Clinical activity of the EGFR tyrosine kinase inhibitor osimertinib in EGFR-mutant glioblastoma

Autor: Igor Makhlin, Ryan D Salinas, Daniel Zhang, Fadi Jacob, Gou-li Ming, Hongjun Song, Deeksha Saxena, Jay F Dorsey, MacLean P Nasrallah, Jennifer JD Morrissette, Zev A Binder, Donald M O'Rourke, Arati S Desai, Steven Brem, Stephen J Bagley
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: CNS Oncology, Vol 8, Iss 3 (2019)
Druh dokumentu: article
ISSN: 2045-0915
2045-0907
DOI: 10.2217/cns-2019-0014
Popis: Glioblastoma (GBM) is the most common primary malignant brain tumor in adults and carries a dismal prognosis. The EGFR gene is among the most commonly deranged genes in GBM and thus an important therapeutic target. We report the case of a young female with heavily pretreated EGFR-mutated GBM, for whom we initiated osimertinib, an oral, third-generation tyrosine kinase inhibitor that irreversibly inhibits EGFR and has significant brain penetration. We then review some of the main challenges in targeting EGFR, including lack of central nervous system penetration with most tyrosine kinase inhibitors, molecular heterogeneity of GBM and the need for enhanced specificity for the EGFR mutations relevant in GBM.
Databáze: Directory of Open Access Journals