Drug intelligence / Profile preview

ZN-1041 + trastuzumab deruxtecan

Development stage
Phase 2
Lead developer
Roche
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

ZN-1041 + trastuzumab deruxtecan is a combination therapy consisting of ZN-1041, a blood-brain barrier (BBB) penetrable HER2 tyrosine kinase inhibitor (TKI), and trastuzumab deruxtecan (Enhertu), an antibody-drug conjugate. This combination is being investigated for the treatment of HER2-positive breast cancer with or without central nervous system (CNS) metastases. Preclinical studies have shown that the combination demonstrates significant improvement in intracranial tumor growth inhibition compared to trastuzumab deruxtecan alone. In clinical trials, the combination has shown promising efficacy in treatment-refractory settings, including in patients who previously progressed on trastuzumab deruxtecan and/or TKI therapy.

Other names
trastuzumab deruxtecanDS-8201aDS8201aDS 8201a
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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