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Research ArticleArticle

Pharmacokinetics of All-trans Retinoic Acid, 13-cis Retinoic Acid, and Fenretinide in Plasma and Brain of Rat

François Le Doze, Daniele Debruyne, Françoise Albessard, Louisa Barre and Gilles Louis Defer
Drug Metabolism and Disposition February 2000, 28 (2) 205-208;
François Le Doze
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Daniele Debruyne
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Françoise Albessard
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Louisa Barre
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Gilles Louis Defer
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Abstract

We have measured the pharmacokinetics of three retinoids, all-trans retinoic acid, 13-cis retinoic acid, and fenretinide in rat blood and rat brain [especially white matter (WM) and gray matter (GM)] to help select retinoids for treating human malignant glioma. All-trans retinoic acid permeated well into the WM, giving peak concentration in WM of 25.7 μg/g, 6 to 7 times higher than the peak serum concentration. There was less 13-cis retinoic acid in WM: area under the curve (AUC)0→∞ WM/AUC0→∞serum = 18.00 μg ml−1 h/32.67 μg ml−1 h. The ratio WM/GM was over 1 for these two compounds, but the half-lives were short in the serum and cerebral tissue (0.57–1.02 h). Fenretinide had different pharmacokinetics: the peak concentrations were in serum (1.7 μg/ml) and WM (1.2 μg/ml)–low, but the AUC0→∞ was large (25.55 μg ml−1 in serum and 57.53 μg ml−1 in WM) due to its long elimination half-life (13.78 h in serum and 17.77 h in WM). These findings provide information that may be used to select a retinoid and establish therapeutic regimens that provide optimal efficacy with minimal toxicity.

Footnotes

  • Send reprint requests to: Danièle Debruyne, Laboratory of Pharmacology, University Hospital Center Côte de Nacre, 14032 Caen Cedex, France. E-mail:debruyne-d{at}chu-caen.fr

  • Abbreviations used are::
    RA
    retinoic acid
    ATRA
    all-trans retinoic acid
    WM
    white matter
    GM
    gray matter
    AUC
    area under the serum or brain concentration versus time curves
    DMSO
    dimethyl sulfoxide
    • Received June 16, 1999.
    • Accepted October 25, 1999.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 28 (2)
Drug Metabolism and Disposition
Vol. 28, Issue 2
1 Feb 2000
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Research ArticleArticle

Pharmacokinetics of All-trans Retinoic Acid, 13-cis Retinoic Acid, and Fenretinide in Plasma and Brain of Rat

François Le Doze, Daniele Debruyne, Françoise Albessard, Louisa Barre and Gilles Louis Defer
Drug Metabolism and Disposition February 1, 2000, 28 (2) 205-208;

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Research ArticleArticle

Pharmacokinetics of All-trans Retinoic Acid, 13-cis Retinoic Acid, and Fenretinide in Plasma and Brain of Rat

François Le Doze, Daniele Debruyne, Françoise Albessard, Louisa Barre and Gilles Louis Defer
Drug Metabolism and Disposition February 1, 2000, 28 (2) 205-208;
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