product name Nevirapine
Description: Nevirapine (also known as NSC 641530) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV-1 infection and AIDS. As with other antiretroviral drugs, HIV rapidly develops resistance if nevirapine is used alone, so recommended therapy consists of combinations of three or more antiretrovirals. Nevirapine in triple combination therapy has been shown to suppress viral load effectively when used as initial antiretroviral therapy.
References: Drug Metab Dispos. 1999 Dec;27(12):1488-95; Drug Metab Dispos. 1999 Dec;27(12):1434-47.
266.3
Formula
C15H14N4O
CAS No.
129618-40-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (199.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
NSC 641530
other peoduct :
| In Vitro |
In vitro activity: Nevirapine (NVP) itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). Nevirapine is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. Nevirapine is also an effective inhibitor of the endogenous RT in murine and human cell lines. Nevirapine exposure rescues the differentiation block present in acute myeloid leukemia (AML) cell lines and primary blasts from two AML patients, as indicated by morphological, functional and immunophenotypic assays. Nevirapine, a dipyridodiazepinone, is a highly specific inhibitor of HIV-1 reverse transcriptase (RT) which exhibits an IC50 = 84 nM in enzyme assays and IC50 = 40nM against HIV-1 replication in cell culture. Nevirapine alters the cleavage specificity of the RNase H, resulting Nevirapine-induced stimulation of RNase H activity beyond the increase expected from the change in cleavage specificity. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 4-CANVP is a major metabolite in all the male animals and the female mouse, dog, and monkey. 3-OHNVP is a major fecal metabolite in all animals except for the male rat. 4-CANVP is a major metabolite along with 12-OHNVP glucuronide in the bile of rats. |
| Animal model | |
| Formulation & Dosage | |
| References | Drug Metab Dispos. 1999 Dec;27(12):1488-95; Drug Metab Dispos. 1999 Dec;27(12):1434-47. |
