Drug intelligence / Profile preview

pyrotinib + trastuzumab + aromatase inhibitor (Hengrui Pharmaceutical)

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

Overview

Pyrotinib is an orally active, irreversible pan-ErbB receptor tyrosine kinase inhibitor that targets EGFR (HER1), HER2, and HER4. Developed by Jiangsu Hengrui Pharmaceuticals, it is approved in China for the treatment of HER2-positive metastatic breast cancer. This specific combination therapy, being evaluated in a Phase II trial sponsored by Peking Union Medical College Hospital, involves the administration of pyrotinib alongside trastuzumab (a HER2-targeted monoclonal antibody) and an aromatase inhibitor (such as anastrozole, letrozole, or exemestane). The regimen is intended for the first-line treatment of patients with HER2-positive and hormone receptor (HR)-positive metastatic or inoperable locally advanced breast cancer, aiming to provide a comprehensive blockade of both the HER2 and estrogen receptor signaling pathways.

Brand names
AiRuiNiHerceptin
Other names
Pyrotinib maleate
02

Targets

EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)CYP19A1 (Aromatase)

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