Drug intelligence / Profile preview

nevirapine + saquinavir

Development stage
Discontinued
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**Nevirapine + saquinavir** is a combination of two antiretroviral drugs used in the management of HIV-1 infection. Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds directly to reverse transcriptase, blocking RNA-dependent and DNA-dependent DNA polymerase activity and inhibiting viral replication. Saquinavir is an HIV-1 protease inhibitor that blocks the protease enzyme, preventing the cleavage of viral polyprotein precursors and resulting in the production of immature, non-infectious viral particles. This combination has been investigated in salvage regimens for patients with treatment failure to other protease inhibitors. Clinical use of nevirapine with saquinavir is complicated by pharmacokinetic interactions; nevirapine induces CYP3A4-mediated metabolism, leading to significantly reduced saquinavir plasma concentrations. This interaction reduces virologic efficacy and presents safety concerns, so this combination is generally **not recommended** outside special circumstances and not established as a standard or approved regimen. When used, it is most frequently as part of multi-agent rescue therapies (e.g., with other drugs like stavudine and nelfinavir for advanced disease or multi-drug resistance)[1][3].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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