1. Academic Validation
  2. Tanovea® for the treatment of lymphoma in dogs

Tanovea® for the treatment of lymphoma in dogs

  • Biochem Pharmacol. 2018 Aug:154:265-269. doi: 10.1016/j.bcp.2018.05.010.
Erik De Clercq 1
Affiliations

Affiliation

  • 1 KU Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Herestraat 49, 3000 Leuven, Belgium. Electronic address: [email protected].
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.

Keywords

Dogs; Lymphoma; PMEG; Tanovea; cPr-PMEDAP.

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