Rovafovir, formerly GS-9131, is a novel nucleotide-analogue reverse transcriptase inhibitor in clinical development. It is a phosphonoamidate prodrug of GS-9148 and has demonstrated potent antiviral activity against viruses containing major mutations associated with resistance to nucleoside-analogue reverse transcriptase inhibitors, such as mK65R, L74V and M184V. In early preclinical studies, rovafovir showed a favorable toxicity, resistance and pharmacokinetic profile including potential for once-daily dosing; low potential for mitochondrial and renal toxicity; and low potential for drug–drug interactions. A phase II functional monotherapy clinical study evaluating the short-term safety and efficacy of rovafovir when added to a failing antiretroviral regimen is currently underway.
- NRTI resistance
- Nucleotide reverse transcriptase inhibitor
ASJC Scopus subject areas
- Pharmacology (medical)