Gleevec's Development Shows Lead Optimization's Iterative Logic
Imatinib (Gleevec) moved from weak BCR-ABL binding to an orally bioavailable CML drug through sequential modifications: improve binding, fix selectivity, then enable oral absorption.
concept
drug-discoverymedicine
Sources
Coursera: *Lead Optimization* (Introduction to Drug Hunting > Introduction to Drug Hunting, part 3), 3:40
Coursera: *Lead Optimization* (Introduction to Drug Hunting > Introduction to Drug Hunting, part 3), 0:03