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TAS-109

Description of TAS-109: TAS-109 is an analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Nucleoside analogue TAS-109 is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:   .Taiho Pharma Inc.

TAS-109 is a novel deoxycitidine analogue with unique mechanism of action. Brief exposure to high concentrations of TAS-109 inhibits DNA polymerase resulting in S-phase arrest, while prolonged exposure to TAS-109 at low concentration causes DNA fragmentation, G2/M phase arrest and apoptosis. TAS-109 demonstrated activity in tumor xenografts resistant to other deoxycitidine analogs. CI of TAS-109 is feasible and well tolerated with myelosuppression as main DLT. The recommended doses are 2 mg/m²/day and 3 mg/m²/day on the 14-day and 7-day CI schedules respectively. Preliminary activity was suggested. PD data demonstrate biological activity at the tested doses. see http://meeting.ascopubs.org/cgi/content/abstract/26/15_suppl/2577.

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