Tanovea® for the treatment of lymphoma in dogs

Biochemical Pharmacology
Erik De Clercq

Abstract

Tanovea® (first named GS-9219, then VDC-1101, generic name: rabacfosadine) is a pro-prodrug or "double" prodrug of PMEG [9-(2-phosphonylmethoxyethyl)guanine], which has been conditionally approved by the US FDA (Food and Drug Administration) for the treatment of lymphoma in dogs. Tanovea has been demonstrated to be effective against non-Hodgkin's lymphoma (NHL) in dogs, as well as canine cutaneous T-cell lymphoma, spontaneous canine multiple myeloma, naïve canine multicentric lymphoma and relapsed canine B-cell lymphoma. As a double prodrug of PMEG, GS-9219 is first converted intracellularly by hydrolysis to cPr-PMEDAP, then deaminated to PMEG, which is then phosphorylated twice to its active metabolite PMEGpp, acting at the level of the cellular DNA polymerases.

Citations

Jun 22, 2019·Cancer Immunology, Immunotherapy : CII·Lidia TaroneFederica Riccardo
Mar 17, 2020·Expert Opinion on Drug Discovery·Michael D Lucroy, Mark A Suckow
Mar 3, 2020·Frontiers in Oncology·David M VailRobert Jeraj
Feb 13, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Guangdi LiLi Tan
Jun 14, 2021·Journal of Comparative Pathology·Yuki MorinagaTakuya Mizuno
Apr 3, 2019·Journal of Medicinal Chemistry·Erik De Clercq

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