Neratinib

Drug Overview

Neratinib (Puma Biotechnology) is an irreversible tyrosine kinase inhibitor that blocks signal transduction through the human epidermal growth factor receptor (HER)1, HER2, HER4, and epidermal growth factor receptor kinases. Inhibition of these kinase domains is thought to lead to apoptosis and down-regulation of the ErbB signaling pathway. Furthermore, irreversible pan-HER drugs illicit prolonged blockade of multiple targets, a mechanism thought to overcome signaling redundancy and adaptability.

Analyst Outlook

Puma Biotechnology has filed regulatory submissions for neratinib (Puma Biotechnology) with the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA) in the extended adjuvant setting based on data from the Phase III ExteNET study. The trial demonstrated that neratinib can fulfill an unmet need in human epidermal growth factor receptor 2-positive (HER2+) breast cancer by improving disease-free survival (DFS) rates in patients who have previously received Herceptin (trastuzumab; Genentech/Roche/Chugai) as an adjuvant therapy. Neratinib is the first targeted therapy to demonstrate a statistically significant clinical benefit in this lucrative treatment setting, which will differentiate it from other established drugs in the HER2+ breast cancer market.