Drug intelligence / Profile preview

pyrotinib + pertuzumab + trastuzumab

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination therapy consists of pyrotinib, an irreversible pan-ErbB tyrosine kinase inhibitor, alongside the monoclonal antibodies pertuzumab and trastuzumab. It is being evaluated as a precision treatment for HER2-positive salivary gland carcinoma in a Phase 2 umbrella trial sponsored by Peking Union Medical College. Pyrotinib inhibits the intracellular kinase domains of HER1 (EGFR), HER2, and HER4, while trastuzumab and pertuzumab bind to distinct epitopes on the extracellular domain of the HER2 receptor to inhibit dimerization and downstream signaling. This multi-pronged approach aims to achieve more complete blockade of the HER2 pathway to overcome resistance and improve efficacy in HER2-driven malignancies.

Brand names
AiRuiNi
Other names
pyrotinib + pertuzumab + trastuzumab-Peking Union Medical College-salivary gland carcinomaHER2-targeted triple therapyHER-2-targeted triple therapyHER 2-targeted triple therapy
02

Targets

EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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