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Therapeutic Drug Monitoring of Kinase Inhibitors in Oncology.

ABSTRACT: Although kinase inhibitors (KI) frequently portray large interpatient variability, a 'one size fits all' regimen is still often used. In the meantime, relationships between exposure-response and exposure-toxicity have been established for several KIs, so this regimen could lead to unnecessary toxicity and suboptimal efficacy. Dose adjustments based on measured systemic pharmacokinetic levels-i.e., therapeutic drug monitoring (TDM)-could therefore improve treatment efficacy and reduce the incidence of toxicities. Therefore, the aim of this comprehensive review is to give an overview of the available evidence for TDM for the 77 FDA/EMA kinase inhibitors currently approved (as of July 1st, 2023) used in hematology and oncology. We elaborate on exposure-response and exposure-toxicity relationships for these kinase inhibitors and provide practical recommendations for TDM and discuss corresponding pharmacokinetic targets when possible.

SUBMITTER: van der Kleij MBA

PROVIDER: S-EPMC10519871 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature

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Therapeutic Drug Monitoring of Kinase Inhibitors in Oncology.

van der Kleij Maud B A MBA Guchelaar Niels A D NAD Mathijssen Ron H J RHJ Versluis Jurjen J Huitema Alwin D R ADR Koolen Stijn L W SLW Steeghs Neeltje N

Clinical pharmacokinetics 20230816 10

Although kinase inhibitors (KI) frequently portray large interpatient variability, a 'one size fits all' regimen is still often used. In the meantime, relationships between exposure-response and exposure-toxicity have been established for several KIs, so this regimen could lead to unnecessary toxicity and suboptimal efficacy. Dose adjustments based on measured systemic pharmacokinetic levels-i.e., therapeutic drug monitoring (TDM)-could therefore improve treatment efficacy and reduce the inciden ...[more]

PMID: 37584840

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