Drug intelligence / Profile preview

ZN-A-1041

Development stage
Phase 2
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

ZN-A-1041 (also known as ZN-1041 or Perzebertinib) is a brain-permeable, selective oral tyrosine kinase inhibitor targeting the human epidermal growth factor receptor 2 (HER2). It is specifically designed to cross the blood-brain barrier and has demonstrated high selectivity and a broad safety margin in preclinical studies. The drug shows promising antitumor activity both as monotherapy and in combination with other agents such as capecitabine and trastuzumab for patients with HER2-positive breast cancer with brain metastases. Clinical trials have shown encouraging efficacy—including partial responses and disease control—in heavily pretreated patients with HER2-positive advanced solid tumors, especially those with central nervous system involvement. The most common adverse events are generally mild to moderate gastrointestinal symptoms or laboratory abnormalities; serious toxicities are rare[1][4][6][8].

Other names
ZN-A-1041ZN-A1041ZN-A 1041ZN-1041ZN1041ZN 1041Perzebertinib
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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