Drug intelligence / Profile preview

DZD1516 + trastuzumab + capecitabine

Development stage
Unknown
Lead developer
Dizal Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen of **DZD1516**, **trastuzumab**, and **capecitabine** under clinical investigation for the treatment of HER2-positive metastatic breast cancer, particularly in patients who have progressed following prior therapies. DZD1516 is a small molecule, highly selective HER2 tyrosine kinase inhibitor designed for optimal blood-brain barrier penetration, aiming to treat or prevent central nervous system metastases. Trastuzumab is a recombinant humanized monoclonal antibody targeted against HER2 (ERBB2), while capecitabine is an oral prodrug of 5-fluorouracil (a cytotoxic antimetabolite). The regimen is being studied for its safety, tolerability, pharmacokinetics, and anti-tumor activity in HER2-positive advanced or metastatic breast cancer, especially those with CNS (brain) metastases[1][3][5].

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)

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