Lead Optimisation

• Taking a lead and converting it into a candidate for pre-clinical evaluation
• The majority of the time is spent solving ADME/T issues
• Separation of pharmacokinetic and pharmacodynamic duration of action can offer unexpected benefits
• Keep an eye on physicochemical properties as you add to the lead molecule
• There are no selective compounds, learn how to put off-target activity/toxicity into context
• Keep an eye on the preclinical requirements
• The best way to gain experience is on the job or reading Case Histories