Valganciclovir hydrochloride Struktur

Valganciclovir hydrochloride

Bezeichnung:Valganciclovir hydrochloride

CAS-Nr175865-59-5

Englisch Name:Valganciclovir hydrochloride

CBNumberCB0380410

SummenformelC14H23ClN6O5

Molgewicht390.82

MOL-Datei175865-59-5.mol

Valganciclovir hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	162-164°C
storage temp.	Keep in dark place,Inert atmosphere,2-8°C
Löslichkeit	H2O: ≥8mg/mL
Aggregatzustand	powder
Farbe	white to tan
Stabilität	Hygroscopic
InChIKey	ZORWARFPXPVJLW-MTFPJWTKSA-N
CAS Datenbank	175865-59-5

Sicherheit

WGK Germany	3
HS Code	2933595960

Gefahreninformationscode (GHS)

Valganciclovir hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
White Crystalline Solid
Originator
Roche (Switzerland)
Verwenden
A pro-drug of ganciclovir. Used in treatment of retro-virus
Verwenden
Valganciclovir hydrochloride hydrate may be used in HIV-related cell signaling studies.
Verwenden
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.
Verwenden
antibacterial, inhibits protein synthesis
Trademarks
Valcyte (Roche).
Allgemeine Beschreibung
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.

Valganciclovir hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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