Drug intelligence / Profile preview

apatinib + fluzoparib

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

Overview

Apatinib + fluzoparib is an investigational oral combination therapy consisting of two small molecule drugs with complementary mechanisms of action. Apatinib is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), functioning as an anti-angiogenic agent, while fluzoparib (also known as fuzuloparib) is a poly(ADP-ribose) polymerase (PARP) inhibitor that impairs DNA repair in tumor cells. The combination has been studied primarily for the treatment of advanced ovarian cancer and triple-negative breast cancer, where it has demonstrated synergistic antitumor activity by inhibiting tumor angiogenesis and enhancing DNA damage in cancer cells. Preclinical studies show that the combination downregulates MEK signaling and homologous recombination pathway proteins such as RAD51 and BRCA1, leading to increased DNA damage marker γH2AX expression[1][2][3]. Clinical trials have established recommended phase 2 dosing and shown promising efficacy with acceptable safety profiles[2][3].

Brand names
Rivoceranib (for apatinib)
Other names
apatinib plus fluzoparibfluzoparib plus apatinib
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)PARP2 (Poly (adp-ribose) polymerase 2)

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