Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization

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.