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Optimizing the “Drug-Like” Properties of Leads in Drug Discovery pp 99–130Cite as

Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization

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Part of the book series: Biotechnology: Pharmaceutical Aspects ((PHARMASP,volume IV))

Abstract

At this symposium, as in much of the literature over the last 5-10 years, there has been continued discussion regarding ways to reduce drug candidate attrition during the more costly drug development phases. Much of this discussion has revolved around the recognized importance of selecting drug candidates that have “drug-like” properties, i.e. physical, chemical and structural properties that appear to differentiate nondrug and drug molecules (Kennedy, 1997; Lipinski et al., 2001; Kola and Landis, 2004). As a result, there has been a conscious effort made to move from highly potent ligands toward a molecule that has “drug-like” properties, presumably with a lower risk to attrit during development. In an effort to address these properties sooner, preclinical groups such as pharmaceutics, metabolism and toxicology have been brought into the drug candidate selection process.

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Author information

Authors and Affiliations

  1. Pharmaceutical Sciences, Pfizer Inc., Kalamazoo, MI, 49001, USA

    Michael J. Hageman

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  1. Michael J. Hageman
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Editors and Affiliations

  1. University of Kansas, Lawrence, KS, 66045, USA

    Ronald T. Borchardt

  2. Wyeth Research, Monmouth Junction, NJ, 08852, USA

    Edward H. Kerns

  3. Pfizer, Inc., Kalamazoo, MI, 49007, USA

    Michael J. Hageman

  4. University of North Carolina, Chapel Hill, NC, 27599, USA

    Dhiren R. Thakker

  5. Eli Lilly Research Laboratory, Greenfield, IN, 46285, USA

    James L. Stevens

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© 2006 American Association of Pharmaceutical Scientists

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Hageman, M.J. (2006). Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization. In: Borchardt, R.T., Kerns, E.H., Hageman, M.J., Thakker, D.R., Stevens, J.L. (eds) Optimizing the “Drug-Like” Properties of Leads in Drug Discovery. Biotechnology: Pharmaceutical Aspects, vol IV. Springer, New York, NY. https://doi.org/10.1007/978-0-387-44961-6_5

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