Practical Guidelines for Therapeutic Drug Monitoring of Anticancer Tyrosine Kinase Inhibitors: Focus on the Pharmacokinetic Targets
There is accumulating evidence for potential benefits of therapeutic drug monitoring (TDM) in the treatment of cancer with tyrosine kinase inhibitors (TKIs). Relationships between exposure and response (efficacy/toxicity) have been established for several TKIs. For example, the pharmacokinetic targe...
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| Veröffentlicht in: | Clinical pharmacokinetics 2014-04, Vol.53 (4), p.305-325 |
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| container_title | Clinical pharmacokinetics |
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| creator | Yu, Huixin Steeghs, Neeltje Nijenhuis, Cynthia M. Schellens, Jan H. M. Beijnen, Jos H. Huitema, Alwin D. R. |
| description | There is accumulating evidence for potential benefits of therapeutic drug monitoring (TDM) in the treatment of cancer with tyrosine kinase inhibitors (TKIs). Relationships between exposure and response (efficacy/toxicity) have been established for several TKIs. For example, the pharmacokinetic targets for efficacy of imatinib, sunitinib and pazopanib have been defined as trough plasma concentrations (
C
trough
) of >1,000, >50 and >20,000 ng/mL for selected indications, respectively. Dose adjustment based on pharmacokinetic targets could therefore increase response rates and duration. Furthermore, with appropriate target concentrations defined, excessive side effects in patients using the current fixed dosing strategy may be prevented. This review provides a practical guideline for TDM for the currently approved TKIs at 28 February 2013. The focus of this article is on the elaboration of exposure and response relationships of TKIs with proposed pharmacokinetic targets, mainly
C
trough
, and further on the interpretation of the pharmacokinetic targets with recommendations for dose titrations. |
| doi_str_mv | 10.1007/s40262-014-0137-2 |
| format | Article |
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C
trough
) of >1,000, >50 and >20,000 ng/mL for selected indications, respectively. Dose adjustment based on pharmacokinetic targets could therefore increase response rates and duration. Furthermore, with appropriate target concentrations defined, excessive side effects in patients using the current fixed dosing strategy may be prevented. This review provides a practical guideline for TDM for the currently approved TKIs at 28 February 2013. The focus of this article is on the elaboration of exposure and response relationships of TKIs with proposed pharmacokinetic targets, mainly
C
trough
, and further on the interpretation of the pharmacokinetic targets with recommendations for dose titrations.</description><identifier>ISSN: 0312-5963</identifier><identifier>EISSN: 1179-1926</identifier><identifier>DOI: 10.1007/s40262-014-0137-2</identifier><identifier>PMID: 24566736</identifier><identifier>CODEN: CPKNDH</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Antineoplastic Agents - administration & dosage ; Antineoplastic Agents - pharmacokinetics ; Antineoplastic Agents - therapeutic use ; Biological and medical sciences ; Drug Monitoring - methods ; General pharmacology ; Humans ; Internal Medicine ; Medical sciences ; Medicine ; Medicine & Public Health ; Neoplasms - drug therapy ; Neoplasms - metabolism ; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions ; Pharmacology. Drug treatments ; Pharmacology/Toxicology ; Pharmacotherapy ; Protein Kinase Inhibitors - administration & dosage ; Protein Kinase Inhibitors - pharmacokinetics ; Protein Kinase Inhibitors - therapeutic use ; Protein-Tyrosine Kinases - antagonists & inhibitors ; Review Article</subject><ispartof>Clinical pharmacokinetics, 2014-04, Vol.53 (4), p.305-325</ispartof><rights>Springer International Publishing Switzerland 2014</rights><rights>2015 INIST-CNRS</rights><rights>Copyright Wolters Kluwer Health Adis International Apr 2014</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c468t-60c03edd988caa21560618c7aa9be690a55e9802b78c5e31acc2a74361786c083</citedby><cites>FETCH-LOGICAL-c468t-60c03edd988caa21560618c7aa9be690a55e9802b78c5e31acc2a74361786c083</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s40262-014-0137-2$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s40262-014-0137-2$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,41464,42533,51294</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=28345037$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24566736$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yu, Huixin</creatorcontrib><creatorcontrib>Steeghs, Neeltje</creatorcontrib><creatorcontrib>Nijenhuis, Cynthia M.