Drug intelligence / Profile preview

A79

Development stage
Preclinical
Lead developer
Fujian Medical University
Modality
Small Molecules
01

Overview

A79 is a novel small-molecule inhibitor of **Ribonucleotide Reductase Regulatory Subunit M2 (RRM2)**, identified through integrative bioinformatic screening and virtual modeling for the treatment of advanced prostate cancer. RRM2 is a critical enzyme in the RB1/E2F1 axis that regulates the production of deoxyribonucleotides (dNTPs) required for DNA synthesis and cell cycle progression. By binding to and inhibiting RRM2, A79 disrupts the dNTP pool, leading to DNA replication stress, S-phase cell cycle arrest, and apoptosis in prostate cancer cells. Preclinical studies have demonstrated that A79 possesses superior anti-tumor efficacy compared to traditional androgen receptor (AR) antagonists in castration-resistant prostate cancer (CRPC) models, suggesting its potential as a therapeutic agent for AR-independent advanced prostate cancer.

02

Targets

RRM2

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