Drug intelligence / Profile preview

fosamprenavir + lopinavir + ritonavir

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Fosamprenavir, lopinavir, and ritonavir are antiretroviral drugs used in combination for the treatment of human immunodeficiency virus (HIV) infection. All three agents are protease inhibitors. Fosamprenavir is a prodrug of amprenavir and inhibits HIV-1 protease, preventing viral polyprotein cleavage and resulting in immature, noninfectious viral particles[1][5]. Lopinavir is a potent inhibitor of HIV-1 protease; its antiviral activity prevents maturation of the virus by blocking the production of mature infectious virions[6]. Ritonavir acts primarily as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A-mediated metabolism, thereby increasing plasma concentrations of other protease inhibitors such as lopinavir and fosamprenavir[2][6]. The combination may be considered in treatment-experienced patients but can result in significant drug-drug interactions that reduce exposure to both amprenavir (the active form of fosamprenavir) and lopinavir[8].

02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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