Drug intelligence / Profile preview

trastuzumab deruxtecan + rilvegostomig + fluorouracil

Development stage
Unknown
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
01

Overview

**trastuzumab deruxtecan + rilvegostomig + fluorouracil** is an investigational combination regimen for first-line treatment of HER2-positive, locally advanced or metastatic gastric or gastroesophageal junction adenocarcinoma. Trastuzumab deruxtecan is an antibody-drug conjugate comprising an anti-HER2 monoclonal antibody linked to a topoisomerase I inhibitor (deruxtecan), inducing tumor cell death by internalizing into HER2-expressing cancer cells and releasing the cytotoxic payload. Rilvegostomig is a bispecific antibody targeting both PD-1 (programmed cell death protein 1) and TIGIT (T-cell immunoreceptor with Ig and ITIM domains), acting as an immune checkpoint inhibitor to stimulate anti-tumor immunity. Fluorouracil is a fluoropyrimidine antimetabolite that inhibits thymidylate synthase, blocking DNA synthesis and impairing tumor cell proliferation. This triple combination is being assessed in phase 3 clinical trials as an alternative to current standard therapies, aiming to enhance efficacy by integrating targeted therapy, immunotherapy, and cytotoxic chemotherapy mechanisms[1][3][6].

Brand names
none for rilvegostomig (investigational)none for fluorouracil
Other names
trastuzumab deruxtecan + AZD2936 + 5-fluorouracilT-DXd + rilvegostomig + 5-FU
02

Targets

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

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