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trastuzumab deruxtecan + volrustomig + capecitabine

Development stage
Preclinical
Lead developer
Daiichi Sankyo
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

This entry describes a **combination regimen** of three drugs: - **Trastuzumab deruxtecan**, an antibody-drug conjugate targeting HER2, delivering the topoisomerase I inhibitor deruxtecan to HER2-expressing tumor cells. - **Volrustomig (MEDI5752)**, a bispecific monoclonal antibody that binds both PD-1 and CTLA-4, facilitating immune checkpoint inhibition. - **Capecitabine**, an oral prodrug converted to 5-fluorouracil, a cytotoxic antimetabolite that interferes with DNA synthesis. This combination is being investigated in clinical trials for HER2-positive and HER2-expressing advanced or metastatic cancers, aiming to leverage tumor targeting, immune activation, and cytotoxic effects. While combinations of trastuzumab deruxtecan with checkpoint inhibitors and capecitabine (a standard chemotherapeutic backbone in HER2-positive breast and gastric cancers) are under study[5][6][7], no specific results are currently available for the combination with volrustomig. Trials with the related bispecific antibody rilvegostomig indicate the therapeutic concept may be similar[4][5].

Other names
fam-trastuzumab deruxtecanDS-8201aDS8201aDS 8201aMEDI5752MEDI-5752MEDI 5752fluoropyrimidine carbamate
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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