Drug intelligence / Profile preview

rilpivirine + tenofovir disoproxil fumarate + lamivudine

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **fixed-dose combination** antiretroviral medication that combines three active agents: **rilpivirine**, **tenofovir disoproxil fumarate**, and **lamivudine**. Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI), while tenofovir disoproxil fumarate and lamivudine are nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs). The combination is designed for the **treatment of HIV-1 infection**. Each component targets reverse transcriptase, an enzyme critical for the replication of HIV, but binds at different sites—rilpivirine non-competitively at the NNRTI pocket; tenofovir and lamivudine are incorporated as nucleotide/nucleoside analogs, causing chain termination during viral DNA synthesis. Tenofovir disoproxil fumarate is a prodrug of tenofovir. This combination offers broad suppression of HIV, reduces pill burden, and is intended for once-daily oral administration in therapy-naïve or experienced individuals, typically as part of **combination antiretroviral therapy (ART)**. Lamivudine is interchangeable in function with emtricitabine in some regimens, but there is no major brand-name single-tablet product of these three together approved globally as of yet; closely related combinations (such as rilpivirine + tenofovir + emtricitabine, branded as Complera or Eviplera, and combinations with lamivudine plus tenofovir and other agents) are approved and marketed[1][2][3][5][6].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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