Drug intelligence / Profile preview

fluzoparib + abiraterone

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

Overview

fluzoparib + abiraterone is a combination therapy primarily investigated for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Fluzoparib is a potent, orally active small-molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2, which induces synthetic lethality in cells with deficient DNA repair mechanisms, such as those with BRCA1/2 mutations. Abiraterone, typically administered as abiraterone acetate, is a selective inhibitor of the enzyme cytochrome P450 17A1 (CYP17A1), which is essential for androgen biosynthesis in the testes, adrenal glands, and prostate tumor tissue. By combining these two agents, the regimen aims to simultaneously inhibit the androgen receptor signaling pathway and the DNA damage response, potentially overcoming resistance mechanisms in advanced prostate cancer. This combination is often administered alongside prednisone to manage mineralocorticoid-related side effects associated with abiraterone.

Other names
fluzoparib and abirateronefluzoparib plus abirateronefluzoparib + abiraterone acetate
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)

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