorylated to ganciclovir triphosphate by intracellular protein kinases and then slowly metabolized in the cell. Ganciclovir inhibits viral activity mainly by inhibiting viral DNA synthesis: (a) competitive inhibition of viral DNA polymerase, so that deoxyguanosine triphosphate cannot bind to DNA. (b) Ganciclovir triphosphate binds to viral DNA to terminate or limit the extension of the viral DNA chain. In vitro, the IC50 range of ganciclovir's antiviral effect on CMV is 0.08mcM (0.02ug/mL)-14mcM (3.5ug/mL).

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Valganciclovir Hydrochloride Tablets
Ingredients	Valganciclovir hydrochloride. Its chemical name is: 1.L-valine,-2[(2-amino-1,6-dihydro-6-oxo-9H-purine-9-yl)methoxy]-3-hydroxy-propyl ester, monohydrochloride. Molecular weight: C12H22N6O5?HCl
Indication	1. Drug interactions with valganciclovir hydrochloride tablets: In situ rat small intestinal permeability model studies have shown that valganciclovir has no interaction with valacyclovir, didanosine, nelfinavir, cyclosporine, omeprazole and mycophenolate mofetil. 2. Valganciclovir hydrochloride tablets are metabolized into ganciclovir, so interactions with ganciclovir are also expected to occur. 3. Drug interactions with ganciclovir: The plasma protein binding rate of ganciclovir is only 1-2%, so there will be no interaction of competing for protein binding sites. 4. Imipenem-cilastatin (Tianon): Convulsions have been reported with the combined use of ganciclovir and imipenem-cilastatin. These two drugs should not be used together unless the possible benefits far outweigh the potential risks (see Warnings). 5. Probenecid (
Specifications	0.45g (calculated as valganciclovir)

Valganciclovir Hydrochloride Tablets
Ingredients	The main ingredient of this product is 496.3 mg of valganciclovir hydrochloride, equivalent to 450 mg of valganciclovir. The chemical name of valganciclovir hydrochloride is: 1. L-valine,-2[(2-amino-1,6-dihydro-6-oxo-9H-purine-9-yl)methoxy]-3-hydroxy-propyl ester, monohydrochloride. Molecular formula: C12H22N6O5bull;HCl, molecular weight: 390.83.
Specifications	0.45 g (calculated as valganciclovir)

Registered Holders

AURORE LIFE SCIENCES PRIVATE LTD

United States
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MAITHRI LABORATORIES PRIVATE LTD

United States
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PHARMATHEN SA

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Guide of Valganciclovir hydrochloride

Description
Basic Attributes
Characteristics
Safety Information
Drug Function and Efficacy
Related Drugs
Registered Holders
Recommended Suppliers
Latest News
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