Potential use of lapatinib in the treatment of head and neck squamous cell carcinoma (Review)

Abstract

To date, cetuximab is the only anti-epidermal growth factor receptor (EGFR) monoclonal antibody (mAb) approved for the targeted therapy of head and neck squamous cell carcinoma (HNSCC). However, this therapy has left an eloquent number of patients with recurrence and local or/and distance failures, which are associated with Erb-B2 receptor tyrosine kinase 2 (ERBB2) signaling. The dual targeting (EGFR/ERBB2) irreversible covalent tyrosine kinase inhibitor (TKI), afatinib, has exhibited promising results in HNSCC trials; however, its toxicity arises from further biosynthesis for receptor recovery. Conversely, lapatinib, a reversible TKI, is almost as potent as afatinib, and its interaction with the unique inactive conformation of EGFR has been shown to be associated with its selectivity, specificity and long residence time, resulting in efficacy. However, as a monotherapy, lapatinib appears minimally active and hepatotoxicity has been reported with its use. The present review article summarizes some of the research conducted over the years in order to determine the profile of lapatinib along, with its potential for use in the treatment of HNSCC and associated challenges.