One day course in Business& Technology Centre Bessemer Drive, Stevenage, Herts SG1 2DX
The course is based on the material taught in the Physchem/ADME module of UCL School of Pharmacy Drug Discovery MSc course and based on the book:Klara Valko: Physicochemical and Biomimetic Properties in Drug Discovery - Chromatograhic Techniques for lead optimization, Wiley 2014
The course explains the answers to the following questions:
What is lipophilicity and why it is important?What type of lipophilicity is used in drug discovery (octanol/water, chromatographic and biomimetic lipophilicity)?
How can we measure octanol/water partition, chromatographic lipophilicity and biomimetic HPLC properties?
How can we compare various lipophilicity measures by the solvation equation approach?
How does lipophilicity depend on the pH?
How can we use the measured lipophilicity (PFI) in early drug discovery for compound’s ranking and progression?
Structure- lipophilicity relationships
What is volume of distribution, tissue plasma partition and why it is important?
What is unbound volume of distribution and drug efficiency?
Which biomimetic properties of the compounds affect in vivo distribution?
How can we use these properties at early stages of the drug discovery process (case histories)?
How in vivo distribution profiles affect the estimated clinical dose?
