Drug intelligence / Profile preview

pyrotinib + trastuzumab + aromatase inhibitor

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

Overview

A combination therapy regimen consisting of pyrotinib, trastuzumab, and an aromatase inhibitor (AI). Pyrotinib is an oral, irreversible pan-HER tyrosine kinase inhibitor (TKI) that targets EGFR (HER1), HER2, and HER4. Trastuzumab is a recombinant DNA-derived humanized monoclonal antibody that selectively binds to the extracellular domain of the human epidermal growth factor receptor 2 (HER2). Aromatase inhibitors (such as letrozole, anastrozole, or exemestane) are endocrine therapies that block the enzyme aromatase, thereby reducing estrogen production. This triplet combination is being investigated by the Tianjin Medical University Cancer Institute and Hospital as a neoadjuvant (preoperative) treatment for patients with stage II-IIIA hormone receptor-positive (HR+) and HER2-positive breast cancer, aiming to achieve synergistic anti-tumor effects through simultaneous dual HER2 blockade and estrogen deprivation.

Other names
pyrotinib + trastuzumab + AIpyrrolitinib + trastuzumab + AI
02

Targets

CYP19A1 (Aromatase)PDGFRB (Platelet-derived growth factor receptor beta)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)KIT (c-KIT proto-oncogene receptor tyrosine kinase)AR (Adrenergic receptors)VEGFR2 (Vascular endothelial growth factor receptor 2)

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