Drug intelligence / Profile preview

raltegravir + lopinavir + ritonavir

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

Overview

raltegravir + lopinavir + ritonavir refers to a combination of antiretroviral medications used in the treatment of HIV-1 infection, specifically involving the integrase strand transfer inhibitor raltegravir and the protease inhibitor combination lopinavir/ritonavir. Raltegravir (Isentress) works by inhibiting the HIV-1 integrase enzyme, which is essential for integrating the viral DNA into the host cell genome. Lopinavir is a protease inhibitor that prevents the processing of viral polyproteins into functional proteins, while ritonavir acts as a pharmacokinetic enhancer by inhibiting the Cytochrome P450 3A4 (CYP3A4) enzyme, thereby increasing the systemic exposure of lopinavir. This specific combination was investigated by the St Stephen's AIDS Trust in a clinical study (NCT00683670) to compare the metabolic effects, such as insulin sensitivity and lipid profiles, of raltegravir-based versus lopinavir/ritonavir-based regimens in healthy volunteers. The study demonstrated that lopinavir/ritonavir significantly reduced insulin sensitivity compared to raltegravir.

Brand names
KaletraNorvir
Other names
raltegravir + lopinavir + ritonavir-St Stephens Aids Trust-HIV infectionraltegravir + lopinavir/ritonavir
02

Targets

CYP3A4 (Cytochrome P450 3A4)Integrase allosteric pocket (HIV)PR (Progesterone receptor)

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