Drug intelligence / Profile preview

fluzoparib + paclitaxel

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

Overview

Fluzoparib is a potent, orally available small molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), developed to target cancers with homologous recombination repair (HR) deficiencies, such as BRCA-mutated ovarian and breast cancers. It induces DNA double-strand breaks, G2/M cell cycle arrest, and apoptosis in HR-deficient cells. Fluzoparib has demonstrated favorable pharmacokinetics and toxicity profiles in preclinical models and sensitizes both HR-deficient and HR-proficient cells to cytotoxic drugs[1][3][5]. Paclitaxel is a microtubule-stabilizing agent from the taxane class that promotes microtubule assembly while preventing depolymerization, thereby inhibiting mitosis and inducing apoptosis in cancer cells[4][6]. The combination of fluzoparib with paclitaxel has shown improved antitumor efficacy compared to either agent alone in preclinical models without increased toxicity[5]. This combination is under clinical investigation for advanced solid tumors including ovarian cancer.

02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)

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