Drug intelligence / Profile preview

lamivudine + tenofovir disoproxil fumarate + lopinavir + ritonavir

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

Overview

The drug combination "lamivudine + tenofovir disoproxil fumarate + lopinavir + ritonavir" is a four-drug antiretroviral regimen used in the treatment of HIV infection. This combination brings together nucleoside reverse transcriptase inhibitors (lamivudine and tenofovir disoproxil fumarate) with a protease inhibitor (lopinavir) boosted by a pharmacokinetic enhancer (ritonavir). ## Mechanism of Action This combination works through multiple mechanisms to suppress HIV replication: - **Lamivudine (3TC)** is a nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV reverse transcriptase, preventing viral DNA synthesis. - **Tenofovir disoproxil fumarate (TDF)** is also an NRTI that blocks reverse transcriptase activity through a similar mechanism. - **Lopinavir** is a protease inhibitor that prevents the cleavage of viral polyproteins, inhibiting the formation of mature viral particles. - **Ritonavir** primarily serves as a pharmacokinetic enhancer (booster) that inhibits the metabolism of lopinavir, increasing its plasma concentration and efficacy. ## Clinical Evidence Research has shown that dual therapy with lopinavir-ritonavir plus lamivudine has non-inferior therapeutic efficacy compared to triple therapy regimens for maintenance of HIV viral suppression. While the specific four-drug combination isn't explicitly mentioned in the search results as a fixed-dose combination product, the components are used together in various HIV treatment regimens. The FDA has listed "Abacavir+lamivudine+lopinavir+ritonavir" as a four-drug combination needed for pediatric formulations under PEPFAR (President's Emergency Plan for AIDS Relief), indicating the importance of similar multi-drug combinations in HIV treatment. ## Available Formulations The individual components are available as separate medications or as part of other fixed-dose combinations: - Lamivudine and tenofovir disoproxil fumarate are available as a dual combination under brand names Cimduo and Temixys. - Lopinavir and ritonavir are available as a fixed-dose combination under the brand name Kaletra. This four-drug regimen represents a comprehensive approach to HIV treatment, targeting multiple stages of the viral life cycle to effectively suppress viral replication and maintain immune function in people living with HIV.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptasePR (Progesterone receptor)

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