Rovafovir etalafenamide (development code GS-9131) is an experimental drug for the treatment of
HIV-1 infection.[1] Rovafovir etalafenamide is a
nucleotide reverse transcriptase inhibitor and
prodrug of GS-9148. Rovafovir etalafenamide itself has no antiviral activity, but once consumed it is metabolized through the
hydrolysis of the phosphonoamidate group to generate the antiviral compound GS-9148.[1]
Chemical strucuture of GS-9148, the active antiviral agent
^Standley EA, Bringley DA, Calimsiz S, Ng JD, Sarma K, Shen J, et al. (2021). "Synthesis of Rovafovir Etalafenamide (Part I): Active Pharmaceutical Ingredient Process Development, Scale-Up, and Impurity Control Strategy". Organic Process Research & Development. 25 (5): 1215–1236.
doi:
10.1021/acs.oprd.1c00059.
S2CID236571091.
^Bringley DA, Roberts BJ, Calimsiz S, Brown BH, Davy JA, Kwong B, et al. (2021). "Synthesis of Rovafovir Etalafenamide (Part II): Dynamic Control for Successful Scale-Up of an Oxygen-Releasing Elimination Reaction Mediated by Oxone". Organic Process Research & Development. 25 (5): 1237–1246.
doi:
10.1021/acs.oprd.0c00439.
S2CID234838465.
^Ambrosi A, Bringley DA, Calimsiz S, Garber JA, Huynh H, Mohan S, et al. (2021). "Synthesis of Rovafovir Etalafenamide (Part III): Evolution of the Synthetic Process to the Phosphonamidate Fragment". Organic Process Research & Development. 25 (5): 1247–1262.
doi:
10.1021/acs.oprd.0c00428.
S2CID235569360.