This three-day course is specifically designed for drug discovery scientists in the pharmaceutical and biotechnology industries, as well as contract research organizations (CROs) engaged in lead optimization and preclinical development of drug candidates.  This includes medicinal chemists and scientists involved in the synthesis, testing, and ADME-Tox profiling of drug candidates.  In addition, those responsible for the direction of multidisciplinary teams and academic researchers involved in drug discovery projects will benefit from this course.

Participants should have some knowledge of the drug discovery process including hit identification, lead selection, and preclinical development activities.  Non-clinical and clinical scientists, managers, and project team leaders will gain a detailed understanding of the relationships between molecular structure and drug-likeness, and how systemic efficacy and safety can be controlled through structure modification.



Learning Objectives

Upon completing this course, participants will have an in-depth knowledge of the physical properties of drugs and how they relate to their absorption, distribution, metabolism, and excretion (ADME) and toxicity profiles. Strategies to optimize each of these parameters via structure modification will be covered in the context of reducing attrition of drug candidates early in the drug discovery process. In addition, attendees will have exposure to the various in vitro and in vivo methods to assess drug-like properties.



Course Description

The content of this course will assist pharmaceutical, biotechnology, and CRO researchers and managers in understanding the challenges associated with developing systemically active and safe drug candidates. Emphasis is placed on the design of molecules possessing those structural characteristics responsible for optimal drug-like properties. Each of the ADME requirements will be addressed in terms of physical properties (e.g. lipophilicity, polarity, ionization), and strategies to assess and optimize each parameter will be discussed. Specific methods, protocols, and applications as well as the latest developments in the field will be highlighted. 

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