Von in vitro zu in vivo: Optimierung von ADME-Tox-Eigenschaften

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Zusammenfassung

Die Wechselwirkung einer Substanz mit der Bindestelle eines therapeutisch relevanten biologischen Makromoleküls ist die entscheidende Grundlage für ihre Eignung als Arzneistoff. Eine andere, nicht minder wichtige Voraussetzung ist die Fähigkeit der Substanz, vom Ort der Applikation auf einem oft sehr verschlungenen Weg zum Wirkort zu gelangen. Dazu muss die Substanz wässrige Phasen und Lipidmembranen durchdringen. Je nach ihrer Wasser- und Lipidlöslichkeit wird sie auf diesem Weg in unterschiedliche Bereiche (Kompartimente) des biologischen Systems gelangen. Durch metabolisierende Enzyme wird sie chemisch verändert. Nach Konjugation oder Abbau wird sie schließlich über die Niere, die Galle und/oder den Darm ausgeschieden (► Abschn. 9.1).

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Correspondence to Gerhard Klebe .

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Klebe, G. (2023). Von in vitro zu in vivo: Optimierung von ADME-Tox-Eigenschaften. In: Wirkstoffdesign. Springer Spektrum, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-67209-9_19

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  • DOI: https://doi.org/10.1007/978-3-662-67209-9_19

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