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ado-trastuzumab emtansine + neratinib
- Development stage
- Unknown
- Lead developer
- Puma Biotechnology
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
Ado-trastuzumab emtansine (T-DM1) plus neratinib is an investigational combination therapy for HER2-positive breast cancer, particularly in patients with brain metastases or molecular residual disease. Ado-trastuzumab emtansine is an antibody-drug conjugate that combines the HER2-targeted monoclonal antibody trastuzumab with the cytotoxic agent DM1, delivering targeted chemotherapy to HER2-overexpressing tumor cells. Neratinib is an irreversible small molecule tyrosine kinase inhibitor targeting HER2 and EGFR family receptors. The combination aims to provide dual blockade of the HER2 pathway, potentially overcoming resistance mechanisms and improving outcomes in heavily pretreated or high-risk patients. This regimen has shown intracranial activity and ctDNA clearance in early-phase clinical trials but is not yet approved as a fixed combination[1][3][4][7].
- Brand names
- Kadcyla + Nerlynx
- Other names
- trastuzumab emtansine + neratinibT-DM1 plus neratinibT-DM-1 plus neratinibT-DM 1 plus neratinib
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)TUBB (Tubulin (alpha and beta subunits))EGFR (Epidermal growth factor receptor)
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