Drug intelligence / Profile preview

fuzuloparib + abiraterone acetate + prednisolone

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

Overview

fuzuloparib + abiraterone acetate + prednisolone is a combination regimen consisting of the poly(ADP-ribose) polymerase (PARP) inhibitor fuzuloparib, the CYP17A1 inhibitor abiraterone acetate, and the corticosteroid prednisolone (or prednisone). Developed by Hengrui Pharma, this combination is primarily investigated as a first-line treatment for patients with metastatic castration-resistant prostate cancer (mCRPC). Fuzuloparib inhibits PARP1 and PARP2, disrupting DNA single-strand break repair and inducing synthetic lethality in cancer cells with homologous recombination repair (HRR) or DNA damage repair (DDR) deficiencies. Abiraterone acetate blocks androgen biosynthesis by selectively inhibiting the CYP17A1 enzyme, thereby reducing testosterone levels that drive prostate cancer growth. Prednisolone is co-administered to prevent mineralocorticoid excess caused by CYP17A1 inhibition. The combination of a PARP inhibitor and an androgen receptor signaling inhibitor (ARSI) provides a synergistic therapeutic effect by simultaneously targeting the androgen receptor pathway and DNA repair mechanisms.

Other names
fuzuloparib + abiraterone + prednisolonefuzuloparib + abiraterone + prednisonefuzuloparib + abiraterone acetate + prednisonefuzuloparib plus abiraterone acetate and prednisolonefuzuloparib plus abiraterone acetate and prednisone
02

Targets

AR (Adrenergic receptors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)

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