Drug intelligence / Profile preview

fluzoparib + chidamide

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Fluzoparib + chidamide is an investigational combination therapy consisting of two small molecule drugs with distinct mechanisms of action, being studied primarily for the treatment of advanced breast cancer, particularly HER2-negative and triple-negative subtypes. Fluzoparib is a poly (ADP-ribose) polymerase (PARP) inhibitor that impairs DNA repair in tumor cells with homologous recombination deficiency, leading to cell death. Chidamide is a selective histone deacetylase (HDAC) inhibitor that modulates gene expression through epigenetic mechanisms and can enhance immune response and reverse drug resistance. Preclinical studies indicate that this combination may overcome resistance to PARP inhibitors by downregulating DNA repair proteins such as RAD51 and MRE11, inducing cell cycle arrest at G2/M phase, and promoting apoptosis in resistant cancer cells. The combination has shown promising antitumor activity in vitro and in vivo models[7]. Clinical trials are ongoing for HRD-positive HER2-negative advanced breast cancer[1][3][5].

02

Targets

HDAC11 (Histone Deacetylase 11)HDAC10 (Histone Deacetylase 10)HDAC1 (Histone Deacetylase 1)PARP2 (Poly (adp-ribose) polymerase 2)26S proteasome

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