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Tytuł pozycji:

A clinical pharmacokinetics study of carzelesin given by short-term intravenous infusion in a phase I study.

Tytuł :
A clinical pharmacokinetics study of carzelesin given by short-term intravenous infusion in a phase I study.
Index Terms :
Sciences bio-médicales et agricoles
Antineoplastic Agents -- administration & dosage
Antineoplastic Agents -- blood
Antineoplastic Agents -- chemistry
Antineoplastic Agents -- pharmacokinetics
Area Under Curve
Benzofurans -- administration & dosage
Benzofurans -- blood
Benzofurans -- chemistry
Benzofurans -- pharmacokinetics
Chromatography, High Pressure Liquid
Humans
Indoles -- administration & dosage
Indoles -- blood
Indoles -- chemistry
Indoles -- pharmacokinetics
Infusions, Intravenous
Lymphoma -- metabolism
Metabolic Clearance Rate
info:eu-repo/semantics/article
info:ulb-repo/semantics/articlePeerReview
info:ulb-repo/semantics/openurl/article
Wydawca :
1998
Dodane szczegóły :
Van Tellingen, Olaf
Punt, Cornelis
Awada, Ahmad
Wagener, Th
Piccart-Gebhart, Martine
Groot, Yvonne
Schaaf, L J
Henrar, R E
Nooijen, W J
Beijnen, J H
Typ dokumentu :
Zasób elektroniczny
URL :
http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/55582">http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/55582
http://worldcat.org/search?q=on:EQY+http://difusion-oai.ulb.ac.be/oai/request+DCG_ENTIRE_REPOSITORY+CNTCOLL">http://worldcat.org/search?q=on:EQY+http://difusion-oai.ulb.ac.be/oai/request+DCG_ENTIRE_REPOSITORY+CNTCOLL
Dostępność :
Open access content. Open access content
Pozostałe numery :
EQY oai:dipot.ulb.ac.be:2013/55582
uri/info:pmid/9523733
764590628
Źródło wspomagające :
UNIV LIBR DE BRUXELLES
From OAIster®, provided by the OCLC Cooperative.
Numer akcesji :
edsoai.ocn764590628
Zasób elektroniczny
We investigated the pharmacokinetic behavior of carzelesin in 31 patients receiving this drug by 10-min intravenous infusion in a Phase I clinical trial, which was conducted at institutions in Nijmegen (institution 1) and Brussels (institution 2). The dose steps were 24, 48, 96, 130, 150, 170, 210, 250, and 300 microg/m2. Carzelesin is a cyclopropylpyrroloindole prodrug that requires metabolic activation via U-76,073 to U-76,074. The lower limit of quantitation (LLQ) of the high-performance liquid chromatography (HPLC) method used in this study was 1 ng/ml for the parent drug and its metabolic products. Carzelesin was rapidly eliminated from plasma (elimination half-life 23 +/- 9 min; mean value +/- SD). At all dose levels, U-76,073 was found as early as in the first samples taken after the start of the infusion. However, the concentration of U-76,074 exceeded the LLQ for only short periods and only at the higher dose levels. Although the plasma levels of all three compounds were well above the respective IC50 values obtained by in vitro clonogenic assays, they were much lower than those observed in a preclinical study in mice. There was a substantial discrepancy in the mean plasma clearance observed between patients from institution 1 (7.9 +/- 2.1 l h[-1] m[-2]) and those from institution 2 (18.4 +/- 13.6 l h[-1] m[-2]; P = 0.038), probably reflecting problems with drug administration in the latter institution. The results recorded for patients in institution 1 indicated that the AUC increased proportionately with increasing doses. There was a good correlation between the maximal plasma concentration and the AUC, enabling future monitoring of drug exposure from one timed blood sample. Urinary excretion of carzelesin was below 1% of the delivered dose.
Clinical Trial
Clinical Trial, Phase I
Journal Article
Multicenter Study
info:eu-repo/semantics/published

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