Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib.
Article Details
- CitationCopy to clipboard
Haouala A, Widmer N, Duchosal MA, Montemurro M, Buclin T, Decosterd LA
Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib.
Blood. 2011 Feb 24;117(8):e75-87. doi: 10.1182/blood-2010-07-294330. Epub 2010 Sep 1.
- PubMed ID
- 20810928 [ View in PubMed]
- Abstract
Several cancer treatments are shifting from traditional, time-limited, nonspecific cytotoxic chemotherapy cycles to continuous oral treatment with specific protein-targeted therapies. In this line, imatinib mesylate, a selective tyrosine kinases inhibitor (TKI), has excellent efficacy in the treatment of chronic myeloid leukemia. It has opened the way to the development of additional TKIs against chronic myeloid leukemia, including nilotinib and dasatinib. TKIs are prescribed for prolonged periods, often in patients with comorbidities. Therefore, they are regularly co-administered along with treatments at risk of drug-drug interactions. This aspect has been partially addressed so far, calling for a comprehensive review of the published data. We review here the available evidence and pharmacologic mechanisms of interactions between imatinib, dasatinib, and nilotinib and widely prescribed co-medications, including known inhibitors or inducers of cytochromes P450 or drug transporters. Information is mostly available for imatinib mesylate, well introduced in clinical practice. Several pharmacokinetic aspects yet remain insufficiently investigated for these drugs. Regular updates will be mandatory and so is the prospective reporting of unexpected clinical observations.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Nilotinib Cytochrome P450 2B6 Protein Humans UnknownInducerDetails Nilotinib Cytochrome P450 2C8 Protein Humans UnknownInhibitorInducerDetails Nilotinib Cytochrome P450 2D6 Protein Humans UnknownInhibitorDetails Nilotinib Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Nilotinib ATP-binding cassette sub-family G member 2 Protein Humans UnknownSubstrateInhibitorDetails Nilotinib P-glycoprotein 1 Protein Humans UnknownSubstrateInhibitorDetails Nilotinib UDP-glucuronosyltransferase 1-1 Protein Humans UnknownInhibitorDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareAcetaminophenGefitinib The serum concentration of Acetaminophen can be increased when it is combined with Gefitinib. AcetaminophenLapatinib The serum concentration of Acetaminophen can be increased when it is combined with Lapatinib. AcetaminophenGenistein The serum concentration of Acetaminophen can be increased when it is combined with Genistein. Acetaminophen3-[4-(1-formylpiperazin-4-yl)-benzylidenyl]-2-indolinone The serum concentration of Acetaminophen can be increased when it is combined with 3-[4-(1-formylpiperazin-4-yl)-benzylidenyl]-2-indolinone. AcetaminophenGeldanamycin The serum concentration of Acetaminophen can be increased when it is combined with Geldanamycin.