Drug intelligence / Profile preview

ethynylcytidine

Development stage
Phase 2
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Intravenous
01

Overview

TAS-106 (ethynylcytidine) is a synthetic nucleoside antimetabolite and cytidine analog developed as an investigational anticancer agent. It acts primarily by inhibiting RNA synthesis through competitive inhibition of RNA polymerases I, II, and III after intracellular conversion to its active triphosphate form (ECTP). This leads to suppression of RNA synthesis, activation of RNase L, and induction of apoptosis in tumor cells. TAS-106 has demonstrated potent antitumor activity in preclinical models with limited toxicity. It was investigated for intravenous administration in solid tumors, including head and neck cancer[1][2][3][4][5][6].

Other names
3'-C-ethynylcytidineethynylcytidine
02

Targets

Pol III (Dna-directed RNA polymerase III)Pol I (RNA polymerase I)Pol II (RNA polymerase II elongation factors)

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