Drug intelligence / Profile preview

saquinavir + ritonavir + stavudine

Development stage
Phase 3
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

A fixed-dose combination of **saquinavir**, **ritonavir**, and **stavudine** used as part of combination antiretroviral therapy (ART) for the treatment of HIV-1 infection. - **Saquinavir** and **ritonavir** are HIV-1 protease inhibitors: ritonavir is primarily used here as a pharmacokinetic enhancer (by inhibiting CYP3A and P-glycoprotein) to increase saquinavir plasma concentrations and optimize its antiviral efficacy[1][2][4]. - **Stavudine** is a nucleoside reverse transcriptase inhibitor (NRTI) that impairs HIV replication by causing premature chain termination during reverse transcription. - This combination is intended for moderately to severely immunosuppressed, protease inhibitor-naive individuals with HIV-1 infection as part of a highly active antiretroviral therapy (HAART) regimen[3]. - Ritonavir substantially boosts saquinavir concentrations, allowing for more effective viral suppression and reduced variability between patients[1]. - This regimen is used in accordance with clinical guidelines for advanced HIV-1 infection, though individual component dosages may require adjustment based on pharmacokinetics and tolerability[1][3][4].

02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)Human immunodeficiency virus type 1 reverse transcriptase

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