Drug intelligence / Profile preview

4'-ethynyl-2'-deoxycytidine

Development stage
Preclinical
Lead developer
Thomas Jefferson University
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

4'-Ethynyl-2'-deoxycytidine (EdC) is a preclinical, small-molecule nucleoside analog and prodrug being investigated for the treatment of hematologic malignancies, specifically diffuse large B-cell lymphoma (DLBCL) and acute lymphoblastic leukemia (ALL). EdC requires intracellular phosphorylation by deoxycytidine kinase (DCK) to its active triphosphate form, which then acts as a DNA chain terminator, inducing replication fork arrest, replicative stress, and S-phase cell cycle accumulation. EdC is designed to resist cytidine deamination and SAMHD1-mediated degradation, overcoming common nucleoside analog resistance mechanisms. It has demonstrated high potency and in vivo efficacy against DLBCL and ALL models.

Other names
2'-deoxy-4'-C-ethynylcytidine2'-deoxy-4'-ethynylcytidine4'-C-ethynyl-2'-deoxycytidine4′-ethynyl-2′-deoxycytidineEdC
02

Targets

DNADCK (Deoxycytidine kinase)

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