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Drug intelligence / Profile preview
trastuzumab rezetecan + retlirafusp alfa
- Development stage
- Phase 2
- Lead developer
- Hengrui Therapeutics
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
SHR-A1811 (trastuzumab rezetecan) is a third-generation HER2-targeted antibody-drug conjugate (ADC) that delivers a cytotoxic payload to HER2-expressing tumor cells. Its mechanism of action involves targeting the human epidermal growth factor receptor 2 (HER2) and delivering a DNA topoisomerase I inhibitor to induce cell death in cancer cells. It has demonstrated efficacy in HER2-mutant non-small cell lung cancer and HER2-positive breast cancer, among other solid tumors[1][5][8]. SHR-1701 (retlirafusp alfa) is a bifunctional fusion protein that targets both programmed death-ligand 1 (PD-L1) and transforming growth factor beta (TGF-β), thereby blocking immune checkpoint signaling and modulating the tumor microenvironment to enhance antitumor immunity[3][4]. The combination of these two agents represents an investigational regimen for advanced or metastatic solid tumors, leveraging both targeted cytotoxicity and immunomodulation.
- Other names
- trastuzumab rezetecanretlirafusp alfa
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)CD274 (Programmed cell death protein 1 ligand 1)TGFB (GARP–latent transforming growth factor beta 1 complex)
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