Drug intelligence / Profile preview

trastuzumab deruxtecan + fluorouracil + durvalumab

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

This combination is an investigational multi-drug regimen under clinical evaluation for **HER2-expressing gastric cancer and gastroesophageal junction (GEJ) adenocarcinoma**[1][2][7]. - **Trastuzumab deruxtecan** is an antibody-drug conjugate targeting HER2, consisting of a humanized anti-HER2 antibody linked to a topoisomerase I inhibitor (deruxtecan), resulting in direct cytotoxicity to HER2-positive cancer cells. - **Fluorouracil (5-FU)** is a cytotoxic antimetabolite that interferes with DNA synthesis, causing cell death by inhibiting thymidylate synthase[3][6]. - **Durvalumab** is an immune checkpoint inhibitor (monoclonal antibody) targeting programmed death ligand 1 (PD-L1), designed to enhance anti-tumor immune response[7]. The regimen is administered intravenously and is under investigation in phase 1/2 clinical trials for the first-line treatment of advanced/metastatic HER2-expressing gastric/GEJ cancers. No formal combination brand name exists. Key developers are AstraZeneca for durvalumab and Daiichi Sankyo for trastuzumab deruxtecan; both are directly involved in clinical development[7].

Brand names
Enhertu (for trastuzumab deruxtecan)None (no combination brand name identified)
Other names
T-DXd + 5-FU + durvalumabtrastuzumab deruxtecan + 5-fluorouracil + durvalumab
02

Targets

TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CD274 (Programmed cell death protein 1 ligand 1)TS (Thymidylate synthase)

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