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DZD1516 + ado-trastuzumab emtansine
- Development stage
- Unknown
- Lead developer
- Dizal Pharmaceutical
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
This drug is a **combination of DZD1516 and ado-trastuzumab emtansine (T-DM1)**. DZD1516 is a highly selective, reversible tyrosine kinase inhibitor (TKI) designed to inhibit HER2 (human epidermal growth factor receptor 2) with full blood-brain barrier penetration for the treatment of HER2-positive metastatic breast cancer, particularly with central nervous system (CNS) metastases. Ado-trastuzumab emtansine (T-DM1) is an antibody-drug conjugate consisting of the monoclonal antibody trastuzumab linked to the cytotoxic agent DM1, which targets HER2-expressing tumor cells and delivers the chemotherapeutic directly. Combined, this regimen is being investigated for enhanced efficacy in HER2-positive cancers with CNS involvement or brain metastases, aiming to leverage DZD1516's CNS penetration and HER2 inhibition with the targeted cytotoxic delivery of T-DM1[1][3].
- Brand names
- Kadcyla (for ado-trastuzumab emtansine)
- Other names
- DZD1516 + T-DM1DZD1516 + trastuzumab emtansine
02
Targets
TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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