</creatorcontrib><creatorcontrib>Schellens, Jan H. M.</creatorcontrib><creatorcontrib>Beijnen, Jos H.</creatorcontrib><creatorcontrib>Huitema, Alwin D. R.</creatorcontrib><title>Practical Guidelines for Therapeutic Drug Monitoring of Anticancer Tyrosine Kinase Inhibitors: Focus on the Pharmacokinetic Targets</title><title>Clinical pharmacokinetics</title><addtitle>Clin Pharmacokinet</addtitle><addtitle>Clin Pharmacokinet</addtitle><description>There is accumulating evidence for potential benefits of therapeutic drug monitoring (TDM) in the treatment of cancer with tyrosine kinase inhibitors (TKIs). Relationships between exposure and response (efficacy/toxicity) have been established for several TKIs. For example, the pharmacokinetic targets for efficacy of imatinib, sunitinib and pazopanib have been defined as trough plasma concentrations (
C
trough
) of >1,000, >50 and >20,000 ng/mL for selected indications, respectively. Dose adjustment based on pharmacokinetic targets could therefore increase response rates and duration. Furthermore, with appropriate target concentrations defined, excessive side effects in patients using the current fixed dosing strategy may be prevented. This review provides a practical guideline for TDM for the currently approved TKIs at 28 February 2013. The focus of this article is on the elaboration of exposure and response relationships of TKIs with proposed pharmacokinetic targets, mainly
C
trough
, and further on the interpretation of the pharmacokinetic targets with recommendations for dose titrations.</description><subject>Antineoplastic Agents - administration & dosage</subject><subject>Antineoplastic Agents - pharmacokinetics</subject><subject>Antineoplastic Agents - therapeutic use</subject><subject>Biological and medical sciences</subject><subject>Drug Monitoring - methods</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Internal Medicine</subject><subject>Medical sciences</subject><subject>Medicine</subject><subject>Medicine & Public Health</subject><subject>Neoplasms - drug therapy</subject><subject>Neoplasms - metabolism</subject><subject>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</subject><subject>Pharmacology. Drug treatments</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacotherapy</subject><subject>Protein Kinase Inhibitors - administration & dosage</subject><subject>Protein Kinase Inhibitors - pharmacokinetics</subject><subject>Protein Kinase Inhibitors - therapeutic use</subject><subject>Protein-Tyrosine Kinases - antagonists & inhibitors</subject><subject>Review Article</subject><issn>0312-5963</issn><issn>1179-1926</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNp1kE1vEzEQhi0EoqHwA7ggS4jjwtjetb3cqkJLRRE9hLM1cWYTl8QO9u6hZ_44XiV8XDhYPvh53xk_jL0U8FYAmHelBallA6KtR5lGPmILIUzfiF7qx2wBSsim67U6Y89KuQcAKwGesjPZdlobpRfs511GPwaPO349hTXtQqTCh5T5cksZDzTVR_4hTxv-JcUwphzihqeBX8Q5FT1V8iGnUnP8c4hYiN_EbVjNaHnPr5KfCk-Rj1vid1vMe_Tpe4Xn2iXmDY3lOXsy4K7Qi9N9zr5dfVxefmpuv17fXF7cNr7Vdmw0eFC0XvfWekQpOg1aWG8Q-xXpHrDrqLcgV8b6jpRA7yWaVmlhrPZg1Tl7few95PRjojK6-zTlWEc6oaFvZausrJQ4Ur7-qmQa3CGHPeYHJ8DN2t1Ru6va3azdzZlXp-Zptaf1n8RvzxV4cwKwVNdDruZC-ctZ1XagTOXkkSuHWTTlf1b87_RfmrGbIw</recordid><startdate>20140401</startdate><enddate>20140401</enddate><creator>Yu, Huixin</creator><creator>Steeghs, Neeltje</creator><creator>Nijenhuis, Cynthia M.</creator><creator>Schellens, Jan H. 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R.