Valganciclovir Hydrochloride

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Cat Number

API175865595

CAS Number

175865-59-5

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CAS Number

175865-59-5

EINECS

641-360-4

Storage

2-8℃

Synonyms

L-Valine,2-[(2-aMino-1,6-dihydro-6-oxo-9H-purin-9-yl)Methoxy]-3-hydroxypropyl ester,hydrochloride;L-Valine, 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester, monohydrochloride hydrate;Valganciclovir hydrochloride hydrate

Molecular Formula

C14H23ClN6O5

Molecular Weight

390.82

Smiles

CC(C)[C@@H](C(=O)OCC(CO)OCN1C=NC2=C1N=C(NC2=O)N)N.Cl

Appearance

White to off-white solid

Melting Point

162-164℃

General Description

Valganciclovir Hydrochloride is a prodrug of ganciclovir, developed to overcome the poor oral bioavailability of ganciclovir itself. It is the L-valyl ester of ganciclovir and is rapidly hydrolyzed after oral administration to ganciclovir. As a synthetic nucleoside analog structurally related to acyclovir, it provides potent activity against cytomegalovirus (CMV) and other herpesviruses.

Mechanism of Action

Following oral absorption and hydrolysis to ganciclovir, Valganciclovir Hydrochloride is phosphorylated by cellular kinases to its active triphosphate form, which selectively inhibits CMV DNA polymerase. The triphosphate accumulates preferentially in CMV-infected cells due to enhanced initial phosphorylation by the viral UL97 kinase, providing targeted antiviral activity with reduced off-target effects.

Application

Valganciclovir Hydrochloride is indicated for the treatment of cytomegalovirus (CMV) retinitis in patients with acquired immunodeficiency syndrome (AIDS) and for the prevention of CMV disease in high-risk solid organ transplant recipients. Its oral administration offers a significant clinical advantage over intravenous ganciclovir while maintaining equivalent systemic exposure.

Valganciclovir HCl (VGH) is used for cytomegalovirus retinitis but requires 900 mg twice daily, causing side effects from repeat dosing. A single-core osmotic pump tablet delivering 450 mg once daily was developed to reduce dose and frequency. The optimized formulation achieved zero-order controlled release over 24 hours. In vivo pharmacokinetic studies showed the single 450 mg dose produced an AUC of 58.415 µg·h/ml, compared to 37.903 and 31.983 µg·h/ml for first and second doses of the marketed formulation. The higher AUC indicates sustained therapeutic levels with lower dose and reduced hepatic/nephrotic load. This osmotic pump formulation offers a promising alternative with improved efficacy and tolerability.

Fig. 1 A single-core osmotic pump tablet of Valganciclovir Hydrochloride. (Gundu R.; et al. 2022)

References

Gundu R, et al. Development and pharmacokinetic evaluation of osmotically controlled drug delivery system of Valganciclovir HCl for potential application in the treatment of CMV retinitis. Drug Delivery and Translational Research, 2022, 12(11): 2708-2729.

What is the recommended storage condition for Valganciclovir Hydrochloride?

It should be stored at 2-8°C in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

What documentation is provided with each batch of Valganciclovir Hydrochloride?

Each batch is accompanied by a Certificate of Analysis (COA) covering identity, potency, and relevant purity tests. Safety Data Sheets (SDS) are available upon request.

What is the minimum order quantity (MOQ) for Valganciclovir Hydrochloride?

Flexible MOQ options are available to support both early-stage research and large-scale manufacturing needs. Our team can tailor order quantities to match your specific requirements.

Can Valganciclovir Hydrochloride be used as a reference standard?

Pharmaceutical-grade material meeting strict identity and specification criteria is available; for reference standard applications, please consult our technical team.