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Ritonavir is an HIV protease inhibitor. It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-1_3B-induced cell death in MT-4 human T cell leukemia cells (EC₅₀ = 25 nM) as well as cell death induced by HIV-1_LAI, HIV-2_ROD, and HIV-2_EHO in human MT-2 cells (IC₅₀s = 0.045, 0.13, and 0.24 μM, respectively).Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC₅₀ = 0.14 μM).It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir , indinavir, nelfinavir, and amprenavir in rat and human liver microsomes in a concentration-dependent manner.Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.

Ritonavir was originally developed as an inhibitor of HIV protease inhibitor (PI). Ritonavir is currently exclusively used as a pharmacokinetic enhancer (booster) of other protease inhibitors, due to ritonavir's potent inhibition of the cytochrome P 450 3A4 (CYP3A4), an enzyme that is responsible for metabolizing most HIV PIs.

Norvir was launched in Germany, the UK and US for treatment of advanced HIV in combination with antiretroviral nucleoside analogs in a record 72 days by the FDA. It is an inhibitor of HIV aspartic protease which is critical in the processing of a propeptide into the gag, gag-pol gene products and the protease itself. This inhibition results in the release of non-infectous immature virus particles. It is greater than 500-fold more selective for viral aspartic protease than the human version, has good oral bioavailability and may increase the bioavailability of other protease inhibitors. Ritonavir was able to increase the CD4 and CD8 lymphocyte count as well as reduce viral RNA. It is more potent than saqunavir and comparible in potency to zidovudine and lamivudine.