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Clinical Pharmacokinetic Studies

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Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays

Abstract

Drug efficacy and response are a function of drug concentration over time. In clinical pharmacokinetic studies, aspects of drug absorption, distribution, metabolism, and excretion over time are assessed. In the early clinical development, the pharmacokinetics of a drug is studied in healthy subjects followed by studies in patient population(s) with the aim to find the relevant dose in the target population(s). Particular pharmacokinetic studies in special populations assess the necessity of a dose adjustment from the planned/established clinical dose for patients.

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Abbreviations

Ae:

Amount of drug excreted unchanged in urine

ANOVA:

Analysis of variance

AUC:

Area under the curve

BMI:

Body mass index

C12,C24 :

Plasma concentration 12 and 24 h after administration

CI 90 %:

90 % confidence Interval

CLCR :

Creatinine clearance

CLR :

Renal clearance

CLtot/F:

Relative total clearance

Cmax :

Maximum concentration

Cmax :

Maximum plasma concentration

CV:

Coefficient of variation

CYP3A4:

Cytochrome P450 3A4

day –1:

Study day prior to day of study medication administration

fu:

Unbound fraction of XYZ123 in plasma

h:

Hour

INN:

International nonproprietary name

IU:

International units

L:

Liter

Mg:

Milligram

MRT:

Mean residence time

NPH:

Neutral protamine Hagedorn (isophane insulin)

Rac:

Accumulation ratio

RHI:

Regular human insulin

s.c.:

Subcutaneous(ly)

t1/2,λ1 :

Main elimination half-life

t1/2,λz :

Terminal elimination half-life

t12t24 :

Time 12 and 24 h after administration

Tmax :

Time to maximum concentration

tmax :

Time to maximum plasma concentration

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Authors and Affiliations

  1. Sanofi Deutschland GmbH, Frankfurt am Main, Germany

    Dr. Axel Steinstraesser, Dr. Roland Wesch & Dr. Annke Frick

Authors
  1. Dr. Axel Steinstraesser
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  2. Dr. Roland Wesch
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  3. Dr. Annke Frick
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Corresponding author

Correspondence to Axel Steinstraesser .

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Editors and Affiliations

  1. Sanofi Pharma Deutschland GmbH, A company of the Sanofi-Aventis Group Industriepark Hoechst, Frankfurt am Main, Germany

    Jochen Maas

  2. Dieburg, Germany

    Franz J. Hock

  3. Idstein, Germany

    Dieter Mayer

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Steinstraesser, A., Wesch, R., Frick, A. (2013). Clinical Pharmacokinetic Studies. In: Vogel, H.G., Maas, J., Hock, F.J., Mayer, D. (eds) Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-25240-2_49

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