Peter Dogterom

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Org 26576 acts by modulating ionotropic AMPA-type glutamate receptors to enhance glutamatergic neurotransmission. The aim of this Phase 1b study (N=54) was to explore safety, tolerability, pharmacokinetics, and pharmacodynamics of Org 26576 in depressed patients. Part I (N=24) evaluated the maximum tolerated dose (MTD) and optimal titration schedule in a(More)
As part of the overall product development and manufacturing strategy, pharmaceutical companies routinely change formulation and manufacturing site. Depending on the type and level of change and the BCS class of the molecule, dissolution data and/or bioequivalence (BE) may be needed to support the change for immediate release dosage forms. In this report,(More)
Background: A key challenge to dose selection in early central nervous system (CNS) clinical drug development is that patient tolerability profiles often differ from those of healthy volunteers (HVs), yet HVs are the modal population for determining doses to be investigated in phase II trials. Without clear tolerability data from the target patient(More)
INTRODUCTION The α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor potentiator Org 26576 represents an interesting pharmacological tool to evaluate the utility of glutamatergic enhancement towards the treatment of psychiatric disorders. In this study, a rat-human translational pharmacokinetic-pharmacodynamic (PK-PD) model of AMPA receptor(More)
To determine the effects of food on the pharmacokinetics of sublingual asenapine. Healthy male volunteers (n = 26, age 19–53 years) randomly received a single sublingual dose of asenapine 5 mg after ≥10 h fasting (Treatment A, reference), after a high-fat meal (Treatment B) and after ≥10 h fasting with a high-fat meal at 4 h post-dose (Treatment C). Blood(More)
Objective: To investigate the effects of rifampin on the steady-state pharmacokinetics of gepirone and metabo-lites after multiple dosing of both drugs. Methods: 24 subjects completed a randomized crossover study with 2 study phases separated by a washout period of at least 4 weeks. The subjects received multiple dosing of gepirone extended-release(More)
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