</creator><general>Springer International Publishing</general><general>Adis International</general><general>Springer Nature B.V</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>4T-</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope></search><sort><creationdate>20140401</creationdate><title>Practical Guidelines for Therapeutic Drug Monitoring of Anticancer Tyrosine Kinase Inhibitors: Focus on the Pharmacokinetic Targets</title><author>Yu, Huixin ; Steeghs, Neeltje ; Nijenhuis, Cynthia M. ; Schellens, Jan H. 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Drug treatments</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacotherapy</topic><topic>Protein Kinase Inhibitors - administration & dosage</topic><topic>Protein Kinase Inhibitors - pharmacokinetics</topic><topic>Protein Kinase Inhibitors - therapeutic use</topic><topic>Protein-Tyrosine Kinases - antagonists & inhibitors</topic><topic>Review Article</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yu, Huixin</creatorcontrib><creatorcontrib>Steeghs, Neeltje</creatorcontrib><creatorcontrib>Nijenhuis, Cynthia M.</creatorcontrib><creatorcontrib>Schellens, Jan H. M.</creatorcontrib><creatorcontrib>Beijnen, Jos H.</creatorcontrib><creatorcontrib>Huitema, Alwin D. 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M.</au><au>Beijnen, Jos H.</au><au>Huitema, Alwin D. R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Practical Guidelines for Therapeutic Drug Monitoring of Anticancer Tyrosine Kinase Inhibitors: Focus on the Pharmacokinetic Targets</atitle><jtitle>Clinical pharmacokinetics</jtitle><stitle>Clin Pharmacokinet</stitle><addtitle>Clin Pharmacokinet</addtitle><date>2014-04-01</date><risdate>2014</risdate><volume>53</volume><issue>4</issue><spage>305</spage><epage>325</epage><pages>305-325</pages><issn>0312-5963</issn><eissn>1179-1926</eissn><coden>CPKNDH</coden><abstract>There is accumulating evidence for potential benefits of therapeutic drug monitoring (TDM) in the treatment of cancer with tyrosine kinase inhibitors (TKIs). Relationships between exposure and response (efficacy/toxicity) have been established for several TKIs. For example, the pharmacokinetic targets for efficacy of imatinib, sunitinib and pazopanib have been defined as trough plasma concentrations (
C
trough
) of >1,000, >50 and >20,000 ng/mL for selected indications, respectively. Dose adjustment based on pharmacokinetic targets could therefore increase response rates and duration. Furthermore, with appropriate target concentrations defined, excessive side effects in patients using the current fixed dosing strategy may be prevented. This review provides a practical guideline for TDM for the currently approved TKIs at 28 February 2013. The focus of this article is on the elaboration of exposure and response relationships of TKIs with proposed pharmacokinetic targets, mainly
C
trough
, and further on the interpretation of the pharmacokinetic targets with recommendations for dose titrations.</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>24566736</pmid><doi>10.1007/s40262-014-0137-2</doi><tpages>21</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0312-5963 |
| ispartof | Clinical pharmacokinetics, 2014-04, Vol.53 (4), p.305-325 |
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| language | eng |
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| source | MEDLINE; SpringerLink Journals - AutoHoldings |
| subjects | Antineoplastic Agents - administration & dosage Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - therapeutic use Biological and medical sciences Drug Monitoring - methods General pharmacology Humans Internal Medicine Medical sciences Medicine Medicine & Public Health Neoplasms - drug therapy Neoplasms - metabolism Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions Pharmacology. Drug treatments Pharmacology/Toxicology Pharmacotherapy Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - therapeutic use Protein-Tyrosine Kinases - antagonists & inhibitors Review Article |
| title | Practical Guidelines for Therapeutic Drug Monitoring of Anticancer Tyrosine Kinase Inhibitors: Focus on the Pharmacokinetic Targets |
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