Drug intelligence / Profile preview

TAS-114 + capecitabine

Development stage
Phase 1
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

TAS-114 + capecitabine is an investigational oral combination therapy for cancer. TAS-114 is a dual inhibitor of deoxyuridine triphosphatase (dUTPase) and dihydropyrimidine dehydrogenase (DPD), designed to enhance the antitumor activity of 5-fluorouracil (5-FU)-based chemotherapy agents such as capecitabine. By inhibiting DPD, TAS-114 prevents the rapid catabolism of 5-FU, increasing its systemic availability and efficacy. As a dUTPase inhibitor, it promotes misincorporation of FdUTP and dUTP into DNA in tumor cells, leading to DNA damage and cell death. Capecitabine is an oral prodrug that is converted to 5-FU in the body; when combined with TAS-114, preclinical studies have shown enhanced antitumor effects compared to either agent alone[2][3][4][5][6]. This combination has been evaluated primarily for solid tumors such as advanced or metastatic cancers.

02

Targets

dUTPase (Deoxyuridine triphosphatase)DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)

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