Abstract
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.
Original language | English (US) |
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Pages (from-to) | 459-469 |
Number of pages | 11 |
Journal | Drugs of the Future |
Volume | 45 |
Issue number | 7 |
DOIs | |
State | Published - Jul 2020 |
Keywords
- GS-9131
- HIV-1
- NRTI resistance
- Nucleotide reverse transcriptase inhibitor
- Rovafovir
ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)