Abstract
Oral multikinase inhibitors and mammalian target of rapamycin (mTOR) inhibitors such as everolimus have been widely used to treat patients with various types of advanced cancer. However, these drugs have variable pharmacokinetic characteristics, and a significant number of patients often experience severe adverse events leading to dose reduction/interruption or treatment discontinuation. Therefore, it is important to develop an individualized dosing strategy for oral targeted therapies. Currently, associations between drug exposure and treatment outcomes have been described for several tyrosine kinase inhibitors as well as everolimus in cancer patients. Hence, the use of therapeutic drug monitoring (TDM) is considered one of such strategies to optimize drug exposure. In this symposium, we will focus on the clinical pharmacokinetics of regorafenib and its metabolites and the mTOR inhibitor everolimus, and the utility of TDM to improve treatment outcomes will be discussed.
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