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trastuzumab deruxtecan + fluorouracil
- Development stage
- Unknown
- Lead developer
- Daiichi Sankyo
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Trastuzumab deruxtecan + fluorouracil is a combination treatment consisting of trastuzumab deruxtecan, an antibody-drug conjugate targeting HER2, and fluorouracil, a standard chemotherapeutic fluoropyrimidine. Trastuzumab deruxtecan consists of a humanized anti-HER2 monoclonal antibody conjugated with a cleavable tetrapeptide-based linker to a topoisomerase I inhibitor payload. It selectively binds to HER2 overexpressed on tumor cells and delivers the cytotoxic payload inside cells, leading to DNA damage and apoptosis. Fluorouracil inhibits thymidylate synthase, disrupting DNA synthesis and repair. This combination is under investigation as adjuvant and first-line therapy in HER2-positive gastric, gastroesophageal junction, and esophageal cancer patients, particularly those with minimal residual disease or advanced/metastatic disease after prior therapies[1][3][6].
- Brand names
- None for the specific combinationEnhertu (trastuzumab deruxtecan)
- Other names
- trastuzumab deruxtecan + 5-fluorouracilT-DXd + 5-FUT-DXd + capecitabine (related protocol variant)
02
Targets
TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)
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