Drug intelligence / Profile preview

zenocutuzumab + abiraterone

Development stage
Unknown
Lead developer
Merus
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous (zenocutuzumab), Oral (abiraterone)
01

Overview

This is an investigational combination regimen consisting of **zenocutuzumab** and **abiraterone**. Zenocutuzumab is a bispecific monoclonal antibody that targets **HER2** and **HER3**, disrupting oncogenic signaling mediated by neuregulin 1 (NRG1) gene fusions. It blocks HER2/HER3 dimerization, thereby inhibiting the PI3K/AKT/mTOR pathway, which is critical for cancer cell growth and survival; it also enlists immune effector functions (ADCC). Abiraterone is a small molecule inhibitor of **CYP17A1**, reducing androgen synthesis and thereby suppressing androgen receptor signaling, a key driver in prostate cancer. The combination is currently under investigation for **metastatic castration-resistant prostate cancer (mCRPC)**, with abiraterone acting as the androgen receptor axis targeting agent and zenocutuzumab as the targeted therapy for tumors exhibiting NRG1 fusions. This regimen has not been approved for any indication as a fixed combination, but is the subject of ongoing clinical trials.

Other names
zenocutuzumab + abiraterone acetate
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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