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capecitabine + trastuzumab emtansine
- Development stage
- Discontinued
- Lead developer
- Genentech
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
Capecitabine + trastuzumab emtansine is a combination regimen used in the treatment of HER2-positive cancers, particularly metastatic breast cancer. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), a small molecule antimetabolite that inhibits DNA synthesis by interfering with thymidylate synthase. Trastuzumab emtansine (also known as T-DM1 or ado-trastuzumab emtansine) is an antibody-drug conjugate composed of the monoclonal antibody trastuzumab linked to the cytotoxic agent DM1 (emtansine), a microtubule inhibitor derived from maytansinoid. Trastuzumab targets and binds to human epidermal growth factor receptor 2 (HER2), blocking downstream signaling and delivering DM1 directly into HER2-overexpressing tumor cells, where it disrupts microtubule function and induces cell death. The combination aims to enhance antitumor activity by leveraging both targeted delivery of cytotoxic therapy and inhibition of DNA synthesis[1][3][5].
- Other names
- capecitabine + T-DM1capecitabine + ado-trastuzumab emtansine
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)
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