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ARV-110 + abiraterone

Development stage: Unknown
Lead developer: Arvinas
Modality: PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration: Oral

Overview

ARV-110 + abiraterone is an investigational combination therapy being studied for the treatment of metastatic castration-resistant prostate cancer (mCRPC), particularly in patients who have developed resistance to abiraterone. ARV-110 (bavdegalutamide) is a PROteolysis TArgeting Chimera (PROTAC) small molecule that selectively degrades the androgen receptor (AR), including wild-type and clinically relevant mutant forms, by recruiting cereblon-containing E3 ubiquitin ligase to induce proteasomal degradation. Abiraterone is a CYP17 inhibitor that blocks androgen biosynthesis, thereby reducing androgen levels and suppressing AR signaling. The rationale for combining these agents is to overcome or delay resistance to abiraterone by directly degrading the androgen receptor with ARV-110 while continuing to suppress androgen production with abiraterone. This combination is currently being evaluated in phase 1b clinical trials for safety, tolerability, pharmacokinetics, and preliminary efficacy in mCRPC patients with PSA progression on prior abiraterone therapy[1][2][4][5].

Brand names: abiraterone (Zytiga, Yonsa)
Other names: bavdegalutamide + abiraterone

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)CRBN (Cereblon)AR (Adrenergic receptors)

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