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Emtricitabine ProTide

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intramuscular, Subcutaneous
01

Overview

Emtricitabine ProTide refers to a prodrug form of emtricitabine (FTC), a nucleoside reverse transcriptase inhibitor (NRTI) used primarily for the treatment and prevention of HIV-1 infection and also active against hepatitis B virus (HBV)[1][2][4]. The ProTide technology is a chemical modification that masks the phosphate group of nucleos(t)ide analogues with an aromatic group and an amino acid ester moiety, enabling efficient intracellular delivery by bypassing membrane transporters[5][7][8]. Once inside cells, enzymatic cleavage releases the active monophosphate form, which is further phosphorylated to the triphosphate that inhibits HIV reverse transcriptase[6][7]. Emtricitabine ProTides such as M2FTC and its nanoformulation NM2FTC have been developed to provide long-acting antiretroviral activity. These formulations show significantly increased cellular uptake and prolonged drug release compared to native FTC, offering potential for less frequent dosing in HIV therapy[2].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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