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trastuzumab rezetecan
- Development stage
- Phase 4
- Lead developer
- Hengrui Therapeutics
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
Trastuzumab rezetecan is a novel antibody-drug conjugate (ADC) designed to target HER2-expressing or HER2-mutant cancers. It consists of the humanized anti-HER2 monoclonal antibody trastuzumab linked via a cleavable tetrapeptide-based linker to a DNA topoisomerase I inhibitor payload (rezetecan, also known as SHR169265 or described as a camptothecin derivative). The drug is engineered to deliver the cytotoxic agent directly into HER2-positive tumor cells after binding and internalization, resulting in targeted DNA damage and cell death. Trastuzumab rezetecan has demonstrated high objective response rates and manageable safety in clinical trials for patients with advanced non-small cell lung cancer (NSCLC) harboring HER2 mutations. It is under development by Jiangsu Hengrui Medicine for multiple solid tumors including breast cancer, biliary tract cancer, colorectal cancer, gastric cancer, cervical cancer, ovarian cancer, endometrial cancer, and gastroesophageal junction adenocarcinoma.
- Brand names
- Avida
- Other names
- Trastuzumab Rezetecan
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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