Drug intelligence / Profile preview

ritonavir + lopinavir + atazanavir + efavirenz

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

Overview

This is a non-standard, multi-drug combination of four antiretroviral agents used in the treatment of HIV-1 infection. The components are: - **Ritonavir** and **lopinavir**, which are protease inhibitors often co-formulated as lopinavir/ritonavir (LPV/r), with ritonavir acting as a pharmacokinetic booster to increase lopinavir levels. - **Atazanavir**, another protease inhibitor, typically boosted with low-dose ritonavir (atazanavir/ritonavir or ATV/r) to enhance its efficacy and pharmacokinetics. - **Efavirenz**, a non-nucleoside reverse transcriptase inhibitor (NNRTI). Each drug targets different steps in the HIV replication cycle. Protease inhibitors block the viral protease enzyme, preventing maturation of infectious virus particles. Efavirenz inhibits reverse transcriptase, blocking conversion of viral RNA into DNA. While each component is approved for use in various recommended regimens for HIV treatment—often in dual or triple combinations—there is no clinical precedent or guideline support for using all four together due to overlapping toxicities, complex drug-drug interactions (notably via CYP3A4 metabolism), and risk of suboptimal efficacy[1][3][5][6]. Some combinations among these drugs are specifically not recommended due to reduced effectiveness or increased adverse effects[5][6].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptasePR (Progesterone receptor)

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