Potential use of lapatinib in the treatment of head and neck squamous cell carcinoma (Review)
- Christina Sri Healthyni
- Toto Subroto
- Sandra Megantara
- Supat Jiranusornkul
- Jutti Levita
Affiliations: Surya Sumirat Pratama Clinic (Health Social Insurance Section of St. Borromeus Hospital), Bandung St. Yusup Hospital, Bandung, West Java 40132, Indonesia, Faculty of Mathematics and Natural Sciences, Padjadjaran University, Sumedang, West Java 45363, Indonesia, Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Padjadjaran University, Sumedang, West Java 45363, Indonesia, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand, Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Padjadjaran University, Sumedang, West Java 45363, Indonesia
- Published online on: September 5, 2022 https://doi.org/10.3892/wasj.2022.170
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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.