Schnider Medicinal Chemist's Guide to Solving ADMET Challenges

1. Auflage 2021
ISBN: 978-1-83916-049-3
Verlag: Royal Society of Chemistry
Format: EPUB
Kopierschutz: 6 - ePub Watermark

E-Book, Englisch, Band Volume 79, 518 Seiten

Reihe: Drug Discovery Series

The Medicinal Chemist’s Guide to Solving ADMET Challenges summarizes a series of design strategies and tactics that have been successfully employed across pharmaceutical and academic laboratories to solve common ADMET issues. These are exemplified with a curated collection of concrete examples displayed in a highly visual “table-of-contents” style format, allowing readers to rapidly identify the most promising approaches applicable to their own challenges. Each ADMET parameter is introduced in a concise yet comprehensive manner and includes background, relevance and screening strategies. Medicinal chemistry knowledge of how best to modify molecular structure to solve ADMET issues is challenging to retrieve from the literature, public databases and even corporate data warehouses. The Medicinal Chemist’s Guide to Solving ADMET Challenges addresses this gap by presenting state-of-the-art design strategies put together by a global group of experienced medicinal chemists and ADMET experts across academia and the pharmaceutical industry.

Autoren/Hrsg.

Schnider, Patrick

Fachgebiete

• Naturwissenschaften Biowissenschaften Biochemie (nichtmedizinisch)
• Naturwissenschaften Chemie Organische Chemie

Inhaltsverzeichnis

Overview of Strategies for Solving ADMET Challenges;Tactics to Improve Solubility;Optimisation of Passive Permeability for Oral Absorption;Targeting Gastrointestinal Uptake Transporters;Drug Efflux Transporters: P-gp and BCRP;OATs and OCTs: The SLC22 Family of Organic Anion and Cation Transporters;OATPs: The SLCO Family of Organic Anion Transporting Polypeptide Transporters;Bile Salt Export Pump (BSEP) Inhibition;Cytochrome P450 Metabolism;Cytochrome P450 Induction;Strategies to Mitigate CYP450 Inhibition;Aldehyde and Xanthine Oxidase Metabolism;Glucuronidation;Sulfation;Reactive Metabolites;Genotoxicity;Drug-induced Photosensitivity;Drug-induced Phospholipidosis;Cardiac Ion Channel Inhibition