Raltegravir (MK-0518): a novel integrase inhibitor for the treatment of HIV infection.
Expert Opin Investig Drugs
; 17(1): 97-103, 2008 Jan.
Article
em En
| MEDLINE
| ID: mdl-18095922
ABSTRACT
Integrase is essential for HIV-1 replication; however, potent inhibition of the isolated enzyme in biochemical assays has not readily translated into antiviral activity in a manner consistent with inhibition of integration. Raltegravir is a novel HIV-1 integrase strand transfer inhibitor with potent in vitro activity against wild-type and multi-class resistant HIV-1 virus (in vitro IC(95) for HIV-1 in 50% normal human serum = 33 nM). Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking the ability of HIV to replicate. Raltegravir is administered orally every 12 h and does not require boosting with low-dose ritonavir (RTV) to achieve therapeutic concentrations. Raltegravir is not a potent inhibitor or inducer of cytochrome P450 3A4, and it is predominantly metabolized by glucuronidation, specifically by the enzyme UDP-glucuronosyltransferase 1A1.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Orgânicos
/
Infecções por HIV
/
HIV-1
/
Inibidores de Integrase de HIV
Limite:
Humans
Idioma:
En
Revista:
Expert Opin Investig Drugs
Assunto da revista:
TERAPIA POR MEDICAMENTOS
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Estados Unidos