Abstract
Abstract Since the genomic aberrations of anaplastic lymphoma kinase (ALK) promote cancer cell proliferation and survival, specific tyrosine kinase inhibitors (TKIs) targeting these molecules have been developed. Besides its original targeting ALK effect, several studies have reported that ALK inhibitors can modulate the ATP-binding cassette (ABC) transporter to reverse the multiple drug resistance (MDR), which is one of the major obstacles for the successful cancer chemotherapy. In this chapter, we highlight reports manifesting that ALK inhibitors, including crizotinib, ceritinib, alectinib, and lorlatinib to antagonize ABC transporters to re-sensitize the anticancer drug in vitro and in vivo. These results give us some hints that specific ALK TKIs in combination with conventional anticancer drugs may be a good strategy to overcome the MDR in the clinic.
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