And Development [portable] - Pharmacology In Drug Discovery

Pharmacology provides the biomarkers that measure target engagement. For example, in cancer drug development, measuring phosphorylated AKT in a tumor biopsy proves that a novel PI3K inhibitor is hitting its target. Without such pharmacology-driven evidence, a failed trial might be due to poor target engagement rather than a bad therapeutic concept.

How the drug and its metabolites are eliminated from the body, typically via the kidneys or bile. Half-life ( t1/2t sub 1 / 2 end-sub ), renal clearance rate, total systemic clearance ( Pharmacodynamics: Receptor Kinetics and Signal Transduction pharmacology in drug discovery and development

By Phase 3, the dose is set. But pharmacology's job isn't over. The large-scale trials are powered by the dose selected from Phase 2 pharmacology data. Furthermore, pharmacology provides the evidence for the drug's label: How the drug and its metabolites are eliminated

PD tells you the dose needed; PK tells you if you can deliver it. The large-scale trials are powered by the dose

The greatest challenge in the field is the "translation gap." Human biology is vastly more complex than animal models or cell cultures. A drug that works beautifully in a mouse model of Alzheimer’s may fail completely in a human patient.