Discovery pharmaceutics--challenges and opportunities.
Most pharmaceutical companies are now evaluating compounds for druglike properties early in the discovery process. The data generated at these early stages allow upfront identification of potential development challenges and thus selection of the best candidates for lead nomination. Most often, lead nomination candidates are selected based on pharmacological and toxicological data. However, many drugs in development suffer from poor biopharmaceutical properties due to suboptimal physiochemical parameters. The poor biopharmaceutical properties often lead to extended timelines and a higher cost of developing the compounds. To avoid these problems and choose the best compounds from a biopharmaceutical perspective, physicochemical parameters such as solubility, lipophilicity, and stability need to be evaluated as early as possible. Furthermore, the preformulation approaches used to evaluate the compounds for their pharmacokinetic and toxicological properties need to be optimized. This minireview summarizes some of the parameters and approaches that can be used to evaluate compounds in the early stages of drug discovery.
Chen
Xue-Qing
XQ
Discovery Pharmaceutics, Preclinical Candidate Optimization, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
Antman
Melissa D
MD
Gesenberg
Christoph
C
Gudmundsson
Olafur S
OS
D001702:Biopharmaceutics / Q000639:trends*; D004345:Drug Industry / Q000639:trends; D004358:Drug Therapy; D005544:Forecasting; D008055:Lipids; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis* / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties
D008055:Lipids; D004364:Pharmaceutical Preparations