Hit and Lead Profiling: Identification and Optimization of Drug-like Molecules

PART 1: Introduction: The one Airplane that Flies -
Selection of the Right one Molecule for Clinical use.
1 Process logistics, testing strategies and automation aspects
2 Prediction of drug-likeness and its integration
3 Integrative risk assessment
PART 2: ADME Profiling: What is Drug Likeness?
4 Solubility and Aggregation
5 In silico tools and in vitro HTS approaches to determine lipophilicity during the drug discovery process
6 Membrane permeability - measurement and prediction in drug discovery
7 Drug Metabolism and Reactive Metabolites
8 Drug-Drug Interactions: Screening for liability and assessment of risk
9 Plasma Protein Binding and Volume of Distribution: Determination, Prediction and Use in Early Drug Discovery
10 Putting it all together
PART 3: Safety Profiling: What is Considered Safe in the Clinic?
11 Genetic Toxicity: in vitro Approaches for Hit and Lead Profiling
12 In vitro Safety Pharmacology Profiling: An important tool to decrease attrition
13 Knowledge-based and Computational Approaches to in vitro Safety Pharmacology
PART 4: Organ Specific Toxicity
14 Discovery Toxicology Screening: Predictive, In Vitro Cytotoxicity
15 Predicting Drug-Induced Hepatotoxicity: In Vitro, In Silico, and In Vivo Approaches
16 Should cardiosafety be ruled by hERG inhibition? Early testing scenarios and integrated risk assessment
17 Haematotoxicity: in vitro and ex vivo compound profiling
18 Profiling Adverse Immune Effects
19 In Vitro Phototoxicity Testing: A Procedure Involving Multiple Endpoints