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Xenobiotica
the fate of foreign compounds in biological systems
Volume 30, 2000 - Issue 8
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Research Article

Pharmacokinetics of the M1-agonist talsaclidine in mouse, rat, rabbit and monkey, and extrapolation to man

A. Leusch Department of Pharmacokinetics and Drug Metabolism, Boehringer Ingelheim Pharma KG, 88397 Biberach, Germany
,
W. Troger Department of Pharmacokinetics and Drug Metabolism, Boehringer Ingelheim Pharma KG, 88397 Biberach, Germany
,
A. Greischel Department of Pharmacokinetics and Drug Metabolism, Boehringer Ingelheim Pharma KG, 88397 Biberach, Germany
&
W. Roth Department of Pharmacokinetics and Drug Metabolism, Boehringer Ingelheim Pharma KG, 88397 Biberach, Germany
Pages 797-814 | Published online: 22 Sep 2008
 
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Abstract

1. Talsaclidine is an M1-agonist under development for the treatment of Alzheimer's disease. The aim of the study was to investigate the absorption, distribution, metabolism and excretion (ADME) of single intravenous and oral doses of [14C]-talsaclidine in mouse, rat, rabbit and monkey. Previous data in humans showed that the drug was mainly excreted into the urine as the unchanged parent drug. The hypothesis was tested if animal data of drugs, which are mainly excreted renally, could be extrapolated to human. 2. The apparent volume of distribution at steady-state (Vss) was comparable in all animal species (2-5 l.kg-1

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