Drug intelligence / Profile preview

ARX517 + abiraterone acetate + prednisone

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

ARX517 + abiraterone acetate + prednisone is an investigational multi-drug regimen being explored for the treatment of **metastatic castration-resistant prostate cancer (mCRPC)**. The regimen combines: - **ARX517**, an antibody-drug conjugate (ADC) targeting prostate-specific membrane antigen (PSMA), delivering a microtubule inhibitor payload specifically to PSMA-expressing tumor cells, causing cytotoxicity and apoptosis. ARX517 uses a noncleavable linker for stability and selective delivery[2][8]. - **Abiraterone acetate**, a prodrug of abiraterone, inhibits CYP17A1, blocking androgen biosynthesis and reducing testosterone and cortisol, while also inducing mineralocorticoid excess[1][7]. - **Prednisone**, a glucocorticoid, compensates for abiraterone-induced cortisol reduction and helps manage mineralocorticoid-related adverse events[1]. The combination intends to leverage ARX517’s cytotoxic specificity alongside hormonal blockade from abiraterone acetate and supportive corticosteroid therapy with prednisone.

Other names
abiraterone acetate + prednisoneARX517 + abiraterone acetate + prednisone
02

Targets

GR (Glucocorticoid receptor)AR (Adrenergic receptors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)TUBB (Tubulin (alpha and beta subunits))

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