Emtricitabine rilpivirine tenofovir
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Mohamed Moubarak, M.D. [2]
Overview
Emtricitabine/rilpivirine/tenofovir (trade name Complera, Eviplera) is a fixed dose combination of antiretroviral drugs for the treatment of HIV.[1] The drug was co-developed by Gilead Sciences and Johnson & Johnson's Tibotec division and was approved by the Food and Drug Administration in August 2011, and by the European Medicines Agency in November 2011 (Eviplera),[2] for patients who have not previously been treated for HIV.[3] It is available as a once-a-day single tablet.
Category
Antiretroviral
US Brand Names
COMPLERA®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
COMPLERA is a fixed-dose combination of the antiretroviral drugs emtricitabine, rilpivirine and tenofovir disoproxil fumarate.[4]
- Emtricitabine: Emtricitabine, a synthetic nucleoside analog of cytidine, is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate. Emtricitabine 5'-triphosphate inhibits the activity of the HIV-1 RT by competing with the natural substrate deoxycytidine 5'-triphosphate and by being incorporated into nascent viral DNA which results in chain termination. Emtricitabine 5′-triphosphate is a weak inhibitor of mammalian DNA polymerase α, β, ε, and mitochondrial DNA polymerase γ.
- Rilpivirine: Rilpivirine is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor of HIV-1 and inhibits HIV-1 replication by non-competitive inhibition of HIV-1 RT. Rilpivirine does not inhibit the human cellular DNA polymerases α, β, and mitochondrial DNA polymerase γ.
- Tenofovir Disoproxil Fumarate: Tenofovir DF is an acyclic nucleoside phosphonate diester analog of adenosine monophosphate. Tenofovir DF requires initial diester hydrolysis for conversion to tenofovir and subsequent phosphorylations by cellular enzymes to form tenofovir diphosphate. Tenofovir diphosphate inhibits the activity of HIV-1 RT by competing with the natural substrate deoxyadenosine 5′-triphosphate and, after incorporation into DNA, by DNA chain termination. Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases α, β, and mitochondrial DNA polymerase γ.
References
- ↑ "Approval of Complera: emtricitabine/rilpivirine/tenofovir DF fixed dose combination". Food and Drug Administration. August 10, 2011.
- ↑ "Eviplera; summary of the European public assessment report". European Medicines Agency. November 2011.
- ↑ "FDA approves Gilead-J&J HIV pill Complera". Business Week. August 10, 2011.
- ↑ "COMPLERA (EMTRICITABINE, RILPIVIRINE HYDROCHLORIDE, AND TENOFOVIR DISOPROXIL FUMARATE) TABLET, FILM COATED [GILEAD SCIENCES, INC.]". Text " accessdate" ignored (help)