New PDF release: Antitargets: Prediction and Prevention of Drug Side Effects

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

ISBN-10: 3527318216

ISBN-13: 9783527318216

This practice-oriented guide surveys present wisdom at the prediction and prevention of difficult drug reactions relating to off-target job of small molecule medicinal drugs. it really is precise in collating the present ways right into a unmarried resource, and contains numerous hugely instructive case reviews which may be used as directions on how you can increase drug improvement tasks. With its huge part on ADME-related results, this can be key wisdom for each drug developer.

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

Example text

The recent proof of concept of kinase inhibitors shows them as a new class of anticancer drugs [17] or immune system regulators [18]. The BioPrintÒ profile is also enriched with an empirical approach based on knowledge and experience. This experience includes an in-depth understanding of the use of biological data to describe relationships between compound structure, in vitro and in vivo data. Including assays for which links between in vivo and in vitro effects are well documented in the literature was of specific interest.

5]). properties and activity on multiple targets (‘promiscuity’) were discussed. One type of analysis shows that smaller (and thus likely simpler in terms of 3D pharmacophoric patterns) compounds hit more assays. 7). 1 BioPrintÒ – General BioPrintÒ consists of a large database and a set of tools with which both the data and the models generated from the data can be accessed. The database contains structural information, in vivo and in vitro data on most of the marketed pharmaceuticals and a variety of other reference compounds.

Taking together all three clinical phases, it has been observed that most drug candidates fail because of a lack of efficacy. The second major problem is toxicity that leads to the termination of approximately one third of all projects. 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.

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


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