rabacfosadine

Rabacfosadine is a guanine nucleotide analog and acyclic nucleotide phosphonate prodrug used for the treatment of lymphoma in dogs. It is marketed under the brand name Tanovea. Developed originally by Gilead Sciences as GS‑9219, rabacfosadine acts as a double prodrug that is hydrolyzed intracellularly to cPrPMEDAP and then deaminated to PMEG, which is subsequently phosphorylated to its active form, PMEG diphosphate (PMEGpp). The active metabolite PMEGpp functions as a potent chain‑terminating inhibitor of major nuclear DNA polymerases, leading to inhibition of DNA synthesis, S phase cell cycle arrest, and induction of apoptosis in lymphoid cells. Rabacfosadine preferentially targets lymphoma cells with reduced systemic toxicity compared with its parent compound PMEG. It was granted conditional FDA approval for canine lymphoma in December 2016 and received full approval in July 2021[1][2][3][5][6][7].

Brand names

TanoveaTanovea-CA1Tanovea-CA-1Tanovea-CA 1

Other names

859209-74-8