Drug intelligence / Profile preview

abiraterone + apalutamide + enzalutamide + rezvilutamide + darolutamide

Development stage
Unknown
Lead developer
Anhui Medical University
Modality
Small Molecules
Administration
Oral
01

Overview

"Abiraterone + apalutamide + enzalutamide + rezvilutamide + darolutamide" is not a single therapeutic combination or fixed-dose product, but rather a collective grouping of five distinct androgen receptor pathway inhibitors (ARPIs). In the context of a prospective, single-center, observational study conducted by Anhui Medical University, these agents serve as the second-generation novel endocrine therapeutic options combined with androgen deprivation therapy (ADT) for patients with newly diagnosed metastatic hormone-sensitive prostate cancer (mHSPC). The study utilizes spatial multi-omics (including whole-exome sequencing, Xenium spatial transcriptomics, and PhenoCycler-Fusion spatial single-cell proteomics) to predict treatment response and delineate the molecular landscape associated with different therapeutic regimens. Each of these small molecule agents targets the androgen receptor signaling pathway, either by inhibiting androgen biosynthesis (abiraterone, a CYP17A1 inhibitor) or by acting as competitive androgen receptor antagonists (apalutamide, enzalutamide, rezvilutamide, and darolutamide).

02

Targets

AR (Adrenergic receptors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)CYP21A2 (Cytochrome P450 21-hydroxylase)GABRR (GABA-A receptor subunit rho)

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