Tanovea® for the treatment of lymphoma in dogs

Biochem Pharmacol. 2018 Aug:154:265-269. doi: 10.1016/j.bcp.2018.05.010. Epub 2018 May 17.

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.

Publication types

  • Review

MeSH terms

  • Alanine / analogs & derivatives*
  • Alanine / chemistry
  • Alanine / metabolism
  • Alanine / therapeutic use
  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use*
  • Dogs
  • Lymphoma / diagnostic imaging
  • Lymphoma / drug therapy*
  • Lymphoma / metabolism
  • Prodrugs / chemistry
  • Prodrugs / metabolism
  • Prodrugs / therapeutic use*
  • Purines / chemistry
  • Purines / metabolism
  • Purines / therapeutic use*
  • Treatment Outcome

Substances

  • Antineoplastic Agents
  • Prodrugs
  • Purines
  • rabacfosadine
  • Alanine