PHAR 505 Lecture Notes - Lecture 8: Diarrhea, Lead Compound, Verapamil

• School: McGill University
• Department: Pharmacology and Therapeutics
• Course: PHAR 505
• Professor: Jean Francois Trempe

Document Summary

What makes a good drug: desirable drug properties. **required reading: kerns, drug-like properties: concepts, structure design and methods (2006) chapters 4-5. To be clear, sbdd is not per se linked to drug-like properties. Structures are rarely used in adme optimisation with a few exceptions: like optimisation of transporters or protein binding. However, the optimisation of a lead compound through sbdd cannot be done without working in parallel to evaluate the adme and ensuring that the molecules have adequate properties. Schematic of some of the barriers encountered by drugs between dosing and the therapeutic target. Examples of pharmaceutical profiling assays that provide info about these barriers are shown in red. Of course the target can be elsewhere along this path, like in the intestine or in the blood. Permeability is the velocity of molecule passage through a membrane barrier. It is a determinant of intestinal absorption and oral bioavailability.