Drug intelligence / Profile preview

trastuzumab deruxtecan + rilvegostomig + capecitabine

Development stage
Unknown
Lead developer
AstraZeneca
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 (trastuzumab Deruxtecan), Intravenous (rilvegostomig), Oral (capecitabine)
01

Overview

This is a **combination therapy** comprised of trastuzumab deruxtecan, rilvegostomig, and capecitabine under active clinical investigation, primarily for **HER2-positive and HER2-low gastric, gastroesophageal junction, and esophageal adenocarcinoma**. - **Trastuzumab deruxtecan** is an antibody-drug conjugate that binds HER2 and delivers a topoisomerase I inhibitor payload via a cleavable tetrapeptide linker, resulting in targeted cytotoxicity to HER2-expressing tumor cells. - **Rilvegostomig** is a bispecific monoclonal antibody targeting both PD-1 and TIGIT, designed to enhance antitumor immune activity by checkpoint inhibition. - **Capecitabine** is a fluoropyrimidine chemotherapy prodrug metabolized into 5-fluorouracil (5-FU), which disrupts DNA synthesis in proliferating cells. This regimen is currently in **Phase 2 and Phase 3 clinical trials** as neoadjuvant, adjuvant, and first-line treatment in HER2-positive and HER2-low populations, often as an alternative to combinations with pembrolizumab or other chemotherapy[1][2][3][4]. Developers and sponsors include AstraZeneca and Daiichi Sankyo.

Brand names
Enhertu
Other names
trastuzumab deruxtecan + rilvegostomig + capecitabine
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)TIGIT (T cell immunoreceptor with Ig and ITIM domains)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP1 (DNA Topoisomerase I)

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