October 21, 2004, 1^st Annual PhysChem Symposium: Early ADME and Medicinal Chemistry

Improving Solubility in Lead Selection and Compound Optimization

Bernard Faller (Novartis Institutes for BioMedical Research)

Abstract

Solubility becomes an increasing issue in drug development as high-throughput screening techniques as well as chemical optimization of binding affinity tend to shift compounds towards more lipophilic and therefore less soluble substances. Solubility plays an essential role in drug disposition as passive drug transport across a biological membrane, the main pathway for drug absorption, is the combined product of both permeability and solubility.

The presentation will:

• Explore the importance of solubility in lead optimization
• Review strategies to improve solubility
• Review strengths and weaknesses of currently available techniques to measure/predict solubility

Download the presentation in Adobe Acrobat format (624 Kb PDF file).