| Day One - Introduction to ADME |
| ADME Made Simple A colourful voyage through the digestive system outlining the elements of ADMET, absorption, permeability, pgp, phase 1&2, enteropatic cycling, toxicity, renal excretion, glomerular filtration, oral absorption, first pass. |
| Round Table Discussion Route of administration. Detection of pharmacologically active metabolites in drug discovery. Ames test. |
| Pharmacokinetics - Definitions and Assays A useful, easy to follow yet comprehensive guide to elimination (half-life, extraction ratio, clearance, AUC) Distribution (volume of distribution, half-life) absorption (bioavailablilty, iv, po), and overview of corresponding assays methodologies. |
| Making the correct Diagnosis - ADME and the Medicinal Chemist A step by step guide to correctly diagnosing the perennial issues in lead optimization for drug design. |
| Workshop: ADMET Issues - Solutions that Work Making the diagnosis and abstracting working solutions to recurrent ADME issues from a range of key medicinal chemistry papers. This team exercise provides a range of quality ideas that have been successfully applied in topical research projects taken from a broad spectrum of pharmaceutical companies. |
| Roundup Session and Outstanding Questions. |
| Day Two - hERG – La Bête Noire |
| hERG – An Introduction hERG and IKr, ECG, TDP, QTC. The hERG channel structure, in silico models, site directed mutagenicty studies. Assay methodologies. Regulatory issues, current issues. |
| The hERG 4 Commandments – Designing out hERG Activity An up to date overview of the literature and summary of key approaches employed by the major players in the field. Lecture illustrated with numerous worked examples on designing out hERG activity. |
| Round up Session |
| WORKSHOP - Strategies for Diluting out hERG A productive group session aimed at working through real life projects designing out hERG activity. The ‘hERG 4 Commandments’ will be evaluated in parallel and discussed. |
| Round up Session: Conclusions and Recommendations |