Drug intelligence / Profile preview

apatinib + letrozole + fluzoparib

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

Overview

apatinib + letrozole + fluzoparib is a combination therapy being investigated for the treatment of estrogen receptor (ER)-positive, platinum-sensitive recurrent ovarian cancer. The regimen consists of fluzoparib, a poly (ADP-ribose) polymerase (PARP) inhibitor; apatinib, a selective tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor-2 (VEGFR-2); and letrozole, a third-generation aromatase inhibitor. This triple-combination approach, studied in clinical trials led by Peking Union Medical College Hospital, aims to provide a maintenance therapy option for patients who have progressed after initial PARP inhibitor treatment by simultaneously inhibiting DNA repair, angiogenesis, and estrogen-driven tumor growth. The combination is designed to overcome resistance mechanisms that often emerge during single-agent PARP inhibitor maintenance.

Other names
Apatinib plus letrozole plus fluzoparibApatinib, letrozole, and fluzoparib combinationfuzuloparib + apatinib + letrozole
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)PARP2 (Poly (adp-ribose) polymerase 2)CYP19A1 (Aromatase)

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