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rovafovir etalafenamide
- Development stage
- Phase 1
- 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
Rovafovir etalafenamide is an investigational small molecule drug developed by Gilead Sciences for the treatment of HIV-1 infection. It is a nucleotide reverse transcriptase inhibitor (NRTI) and functions as a prodrug of GS-9148. Rovafovir etalafenamide itself has no antiviral activity; after administration, it undergoes hydrolysis to release the active antiviral compound GS-9148. The drug was designed to retain activity against HIV strains with major mutations conferring resistance to other nucleoside analog reverse transcriptase inhibitors commonly used in antiretroviral therapy[1][2][4]. Clinical development included trials in treatment-experienced adults with HIV, but further development was suspended after phase II due to insufficient antiviral response[4].
- Other names
- rovafovir etalafenamide [USAN]U8S0IC8DY7U-8S0IC8DY7U 8S0IC8DY7UNII-U8S0IC8DY7UNII-U-8S0IC8DY7UNII-U 8S0IC8DY7
02
Targets
Human immunodeficiency virus type 1 reverse transcriptase
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