Pharmacokinetics of Dasatinib.

Jana Hořínková,Ondřej Slanař,Martin Šíma

doi:10.14712/23362936.2019.10

Abstract

Tyrosine kinase inhibitors have recently become an essential tool in management of chronic myeloid leukaemia (CML). Dasatinib, a representative of those drugs, acts by inhibiting key proteins included in CML development, predominantly Bcr-Abl and Src. Its advantage is that it shows activity in many cases where other agents bring no improvement due to resistance. Pharmacokinetics of dasatinib has specific characteristics that may play an important role in achieving sufficient exposure in patients. Therefore, the key pharmacokinetic properties are summarized in this report. For example, dasatinib absorption is significantly influenced by gastric pH and its modulation can be a source of serious interactions, as well as simultaneous administration of drugs affecting cytochrome P450.

Highlights

Pharmacokinetics of DasatinibA representative of those drugs, acts by inhibiting key proteins included in chronic myeloid leukaemia (CML) development, predominantly Bcr-Abl and Src. Its advantage is that it shows activity in many cases where other agents bring no improvement due to resistance
Possibilities of chronic myeloid leukaemia (CML) therapy have recently been broadening as there are new agents with antitumor activity that can be used to treat this hematologic malignancy
Indications in adults include Philadelphia chromosomepositive chronic myeloid leukaemia (Ph+ CML) in chronic phase and Philadelphia chromosome-positive acute lymphoblastic leukaemia (Ph+ ALL), it is approved for treatment of Ph+ CML in chronic phase in paediatric patients (Bristol-Myers Squibb, 2017)

Summary

Pharmacokinetics of Dasatinib

A representative of those drugs, acts by inhibiting key proteins included in CML development, predominantly Bcr-Abl and Src. Its advantage is that it shows activity in many cases where other agents bring no improvement due to resistance. Dasatinib absorption is significantly influenced by gastric pH and its modulation can be a source of serious interactions, as well as simultaneous administration of drugs affecting cytochrome P450.

Introduction

Clinical data

Findings

Conclusion