Drug intelligence / Profile preview

gemcitabine + cedazuridine

Development stage
Preclinical
Lead developer
Helix BioPharma
Modality
Small Molecules
Administration
Oral
01

Overview

**Gemcitabine + cedazuridine** is an investigational oral combination of the nucleoside metabolic antagonist gemcitabine and cedazuridine, a cytidine deaminase (CDA) inhibitor. Cedazuridine inhibits CDA-mediated deamination of gemcitabine in the gastrointestinal tract and liver, boosting its oral bioavailability to approximately 90%, comparable to intravenous administration, enabling flexible dosing schedules like maintenance or metronomic therapy for solid tumors. Developed by Helix Biopharma as GEMCEDA, a first-in-class oral prodrug of gemcitabine, it leverages gemcitabine's mechanism of incorporating into DNA as difluorodeoxycytidine triphosphate (dFdCTP) to chain-terminate synthesis and inhibit ribonucleotide reductase, inducing apoptosis in rapidly dividing cancer cells.[3][4][7]

Brand names
GEMCEDA
Other names
Gemcitabine prodrug/Cedazuridine
02

Targets

DNARRM1CDA (Cytidine deaminase)RRM2

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