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Valganciclovir hydrochloride
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API and Intermediates
- Product description
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Product Intro
Valganciclovir hydrochloride is an oral anti cytomegalovirus (CMV) infection drug developed by Roche, Switzerland. It was approved by FDA in May 2001. It is clinically used to treat acute retinitis caused by CMV infection in patients with acquired immunodeficiency syndrome (AIDS). Its indications were expanded in May 2003 to prevent and treat CMV infection secondary to organ transplantation. This product is the prodrug of ganciclovir. After oral administration, it is rapidly hydrolyzed into ganciclovir by esterase in intestinal and liver cells, so as to exert its efficacy. The bioavailability of oral absorption is 60%, and the toxicity is greatly reduced.
Function
Valganciclovir is a DNA polymerase inhibitor. After oral administration, it is rapidly hydrolyzed to ganciclovir under the action of intestinal mucosal cell esterase and liver esterase. Therefore, its pharmacodynamic characteristics are the pharmacodynamic characteristics of ganciclovir. Ganciclovir generates ganciclovir triphosphate under the phosphorylation of viral and intracellular enzymes. The latter competes with deoxyguanosine triphosphate (dGTP) as the substrate of viral DNA polymerase, so it inhibits the synthesis of viral DNA and produces anti CMV activity. The in vitro anti CMV activity of ganciclovir was 26 times that of alovir, and its IC50 was 0.6 ~ 4.9 μ Mol · L-1, average 2.7 μ mol·L-1 。
Application
Valganciclovir hydrochloride is mainly used to treat CMV infection in immunodeficient patients, such as retinitis, pneumonia, gastroenteritis, liver and central nervous system infection. The main characteristics of ganciclovir are its efficacy in treating CMV virus and hepatitis B virus infection. In vitro experiments showed that ganciclovir had strong activities against cytomegalovirus, HSV-1, HSV-2, varicella zoster virus and EB virus. The inhibitory activities against cytomegalovirus and E-B virus were 50 times stronger than acyclovir and 15 ~ 19 times stronger than foscarnet.
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