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HLX91-048-based HER2 ADC
- Development stage
- Preclinical
- Lead developer
- Henlius
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
HLX91-048-based HER2 ADC (also known as HLX91) is a preclinical antibody-drug conjugate (ADC) being developed by Shanghai Henlius Biotech. It consists of a HER2-targeting monoclonal antibody conjugated to a novel small-molecule payload, HLX91-048, via a cleavable GGFG linker, with a drug-to-antibody ratio (DAR) of 4 or 8. HLX91-048 features a 3-(4-hydroxyphenyl) indoline-2 scaffold and acts through a distinct mechanism of action involving the prolonged activation of the unfolded protein response (UPR). This candidate has demonstrated potent antitumor efficacy in preclinical models of HER2-positive breast cancer and DS-8201-resistant gastric cancer, showing enhanced cytotoxicity, stronger bystander killing, and greater plasma stability compared to a DS-8201 analog.
- Other names
- HER2-GGFG-HLX91-048 ADCHER-2-GGFG-HLX91-048 ADCHER 2-GGFG-HLX91-048 ADC
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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