Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …

The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …

Background Dacomitinib is a second-generation, irreversible EGFR tyrosine kinase inhibitor.
We compared its efficacy and safety with that of the reversible EGFR tyrosine kinase inhibitor …

Patients with non-small-cell lung cancer (NSCLC) whose tumours harbour activating
mutations within the epidermal growth factor receptor (EGFR) frequently derive significant …

The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

Purpose ARCHER 1050, a randomized, open-label, phase III study of dacomitinib versus
gefitinib in treatment-naïve patients with advanced non–small-cell lung cancer (NSCLC) and …

Background The EGFR T790M mutation is the most common mechanism of drug resistance
to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in patients who have …