Drug Hunting: The Science of Making New Medicines Specialisation

Introduction to Drug Hunting:

A summary of the different stages of preclinical drug discovery and clinical trials. Includes: drugs for unmet medical needs and what are the key scientific questions; in vitro pharmacology; pharmacokinetics; lead selection; in vivo pharmacology; preclinical PK/PD; lead optimisation; preclinical safety, FDA clinical trial strategies and competitive intelligence.

Targets, Assays & Screening:

Target Based Drug Discovery, Phenotypic Drug Discovery, Factors in Assay Design, Molecular Space, Compound Libraries, HTS (Primary Assay, Orthogonal Assays, Counterscreens and PAINS), Fragment-Based Drug Discovery, In Silico Screening, Hit Validation, Future Direction for Screening

Pharmacokinetics:

Routes of Administration; PK of Biologics; Phase I & Phase II Metabolism; Metabolic Stability & Clearance; Membranes; Permeability & Transporters; Plasma Protein Binding; Drug-Drug Interactions; PK/PD Relationships; Anticipated Human Dose.

Preclinical Safety

Toxicity; Preclinical Safety Testing; In Vivo Toxicity and Safety Studies; Basics of Safety Risk Assessment; Therapeutic Index and Quantifying Safety; Preclinical studies supporting human clinical trials; Safety considerations for selecting a human dose; Toxicology in Phase II and Phase lII

Lead Selection and Optimisation

Pharmacophores and Lead Optimisation; Assays for Guiding Lead Optimisation; Hit Criteria and Characterisation; Composite Parameters in Discover; SAR of a Compound Series; Optimisation of ADME Properties; In Vivo Pharmacokinetics; Biomarkers; In vivo Pharmacology and Safety.

Pre-formulation

Physicochemical Properties; Routes of Administration; Drug Products; Classification; Crystallisation; Drug Substance Stability; Drug Product Stability; Impurities; Clinical Formulation Development; Biologics