Download Antitargets: Prediction and Prevention of Drug Side Effects by Roy J. Vaz, Thomas Klabunde, Raimund Mannhold, Hugo Kubinyi, PDF

By Roy J. Vaz, Thomas Klabunde, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers

This practice-oriented guide surveys present wisdom at the prediction and prevention of inauspicious drug reactions relating to off-target task of small molecule medications. it's targeted in collating the present techniques right into a unmarried resource, and comprises numerous hugely instructive case stories which may be used as directions on the right way to enhance drug improvement initiatives. With its huge part on ADME-related results, this can be key wisdom for each drug developer.

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Extra info for Antitargets: Prediction and Prevention of Drug Side Effects

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2007) Simulation and prediction of in vivo drug metabolism in human populations from in vitro data. Nature Reviews. Drug Discovery, 6, 140–148. , Laggner, C. and Langer, T. (2006) Highthroughput structure-based pharmacophore modelling as a basis for successful parallel virtual screening. Journal of Computer-Aided Molecular Design, 20, 703–715. D. and Langer, T. (2007) Parallel Screening and Activity Profiling with HIV Protease Inhibitor Pharmacophore Models. Journal of Chemical Information and Modeling, 47 (2), 563–571.

Especially cardiovascular toxicity and hepatotoxicity played a crucial role in the decisions for withdrawing drugs from the market. 1 Drugs withdrawn from the market from 1992 to 2006. 3 Reasons for the market withdrawal of the investigated drugs (n ¼ 17, left). Toxicity profile of the withdrawn drugs (right). currently no reliable test models for such toxicity problems available, for otherwise these drugs would never have entered the market at all. 2. As these drugs remain available on the Western market, they are not included in our statistics.

5. 4 Reasons for project termination in clinical phases I (left), II (middle) and III (right) from 1992 to 2002. 5 General reasons (left) and toxicity issues (right) leading to project termination in clinical phases I–III from 1992 to 2002. 5 Strategies for Avoiding Failure The recent example of torcetrapib, where the world’s largest drug company lost its potentially biggest drug, underlines the continued need for strategies to avoid failure during drug development. Despite the increased efforts in synthesis and testing via combinatorial synthesis and high-throughput screening (HTS) methods, the number of new drugs being approved is slowly declining and companies’ drug pipelines are drying up.

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