Drug intelligence / Profile preview

trastuzumab deruxtecan + capecitabine + oxaliplatin

Development stage
Phase 2
Lead developer
Daiichi Sankyo
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous (trastuzumab Deruxtecan, Oxaliplatin), Oral (capecitabine)
01

Overview

A triple drug combination of **trastuzumab deruxtecan** (an antibody-drug conjugate targeting HER2), **capecitabine** (an oral prodrug of 5-fluorouracil, a pyrimidine analog antimetabolite), and **oxaliplatin** (a platinum-based chemotherapeutic). Trastuzumab deruxtecan is an anti-HER2 antibody linked to a topoisomerase I inhibitor payload via a cleavable linker, designed to inhibit HER2-positive tumor cells by delivering cytotoxic activity directly, causing double-strand breaks and cell death. Capecitabine is converted to 5-fluorouracil in the body, inhibiting thymidylate synthase and blocking DNA synthesis. Oxaliplatin forms DNA adducts that trigger cell cycle arrest and apoptosis. The combination is under investigation in clinical trials for HER2-positive gastric, gastroesophageal, and esophageal cancers, aiming to maximize antitumor activity by integrating targeted and cytotoxic modalities[3][5].

Brand names
Enhertu (for trastuzumab deruxtecan)
Other names
T-DXd + capecitabine + oxaliplatin
02

Targets

DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)

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