Drug intelligence / Profile preview

trastuzumab rezetecan + capecitabine

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

Overview

SHR-A1811 + capecitabine is an investigational combination therapy consisting of trastuzumab rezetecan (SHR-A1811), a HER2-targeted antibody-drug conjugate (ADC), and capecitabine, an oral fluoropyrimidine chemotherapy. Trastuzumab rezetecan comprises a humanized anti-HER2 IgG1 monoclonal antibody conjugated to a DNA topoisomerase I inhibitor payload (SHR9265) via a cleavable tetrapeptide-based linker, featuring a high drug-to-antibody ratio (DAR) of 6. Capecitabine acts as a prodrug of 5-fluorouracil, which is converted into active metabolites that inhibit thymidylate synthase, thereby interfering with DNA synthesis and cell proliferation. This combination is primarily being developed by Jiangsu Hengrui Pharmaceutical (via Suzhou Suncadia Biopharmaceuticals) for the treatment of HER2-expressing advanced or metastatic gastric and gastroesophageal junction (GEJ) adenocarcinomas, aiming to leverage the targeted delivery of the ADC alongside the systemic cytotoxic effects of capecitabine.

Other names
SHR-A1811 + capecitabineSHR-A1811 plus capecitabineSHR-A-1811 plus capecitabineSHR-A 1811 plus capecitabine
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)DNA

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