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trastuzumab rezetecan + capecitabine
- Development stage
- Phase 2
- Lead developer
- Jiangsu HengRui Medicine Co., Ltd.
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- 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)TS (Thymidylate synthase)
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