Drug intelligence / Profile preview

neratinib

Development stage
Approved
Lead developer
Puma Biotechnology
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Neratinib is an orally available, irreversible pan-HER tyrosine kinase inhibitor used primarily for the treatment of HER2-positive breast cancer. It binds covalently to cysteine residues in the ATP-binding pocket of the tyrosine kinase domains of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and HER4, thereby inhibiting their autophosphorylation and downstream signaling through pathways such as MAPK and AKT[4][7][8]. This inhibition slows or stops the proliferation of cancer cells that overexpress these receptors. Neratinib is indicated for extended adjuvant treatment in adults with early-stage HER2-overexpressed/amplified breast cancer following adjuvant trastuzumab-based therapy, as well as in combination with capecitabine for advanced or metastatic hormone receptor-positive/HER2-positive breast cancer after prior therapies[2][3][5]. The drug was developed by Puma Biotechnology.

Brand names
Nerlynx
Other names
NERLYNXNERLYNX SKUOuyoubi
02

Targets

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

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