Drug intelligence / Profile preview

LY-2334737

Development stage
Phase 1
Lead developer
Eli Lilly
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

LY-2334737 is an orally available amide prodrug of gemcitabine designed to improve the delivery and efficacy of gemcitabine in cancer treatment. It is a valproic acid ester of gemcitabine that allows for oral administration and slow systemic release of active gemcitabine over time. As a nucleoside analog antimetabolite, it exerts antitumor effects by interfering with DNA synthesis in rapidly dividing cells. The drug has demonstrated both anticancer and antiviral activity in preclinical studies. Developed primarily for the treatment of solid tumors—including metastatic and malignant solid tumors—LY‑2334737 was investigated as monotherapy and in combination with other agents such as erlotinib or capecitabine[1][3][6][8].

Other names
gemcitabine prodrug LY2334737N-{1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxo-1,2-dihydropyrimidin-4-yl}-2-propylpentanamide
02

Targets

DNARNR (Ribonucleotide reductase)

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