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Darunavir is an oral nonpeptidic HIV-1 protease inhibitor PI that is used, together with a low boosting dose of ritonavir, as part of an antiretroviral therapy ART regimen in treatment-experienced and -naive patients with HIV-1 infection. In clinical trials in treatment-experienced patients with HIV-1 infection receiving an optimized background regimen OBR, twice-daily boosted darunavir was more effective than investigator-selected ritonavir-boosted control PIs CPIs or ritonavir-boosted lopinavir.
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Pharmacokinetic enhancement involves the use of one drug to inhibit the metabolism of another, leading to improved drug exposure. Ritonavir increases exposure and slows the metabolism of other protease inhibitors leading to potential for using fewer tablets and having less frequent dosing. It also removes the need for food restrictions and at least with saquinavir the need to separate dosing from buffered ddI. Furthermore, the interpatient variability in exposure with PIs is diminished when ritonavir co-dosing is used. Ritonavir is also known to inhibit p-glycoprotein, a cellular efflux pump.
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