Drug intelligence / Profile preview

pyrotinib + trastuzumab + aromatase inhibitor

Development stage
Unknown
Lead developer
Hengrui Therapeutics
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

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

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