Medicine CAS 175865-59-5 Valganciclovir Hcl Powder Antiviral Valganciclovir Hydrochloride Pharmaceutical Chemical Valganciclovir
Product Description
Product Details
Product Name |
Valganciclovir |
CAS No. |
175865-59-5 |
MF |
C14H23ClN6O5 |
MW |
390.82 |
Appearance and shape |
Off-white powder |
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. 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.
Application & Function
It is used to prevent and treat CMV infection secondary to organ transplantation. The drug is a prodrug of ganciclovir (ganciclovir), which is an active ganciclovir valine ester. After oral administration, it can be quickly hydrolyzed into ganciclovir by phosphatase in the intestinal and liver cells. Its antiviral spectrum and mechanism of action are similar to ganciclovir, but its bioavailability is significantly higher than ganciclovir, and its oral absorption bioavailability is 62.4%, which is 10 times that of ganciclovir , And the toxicity is greatly reduced.
Specification