Drug intelligence / Profile preview

emtricitabine + tenofovir disoproxil fumarate + third agent

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

Overview

This is a **combination regimen** consisting of two nucleoside/nucleotide reverse transcriptase inhibitors (**NRTIs**): emtricitabine and tenofovir disoproxil fumarate, paired with a third agent (frequently a non-nucleoside reverse transcriptase inhibitor, integrase inhibitor, or protease inhibitor). - **Emtricitabine** is a synthetic nucleoside analog of cytidine; it inhibits HIV-1 reverse transcriptase, terminating viral DNA chain elongation[1][4]. - **Tenofovir disoproxil fumarate** is a prodrug of tenofovir (an acyclic nucleotide analog of adenosine monophosphate), which also inhibits HIV-1 reverse transcriptase through DNA chain termination upon incorporation into viral DNA[1][4]. - The **third agent** serves as a complementary antiviral mechanism (such as integrase inhibition, protease inhibition, or further reverse transcriptase inhibition). This regimen forms the foundation of highly active antiretroviral therapy (**HAART**) for HIV-1 infection and is also used for **pre-exposure prophylaxis (PrEP)** when the third agent is omitted or present as part of combined therapy[2][3][4]. This regimen is not curative, but it suppresses viral replication, preserves immune function, and reduces transmission risk.

Other names
emtricitabine plus tenofovir disoproxil fumarate plus third agent
02

Targets

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

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