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rilvegostomig + trastuzumab deruxtecan + fluoropyrimidine

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

Overview

This is a combination regimen composed of three distinct agents: - **Rilvegostomig** is an investigational bispecific monoclonal antibody targeting PD-1 and LAG-3, designed to modulate immune checkpoint activity and enhance antitumor T-cell responses. - **Trastuzumab deruxtecan** (brand name Enhertu, also fam-trastuzumab deruxtecan-nxki) is an antibody-drug conjugate linking the HER2-targeted monoclonal antibody trastuzumab to the topoisomerase I inhibitor deruxtecan. It selectively binds HER2-expressing cells, is internalized, and releases deruxtecan to inhibit DNA replication and cause cell death, with activities in breast, gastric, and other HER2-positive tumors[1][2][3][4]. - **Fluoropyrimidine** refers to a class of antimetabolite chemotherapeutic agents (such as 5-fluorouracil or capecitabine) that function as pyrimidine analogs, interfering with DNA synthesis and causing cytotoxicity in dividing cells. This combination is under investigation for advanced gastrointestinal cancers, particularly HER2-positive gastric/gastroesophageal cancers, and is not currently approved for any indication as a combined regimen.

Other names
fam-trastuzumab deruxtecan-nxki
02

Targets

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

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