Drug intelligence / Profile preview

lopinavir + ritonavir (Abbott Laboratories)

Development stage
Phase 4
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

Lopinavir + ritonavir + ritonavir, commonly referred to as super-boosted lopinavir/ritonavir (LPV/r), is an antiretroviral combination regimen consisting of the HIV-1 protease inhibitors lopinavir and ritonavir. While the standard co-formulation (marketed as Kaletra or Aluvia) typically utilizes a 4:1 ratio of lopinavir to ritonavir, the super-boosted regimen adds an additional dose of ritonavir to achieve a 1:1 ratio (400 mg lopinavir / 400 mg ritonavir). This specific dosing strategy was developed to manage HIV-1 infection in patients co-infected with tuberculosis who are receiving rifampin-based therapy. Rifampin is a potent inducer of the Cytochrome P450 3A4 (CYP3A4) enzyme, which significantly accelerates the metabolism of lopinavir; the extra ritonavir acts as a pharmacokinetic booster by inhibiting CYP3A4 to maintain therapeutic lopinavir concentrations. The regimen was primarily studied by the University of Miami, though clinical trials were terminated due to a lack of funding.

Brand names
KaletraAluviaNorvir
Other names
super-boosted lopinavir/ritonavirsuper-boosted LPV/rlopinavir + ritonavir + ritonavirLPV/r 400/400
02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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