Introduction to Pre-Clinical Drug Discovery

Introduction to Pre-Clinical Drug Discovery will dive into the key aspects of the drug discovery process. Guided by leading experts from industry, you’ll explore the key phases and challenges of drug discovery. You'll delve into core principles of receptor pharmacology, including affinity, potency, selectivity, and efficacy, while gaining hands-on insight into the tools used to triage compounds and advance molecules from hit identification to lead optimisation.

Explore the intricacies of high-throughput screening (HTS) and Design-Make-Test-Analyse (DMTA) workflows, with a focus on assay robustness and reproducibility. The program also covers key concepts in Drug Metabolism and Pharmacokinetics (DMPK), including in vitro and in vivo absorption, distribution, metabolism and excretion (ADME) studies. You will see how this data, coupled with the pharmacology learnings, can be used to estimate likely effective human doses. This, along with an awareness of some of the key challenges and risks, will equip you with a well-rounded understanding of pre-clinical evaluation. The course consists of several seminars, case studies and interactive sessions to discuss and develop key themes introduced in the talks.  

Who Should Attend?

• Post-docs, recent graduates or career-changers – position yourself at the forefront of experts in pharmaceutical drug discovery  
• Laboratory based scientists and early career scientists - build confidence in pre-clinical drug discovery  
• Scientists aspiring to lead drug discovery projects 

Course Benefits

This course delivers essential insights for anyone embarking on a career in drug discovery, making the leap from academia to industry, or aiming to deepen their understanding of pre-clinical drug discovery. You will learn:

• Industry-Relevant Skills: Learn the full pipeline from hit identification to preclinical development, including pharmacology, ADME/DMPK, and lead optimisation. 
• Multidisciplinary Insight: Understand how DMTA screening cycles, data science, and DMPK intersect in drug discovery. Learn how the data and insight from the different disciplines comes together to facilitate project progression. 
• Confidence in Decision-Making: Build the analytical skills needed to evaluate compounds, interpret data, and guide progression decisions. Have a greater appreciation of some of the risks and challenges associated with pre-clinical drug discovery. 
• Networking Opportunities: Connect with industry experts, researchers, and peers 

Course Topics

• Principles and challenges of drug discovery 
• Key cellular, biochemical and biophysical tools  
• HTS and DMTA screening processes, with a focus on assay robustness and reproducibility 
• Screening cascades for hit triaging and validation of target engagement  
• Drug target classes  
• Receptor pharmacology  
• Fundamentals concepts of DMPK in pre-clinical drug discovery 
• In vitro and in vivo ADME assays 
• Key pharmacokinetic parameters  
• Tools to predict human pharmacokinetics and dose 
• Awareness of risks and challenges associated with DMPK  

Instructors

Sinéad Driver, PhD
Sygnature Discovery

With twenty years of industrial experience in biotech and biopharmaceuticals, Sinéad is an expert in the field of drug discovery, small molecule screening, phenotypic screening and target validation.  

Driver is currently Senior Principal Scientist and Section Head at Global CRO Sygnature Discovery working closely with SMEs and biotech companies to develop and progress drug discovery projects from early hit identification in high-throughput screening through to lead optimization and candidate selection. 

Her previous roles include Associate Principal Scientist within the Functional Genomics and High Content Biology groups in AstraZeneca. She is currently an Associate Editor for SLAS Discovery.

 

Philip MacFaul 
Sygnature Discovery

With over twenty years of industrial experience, Philip is an expert in the field of DMPK in pre-clinical drug discovery. Originally trained as a chemist, Philip has built extensive knowledge in both the in vitro and in vivo aspects of DMPK. 

MacFaul is currently Senior Principal Scientist at Sygnature Discovery working closely with project teams to understand and optimize compound properties enabling projects to progress from the hit identification phase through to candidate nomination across numerous therapy areas. 

Philip’s previous roles include positions in DMPK teams at AstraZeneca, Redx Pharma and two CROs. He has published over 50 peer-reviewed articles and co-authored contributions to two book chapters.