Drug intelligence / Profile preview

tenofovir + lamivudine + emtricitabine + lopinavir + ritonavir + raltegravir

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

This is a non-standard, multi-drug antiretroviral combination regimen composed of six agents commonly used in the treatment and prevention of HIV-1 infection. The drugs included are: - Tenofovir (a nucleotide reverse transcriptase inhibitor, NRTI) - Lamivudine (a nucleoside reverse transcriptase inhibitor, NRTI) - Emtricitabine (a nucleoside reverse transcriptase inhibitor, NRTI) - Lopinavir (an HIV protease inhibitor) - Ritonavir (an HIV protease inhibitor and pharmacokinetic booster for other PIs such as lopinavir) - Raltegravir (an integrase strand transfer inhibitor) Each drug targets a different stage of the HIV replication cycle. Tenofovir, lamivudine, and emtricitabine inhibit viral reverse transcriptase; lopinavir and ritonavir inhibit viral protease; raltegravir inhibits viral integrase. This combination would be expected to have potent antiretroviral activity but is not a standard fixed-dose or co-formulated product. Such regimens may be considered in salvage therapy or post-exposure prophylaxis when resistance or intolerance to standard regimens exists[2][5][6].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseIntegrase allosteric pocket (HIV)PR (Progesterone receptor)

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