Drug intelligence / Profile preview

capravirine + lopinavir + ritonavir + nucleoside reverse transcriptase inhibitors

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a combination antiretroviral regimen composed of **capravirine (a non-nucleoside reverse transcriptase inhibitor)**, **lopinavir** and **ritonavir (both protease inhibitors)**, and **nucleoside reverse transcriptase inhibitors (NRTIs)**. The combination is designed for the treatment of **HIV-1 infection**, using multiple complementary mechanisms: - Capravirine inhibits the HIV reverse transcriptase through non-nucleoside binding, blocking the transcription of viral RNA into DNA. - Lopinavir inhibits the HIV protease, preventing cleavage of viral polyproteins, thus blocking viral maturation; ritonavir boosts lopinavir’s blood levels by inhibiting CYP3A4. - NRTIs serve as faulty building blocks for viral DNA, halting its synthesis. Such combinations are standard in highly active antiretroviral therapy (HAART) to enhance efficacy and reduce the risk of resistance[1][2][3][4][6][7][8].

Brand names
Kaletra (for lopinavir/ritonavir)
Other names
LPV/r (for lopinavir/ritonavir)
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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