Neratinib (CAS 698387-09-6) Suppliers and Product Information

Neratinib is an oral pan-HER inhibitor that irreversibly inhibits the tyrosine kinase activity of epidermal growth factor receptors. It is primarily used for the treatment of HER2-positive breast cancer and has shown efficacy in clinical trials for non-small cell lung cancer and colon cancer. Neratinib selectively inhibits HER-1 and HER-2 of the EGFR family with IC50 values of 92 nmol/L and 59 nmol/L, respectively.

Frequently Asked Questions about Neratinib

Q: What is the mechanism of action of Neratinib?

A: Neratinib is an irreversible inhibitor of the HER2 kinase. It forms a covalent bond with Cys-797 at the edge of the active site cleft, making its binding irreversible. This mechanism allows it to potentially circumvent acquired resistance developed against reversible inhibitors.

Q: What are the main side effects of Neratinib?

A: The most common side effects of Neratinib include diarrhea, nausea, vomiting, and fatigue.

Q: Has Neratinib shown efficacy in clinical trials?

A: Yes, Neratinib has shown efficacy in clinical trials. In a phase II trial for advanced HER2-positive breast cancer, it demonstrated 16-week progression-free survival rates of 59% for patients with previous trastuzumab treatment and 78% for trastuzumab-naive patients.

Q: Is Neratinib genotoxic?

A: According to studies, Neratinib and its metabolites were not found to be genotoxic. However, it did show some effects on embryo-fetal development in animal studies at certain doses.