Clinical Pharmacokinetics and Pharmacodynamics of Bosutinib.

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Abbas R, Hsyu PH

Clinical Pharmacokinetics and Pharmacodynamics of Bosutinib.

Clin Pharmacokinet. 2016 Oct;55(10):1191-1204. doi: 10.1007/s40262-016-0391-6.

PubMed ID

27113346 [ View in PubMed

]

Abstract

Chronic myeloid leukemia (CML) is a clonal myeloproliferative stem cell disorder. Bosutinib is an oral, once-daily SRC/ABL tyrosine kinase inhibitor with very potent inhibitory activity. Bosutinib is effective against all phases of intolerant or resistant Philadelphia chromosome-positive CML that do not harbor the T315I or V299LABL kinase domain mutations. Peak plasma concentrations of bosutinib occur at 4-6 h following oral administration, and dose-proportional increases in exposure are observed at doses ranging from 200 to 800 mg. Absorption of bosutinib increases with food. Bosutinib is distributed extensively into the tissues. It is highly plasma protein bound (94 %) and is primarily metabolized in the liver by cytochrome P450 3A4. Bosutinib is well tolerated overall and has a unique but manageable toxicity profile. This article provides a review of the available clinical pharmacokinetic, pharmacodynamic, and drug-drug interaction data on bosutinib in healthy subjects, patients with CML, and special populations.

DrugBank Data that Cites this Article

Drug Reactions

Reaction
Bosutinib DB06616 Cytochrome P450 3A4 N-desmethylbosutinib DBMET03736	Details
Bosutinib DB06616 Cytochrome P450 3A4 Oxydechlorinated bosutinib DBMET03737	Details

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
Integrate drug-drug interactions in your software
Bosutinib Magnesium oxide	Magnesium oxide can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Sodium bicarbonate	Sodium bicarbonate can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Aluminum hydroxide	Aluminum hydroxide can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Calcium carbonate	Calcium carbonate can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Magaldrate	Magaldrate can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.