Tyrosine kinase inhibitors for brain metastases in HER2-positive breast cancer

Cancer Treatment Reviews
Renata DuchnowskaJacek Jassem

Abstract

Approximately 30-50% of advanced HER2-positive breast cancer patients will develop central nervous system (CNS) metastases, with an annual risk of around 10%, and a half of them will die from brain progression. An increased risk of brain metastases is also seen in patients with early HER2-positive breast cancer administered curative therapy. Brain metastases in HER2-positive breast cancer patients usually constitute the first site of recurrence. The administration of anti-HER2 monoclonal antibodies, trastuzumab and pertuzumab, considerably delays the onset of symptomatic brain disease: however, the limited penetration of these compounds into the CNS hinders their efficacy. The small-molecule tyrosine kinase inhibitors of epidermal growth factor receptors family have established activity in HER2-positive breast cancer in both advanced disease and neoadjuvant setting. Favorable physico-chemical properties of these compounds allow them for a more efficient penetration through the blood-brain barrier, and hold the promise for more effective prevention and treatment of brain metastases. In this article we review the role of currently available or investigational HER2 tyrosine kinase inhibitors: lapatinib, neratinib, afatinib and tuc...Continue Reading

Citations

Mar 13, 2020·Journal of Translational Medicine·Wen JianChun Gui
Aug 31, 2020·Expert Review of Anticancer Therapy·Mafalda OliveiraCristina Saura
Feb 20, 2019·International Journal of Molecular Sciences·Catarina Roma-RodriguesAlexandra R Fernandes
Feb 9, 2021·PLoS Neglected Tropical Diseases·Conall SauveyRuben Abagyan
Nov 18, 2020·International Journal of Molecular Sciences·Jorge Esteban-VillarrubiaJavier Molina-Cerrillo
Mar 7, 2021·International Journal of Molecular Sciences·Jinsha LiuSepideh Afshar
May 11, 2019·Experimental Cell Research·Daniel W ColeAndrew M Fribley
Aug 21, 2021·Bioorganic & Medicinal Chemistry·Thais Cristina Mendonça Nogueira, Marcus Vinicius Nora de Souza

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