1.2 Drug Discovery Process $ SS $SS $$$-$$$$$$$$$ Target Lead Lead Preclinical Phase Phase Phase Identification Generation Optimisation Development 个 Candidate Drug First in human High Risk,High investment,High reward Drug safety and ->$1 billion,12 years! dosage Development is far more expensive than discovery don't fail late Efficacy 。 Discovery bottlenecks Validated targets Quality Hits subsequent Leads - Optimisation of the Leads Launch Only quality compounds should leave Discovery(前面10%的贡献度决定后面90%的命运) Paul et al,Nature Reviews Drug Discovery,2010,9,203 Candidate Drug First in human Drug safety and dosage Efficacy Launch Phase III Phase II Phase I Target Identification Lead Generation Lead Optimisation Preclinical Development $ $ $$ $$$ $$$$ - $$$$$$$$$$$$$$ Paul et al, Nature Reviews Drug Discovery, 2010, 9, 203 • High Risk, High investment, High reward – >$1 billion, 12 years! • Development is far more expensive than discovery – don’t fail late • Discovery bottlenecks – Validated targets – Quality Hits & subsequent Leads – Optimisation of the Leads • Only quality compounds should leave Discovery (前面10%的贡献度决定后面90%的命运） 1.2 Drug Discovery Process 7