Presentation Outline:

- Assessing pharmacokinetic properties in drug discovery – what we look for and why
- Synthetic peroxide antimalarial drug discovery project: case study to illustrate:
a. How solubility, metabolism and clearance are optimized in drug discovery
b. How optimized pharmacokinetic properties can lead to better efficacy.

Drug Discovery and Development:

- Compounds fail in clinical development due to:
a. Lack of efficacy
b. Side effects / toxicity
c. Poor pharmacokinetic properties (Low BA, Short T1/2, high CL) **
d. Marketing issues.
- Clinical failures are expensive, both in time and dollars.
- Identify problems early, have opportunity to fix problem with a new compound.
- Progress only the best compounds into clinical development.
- Saves time and money
- Improves IP position and licensing opportunities (long term potential for success of
the compound is improved.

Half Life
Volume of Distribution

Clearance

Vo

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