Source:http://linkedlifedata.com/resource/pubmed/id/10806604
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2000-7-12
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pubmed:abstractText |
Tenecteplase is a site-specific engineered tissue plasminogen activator (t-PA) variant that can be administered as a single intravenous bolus injection because of its slower plasma clearance. The objective of this study was to investigate the dose-ranging pharmacokinetics and pharmacodynamics of intravenous bolus tenecteplase compared with intravenous alteplase recombinant t-PA in patients with acute myocardial infarction. A total of 103 patients received intravenous bolus doses of 30, 40, or 50 mg tenecteplase, and 56 patients received 100 mg rt-PA as the accelerated 90-minute infusion regimen in this randomized, open-label study. Tenecteplase and r-tPA plasma concentrations were measured for 6 hours. Tenecteplase exhibited biphasic elimination from the plasma with a mean initial half-life of 22 minutes and a mean terminal half-life of 115 minutes. The mean plasma clearance was 105 mL/min and did not depend on tenecteplase dose over the dose range studied. In comparison, rt-PA has a fourfold faster plasma clearance. Pharmacokinetic-pharmacodynamic evaluation showed that a dose of approximately 0.5 mg/kg results in a plasma AUC value that provides a TIMI 3 flow at 90 minutes that is comparable to that reported with accelerated r-tPA. In conclusion, tenecteplase has a fourfold slower plasma clearance compared with rt-PA, allowing dosing as an i.v. bolus injection. Weight-adjusted dosing of tenecteplase may optimize the therapeutic regimen of tenecteplase.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0091-2700
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
40
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
508-15
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:10806604-Adult,
pubmed-meshheading:10806604-Age Factors,
pubmed-meshheading:10806604-Aged,
pubmed-meshheading:10806604-Aged, 80 and over,
pubmed-meshheading:10806604-Area Under Curve,
pubmed-meshheading:10806604-Body Weight,
pubmed-meshheading:10806604-Dose-Response Relationship, Drug,
pubmed-meshheading:10806604-Female,
pubmed-meshheading:10806604-Fibrinolytic Agents,
pubmed-meshheading:10806604-Humans,
pubmed-meshheading:10806604-Infusions, Intravenous,
pubmed-meshheading:10806604-Injections, Intravenous,
pubmed-meshheading:10806604-Male,
pubmed-meshheading:10806604-Metabolic Clearance Rate,
pubmed-meshheading:10806604-Middle Aged,
pubmed-meshheading:10806604-Myocardial Infarction,
pubmed-meshheading:10806604-Tissue Plasminogen Activator
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pubmed:year |
2000
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pubmed:articleTitle |
Pharmacokinetics and pharmacodynamics of tenecteplase: results from a phase II study in patients with acute myocardial infarction.
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pubmed:affiliation |
Genentech, Inc., San Francisco, CA, USA.
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Comparative Study,
Randomized Controlled Trial,
Research Support, Non-U.S. Gov't,
Clinical Trial, Phase II
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