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Review

The Emerging Therapeutic Landscape of ALK Inhibitors in Non-Small Cell Lung Cancer

1
Department of Surgical, Oncological and Oral Sciences, University of Palermo, 90127 Palermo, Italy
2
Department of Biomedicine, Neuroscience and Advanced Diagnostics (Bi.N.D.), Section of Medical Oncology, University of Palermo, 90127 Palermo, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
These authors are co-last.
Pharmaceuticals 2020, 13(12), 474; https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120474
Received: 29 October 2020 / Revised: 3 December 2020 / Accepted: 16 December 2020 / Published: 18 December 2020
(This article belongs to the Special Issue Treatment Options and Therapeutics for Non-small Cell Lung Cancer)
The treatment of metastatic non-small cell lung cancer (NSCLC) has undergone a paradigm shift over the last decade. Better molecular characterization of the disease has led to the rapid improvement of personalized medicine and the prompt delivery of targeted therapies to patients with NSCLC. The discovery of the EML4-ALK fusion gene in a limited subset of patients affected by NSCLC and the subsequent clinical development of crizotinib in 2011 has been an impressive milestone in lung cancer research. Unfortunately, acquired resistances regularly develop, hence disease progression occurs. Afterward, modern tyrosine kinase inhibitors (TKIs), such as ceritinib, alectinib, brigatinib, and lorlatinib, have been approved by the Food and Drug Administration (FDA) for the management of anaplastic lymphoma kinase (ALK)-positive NSCLCs. Several compounds are currently under investigation to achieve the optimal strategy of therapy. Additionally, the results of ongoing clinical trials with novel-generation TKI will provide more evidence on the best sequence in the treatment of ALK-positive NSCLC patients. In this review, we provide a comprehensive overview of the state-of-the-art targeted therapy options in ALK-positive NSCLCs. Resistance, potential therapeutic strategies to overcome drug resistance, and future perspectives for this subset of patients are critically analyzed and summarized. View Full-Text
Keywords: non-small cell lung cancer (NSCLC); tyrosine kinase inhibitors (TKIs); ALK inhibitors; crizotinib; ceritinib; alectinib; brigatinib; lorlatinib; ensartinib non-small cell lung cancer (NSCLC); tyrosine kinase inhibitors (TKIs); ALK inhibitors; crizotinib; ceritinib; alectinib; brigatinib; lorlatinib; ensartinib
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MDPI and ACS Style

Gristina, V.; La Mantia, M.; Iacono, F.; Galvano, A.; Russo, A.; Bazan, V. The Emerging Therapeutic Landscape of ALK Inhibitors in Non-Small Cell Lung Cancer. Pharmaceuticals 2020, 13, 474. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120474

AMA Style

Gristina V, La Mantia M, Iacono F, Galvano A, Russo A, Bazan V. The Emerging Therapeutic Landscape of ALK Inhibitors in Non-Small Cell Lung Cancer. Pharmaceuticals. 2020; 13(12):474. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120474

Chicago/Turabian Style

Gristina, Valerio, Maria La Mantia, Federica Iacono, Antonio Galvano, Antonio Russo, and Viviana Bazan. 2020. "The Emerging Therapeutic Landscape of ALK Inhibitors in Non-Small Cell Lung Cancer" Pharmaceuticals 13, no. 12: 474. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120474

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