Anaplastic lymphoma kinase (ALK) inhibitors are important treatment options
for non-small-cell lung cancer (NSCLC), associated with ALK gene rearrangement. Patients
with ALK gene rearrangement show sensitivity to and benefit clinically from treatment with
ALK tyrosine kinase inhibitors (ALK-TKIs). To date, crizotinib, ceritinib, alectinib, brigatinib, lorlatinib, and entrectinib have received approval from the US Food and Drug
Administration and/or the European Medicines Agency for use during the treatment of ALKgene-rearrangement forms of NSCLC. Although the oral route of administration is convenient and results in good compliance among patients, oral administration can be affected by
many factors, such as food, intragastric pH, cytochrome P450 enzymes, transporters, and
p-glycoprotein. These factors can result in increased risks for serious adverse events or can
lead to reduced therapeutic effects of ALK-TKIs. This review characterizes and summarizes
the pharmacokinetic parameters and drug–-drug interactions associated with ALK-TKIs to
provide specific recommendations for oncologists and clinical pharmacists when prescribing
ALK-TKIs READ ARTICLE
Drug Design, Development and Therapy DOI:10.2147/DDDT.S249098
Authors: Dehua Zhao, Jing Chen, Mingming Chu, Xiaoqing Long, Jisheng Wang