title: Efficacy and mechanism of action of the tyrosine kinase inhibitors gefitinib, lapatinib and neratinib in the treatment of HER2-positive breast cancer: preclinical and clinical evidence.
abstract: An increasing number of tumors, including breast cancer, overexpress proteins of the epidermal growth factor receptor (EGFR) family. The interaction between family members activates signaling pathways that promote tumor progression and resistance to treatment. Human epidermal growth factor receptor type II (HER2) positive breast cancer represents a clinical challenge for current therapy. It has motivated the development of novel and more effective therapeutic EGFR family target drugs, such as tyrosine kinase inhibitors (TKIs). This review focuses on the effects of three TKIs mostly studied in HER2- positive breast cancer, lapatinib, gefitinib and neratinib. Herein, we discuss the mechanism of action, therapeutic advantages and clinical applications of these TKIs. To date, TKIs seem to be promising therapeutic agents for the treatment of HER2-overexpressing breast tumors, either as monotherapy or combined with other pharmacological agents.
authors.affiliation: Departamento de Biología de la Reproducción, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán Avenida Vasco de Quiroga No. 15, Col. Belisario Domínguez Sección XVI, Tlalpan 14080, México, D. F., México ; Posgrado en Ciencias Biológicas, Universidad Nacional Autónoma de México, Circuito Interior, Cuidad Universitaria Av. Universidad 3000, Coyoacán 04510, México D. F, México.
authors.forename: Mariana
authors.initials: M
authors.lastname: Segovia-Mendoza
authors.affiliation: Departamento de Biología de la Reproducción, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán Avenida Vasco de Quiroga No. 15, Col. Belisario Domínguez Sección XVI, Tlalpan 14080, México, D. F., México.
authors.forename: María E
authors.initials: ME
authors.lastname: González-González
authors.affiliation: Departamento de Biología de la Reproducción, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán Avenida Vasco de Quiroga No. 15, Col. Belisario Domínguez Sección XVI, Tlalpan 14080, México, D. F., México.
authors.forename: David
authors.initials: D
authors.lastname: Barrera
authors.affiliation: Departamento de Biología de la Reproducción, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán Avenida Vasco de Quiroga No. 15, Col. Belisario Domínguez Sección XVI, Tlalpan 14080, México, D. F., México.
authors.forename: Lorenza
authors.initials: L
authors.lastname: Díaz
authors.affiliation: Departamento de Biología de la Reproducción, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán Avenida Vasco de Quiroga No. 15, Col. Belisario Domínguez Sección XVI, Tlalpan 14080, México, D. F., México.
authors.forename: Rocío
authors.initials: R
authors.lastname: García-Becerra
keywords: HER2-positive breast cancer; epidermal growth factor receptor family; gefitinib; lapatinib; neratinib; tyrosine kinase inhibitors