Drug intelligence / Profile preview

lopinavir + ritonavir + saquinavir

Development stage
Unknown
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **triple combination** of the HIV-1 protease inhibitors **lopinavir**, **ritonavir**, and **saquinavir** used in the treatment of HIV infection, primarily in patients with previous antiretroviral treatment experience. The regimen leverages the pharmacokinetic boosting effect of ritonavir, which is a potent inhibitor of the cytochrome P450 3A4 enzyme (CYP3A4) and P-glycoprotein drug transporter, thereby increasing plasma concentrations of both lopinavir and saquinavir to enhance virologic suppression and reduce the likelihood of resistance. Lopinavir and saquinavir act as competitive inhibitors of the HIV-1 protease enzyme, crucial for the maturation of infectious viral particles. Ritonavir is included at subtherapeutic doses as a pharmacokinetic enhancer. The combination has shown efficacy in virologic suppression and CD4 count improvement, especially in children and adults with prior antiretroviral therapy failure[1][5].

Other names
lopinavir/r + saquinavirLPV/r + SQVdouble-boosted protease inhibitor regimen (lopinavir/ritonavir plus saquinavir)
02

Targets

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

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