Practical guidelines for therapeutic drug monitoring of anticancer tyrosine kinase inhibitors: focus on the pharmacokinetic targets.

作者: Huixin Yu , Neeltje Steeghs , Cynthia M. Nijenhuis , Jan H. M. Schellens , Jos H. Beijnen

DOI: 10.1007/S40262-014-0137-2

关键词: Tyrosine kinaseDosingTherapeutic drug monitoringPharmacologyPazopanibSorafenibMedicineSunitinibImatinibPharmacokinetics

摘要: There is accumulating evidence for potential benefits of therapeutic drug monitoring (TDM) in the treatment cancer with tyrosine kinase inhibitors (TKIs). Relationships between exposure and response (efficacy/toxicity) have been established several TKIs. For example, pharmacokinetic targets efficacy imatinib, sunitinib pazopanib defined as trough plasma concentrations (Ctrough) >1,000, >50 >20,000 ng/mL selected indications, respectively. Dose adjustment based on could therefore increase rates duration. Furthermore, appropriate target defined, excessive side effects patients using current fixed dosing strategy may be prevented. This review provides a practical guideline TDM currently approved TKIs at 28 February 2013. The focus this article elaboration relationships proposed targets, mainly Ctrough, further interpretation recommendations dose titrations.

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