Drug intelligence / Profile preview

pyrotinib

Development stage
Phase 4
Lead developer
Hengrui Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Pyrotinib is an orally administered, irreversible small molecule tyrosine kinase inhibitor that targets multiple members of the ErbB family, specifically epidermal growth factor receptor (EGFR/HER1), human epidermal growth factor receptor 2 (HER2/ErbB2), and HER4. By covalently binding to the ATP-binding site of these receptors' intracellular kinase domains, pyrotinib blocks their phosphorylation and activation, thereby inhibiting downstream signaling pathways such as RAS/RAF/MEK/MAPK and PI3K/AKT. This results in reduced tumor cell proliferation and increased apoptosis. Pyrotinib was developed primarily for the treatment of HER2-positive advanced or metastatic breast cancer, especially in patients previously treated with anthracyclines or taxanes. It has demonstrated efficacy even in trastuzumab-resistant cases and is conditionally approved in China for use in combination with capecitabine for this indication[1][3][4][5][7][8].

Brand names
Irene
Other names
pyrroltinib maleate
02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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