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datopotamab deruxtecan + 5-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
This is a **combination therapy** composed of datopotamab deruxtecan, an *antibody-drug conjugate (ADC)* targeting TROP2 (trophoblast cell surface antigen 2), and 5-fluorouracil, a classic *antimetabolite chemotherapeutic* agent. - **Datopotamab deruxtecan** consists of a humanized anti-TROP2 IgG1 monoclonal antibody conjugated to a topoisomerase I inhibitor (deruxtecan) via a stable, cleavable tetrapeptide linker. It delivers the cytotoxic deruxtecan payload specifically to TROP2-expressing tumor cells, causing DNA damage and cell death[1][2][3]. - **5-fluorouracil** is a pyrimidine analog that inhibits thymidylate synthase, interfering with DNA and RNA synthesis, and is utilized broadly in oncology. This combination is under clinical investigation for the treatment of advanced/metastatic solid tumors, including endometrial cancer[3].
- Brand names
- Adrucil (for 5-fluorouracil)
- Other names
- Dato-DXd + 5-FU
02
Targets
TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)TACSTD2 (Tumor-associated calcium signal transducer 2)
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