Valganciclovir hydrochloride Property

Melting point:

162-164°C

storage temp. 

Keep in dark place,Inert atmosphere,2-8°C

solubility 

H2O: ≥8mg/mL

form 

powder

color 

white to tan

Stability:

Hygroscopic

InChIKey

ZORWARFPXPVJLW-MTFPJWTKSA-N

CAS DataBase Reference

175865-59-5

Safety

WGK Germany 

3

HS Code 

2933595960

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P330Rinse mouth.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

Valganciclovir hydrochloride Chemical Properties,Usage,Production

Description

Valganciclovir hydrochloride, a prodrug of the antiviral ganciclovir, was launched in the US for the oral treatment of cytemegalovirus (CMV) retinitis, a sight-threatening complication in patients with AIDS. This L-Valyl ester prodrug can be prepared in three steps from the nucleoside analog ganciclovir by trimethylsilyl-protection of the amino group, coupling with N-benzyloxycarbonyl-L-valine-N-carboxyanhydride, hydrolysis with hydrochloric acid and hydrogenolysis of the Cbz-protecting group. Valganciclovir is well absorbed and rapidly hydrolyzed to ganciclovir by intracellular esterases in the intestinal mucosal cells and by hepatic esterases. Unlike ganciclovir, valganciclovir was demonstrated to be actively transported by the intestinal peptide transporter PEPT1 in Caco-2 cells. As a consequence, its absolute bioavailability in human was 10-fold higher compared to ganciclovir (6%). In clinical trials, it was shown that a twice-daily 900 mg dose of valganciclovir resulted in similar systemic ganciclovir exposure to 5 mg/kg twice-daily intravenous injection of ganciclovir. Valganciclovir concentrations could not be quantified in most patients within three to four hours. In a randomized non-blind phase III clinical trial, oral valganciclovir (900 mg twice daily for three weeks then 900 mg once daily for one week) was as effective as intravenous ganciclovir (5 mg/kg twice daily for three weeks then 5 mg/kg once daily). Oral treatment with valganciclovir avoided catheter-related infection that sometimes occurred with intravenous ganciclovir.

Chemical Properties

White Crystalline Solid

Originator

Roche (Switzerland)

Uses

Valganciclovir hydrochloride hydrate may be used in HIV-related cell signaling studies.

Uses

A pro-drug of ganciclovir. Used in treatment of retro-virus

Uses

antibacterial, inhibits protein synthesis

Uses

Valganciclovir is the valyl ester prodrug of ganciclovir , an antiviral agent used for the treatment of HIV associated retinitis and for the prevention of post transplant cytomegalovirus (CMV) infections. Upon oral administration, intestinal and hepatic esterases rapidly convert valganciclovir to ganciclovir, which can inhibit viral DNA synthesis (IC50 = 0.95 μM) by targeting the CMV polymerase.

brand name

Valcyte (Roche).

General Description

Valganciclovir Hydrochloride is the L-valyl ester of ganciclovir and an antiviral drug, widely used to treat cytomegalovirus infections.
Certified pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to pharmacopeia primary standards.

Biochem/physiol Actions

Valganciclovir hydrochloride hydrate is an antiviral used to treat cytomegalovirus infection. It is the prodrug of ganciclovir, a synthetic analog of 2′-deoxy-guanosine which is phosphorylated to a dGTP analog that competitively inhibits the incorporation of dGTP by viral DNA polymerase.

Side effects

Side effects of Valganciclovir hydrochloride include: leukopenia, neutropenia, anaemia, thrombocytopenia, pancytopenia, bone marrow failure and aplastic anaemia. Based on animal data and limited human data, Valganciclovir Oral Solution may temporarily or permanently inhibit spermatogenesis in males and inhibit fertility in females, which in turn may lead to birth defects in humans. It may also cause cancer in humans.