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Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
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Author Spotlight: Cost-Effective Transcriptomic Drug Screening - Unlocking New Targets
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Using transcriptomics to guide lead optimization in drug discovery projects: Lessons learned from the QSTAR project.

Bie Verbist1, Günter Klambauer2, Liesbet Vervoort3

  • 1Department of Mathematical Modeling, Statistics and Bioinformatics, Ghent University, Coupure Links 653, B-9000 Gent, Belgium.

Drug Discovery Today
|January 14, 2015
PubMed
Summary

Gene expression profiling can identify potential safety issues early in drug development, improving R&D efficiency. This method helps de-risk drug candidates, leading to better decision-making and fewer late-stage failures.

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Area of Science:

  • Pharmacology
  • Genomics
  • Drug Discovery

Background:

  • Pharmaceutical R&D efficiency is declining, with high rates of late-stage drug candidate failure.
  • Safety issues and unforeseen side-effects are primary reasons for these failures, increasing development costs.

Purpose of the Study:

  • To evaluate the utility of gene expression data in early-phase drug development.
  • To determine if gene expression profiling can de-risk drug candidates by detecting biological effects.

Main Methods:

  • Analysis of gene expression data across eight drug discovery projects.
  • Assessment of compound effects across diverse disease areas, targets, and scaffolds.

Main Results:

  • Gene expression data proved informative in supporting go/no-go decisions for drug candidates.
  • Gene expression profiling successfully detected adverse effects of compounds in early development.

Conclusions:

  • Gene expression profiling is a valuable tool for early-stage drug discovery decision-making.
  • Utilizing gene expression data can mitigate risks associated with drug development and improve R&D efficiency.