Drug intelligence / Profile preview

tenofovir + abacavir

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tenofovir + abacavir is a two-drug antiretroviral combination consisting of tenofovir (a nucleotide reverse transcriptase inhibitor, NRTI) and abacavir (a nucleoside reverse transcriptase inhibitor, NRTI). Both drugs act by inhibiting the HIV-1 reverse transcriptase enzyme, thereby blocking viral replication. Tenofovir is a prodrug that, once activated intracellularly to its diphosphate form, competes with deoxyadenosine 5'-triphosphate and causes chain termination during viral DNA synthesis[6]. Abacavir is converted to carbovir triphosphate inside cells; it acts as a guanosine analogue that inhibits HIV-1 reverse transcriptase by competing with dGTP and causing premature DNA chain termination[8][10]. This combination has been studied in clinical practice but is not widely used as a fixed-dose product due to concerns about efficacy compared to other regimens. It may be considered in select situations or when other options are unsuitable[9].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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