Key insights from the Summer Course Essentials of Drug Discovery
From 15 to 19 June, Radboud University, in collaboration with HAN University of Applied Sciences, Crossfire Oncology and Pivot Park, organized the Summer Course Essentials of Drug Discovery, an inspiring programme that offered participants a broad and practical insight into the journey from an early scientific idea to a potential therapy. The presentations were rich in content and offered many valuable insights. Below, we highlight some of the key lessons participants took away from the week.
The course started with a broad introduction to drug discovery, giving participants the essential terminology and fundamentals of the field. They learned how drugs interact with biological targets, how chemical starting points can be found and why developing a safe, effective and developable therapy is such a complex challenge. It became clear to them that drug discovery is not a linear process, but a multidisciplinary journey in which biology, chemistry, pharmacology, safety, data, intellectual property and the translation of scientific insights into viable patient treatments all come together.
The programme started with the fundamentals of drug discovery, introducing participants to the terminology, principles and complexity of moving from an early scientific idea towards a potential therapy. It showed that successful drug discovery is not only about finding activity against a biological target, but also about understanding whether a compound can behave safely and predictably in the body, and vice versa. Sessions on ADME, DMPK and toxicology explained how a compound is absorbed, distributed, metabolised and eliminated, how this influences dosing, efficacy and safety, and why risk assessment is essential before a candidate can move further into development.
From there, the programme moved into the diversity of therapeutic approaches used in modern drug discovery. Participants were introduced to biologics, monoclonal antibodies, antibody drug conjugates, peptides, RNA therapeutics, cell therapies and newer strategies such as PROTACs and molecular degraders. These examples showed that each therapeutic approach brings its own scientific and development challenges. These challenges can, for example, include choosing the right target, delivering the treatment effectively, ensuring it can be developed and manufactured, and meeting safety and regulatory requirements. The course then connected these topics to the practical process of building a drug discovery project. Medicinal and computational chemistry showed how early hits can be optimised into stronger candidates by balancing potency, solubility, absorption, metabolic stability and safety. Throughout the programme, the importance of choosing the right target remained a central theme. Sessions on target validation and protein-protein interactions introduced the participants to the importance of understanding biological targets in detail. This included examples such as 14-3-3 protein complexes and molecular glues. Lectures on public data platforms then showed how biological evidence, molecular mechanisms and integrated data can guide target identification.
The strategic side of drug discovery was also addressed through sessions on patents and the investment landscape across different stages of drug development. Participants learned how patents work, what requirements apply, how the granting process is structured and how patent information can be used to support development decisions. The programme concluded with a concrete example from SARS CoV 2 antiviral research, focusing on the development of potent dual mode inhibitors targeting SARS CoV 2 Mpro and cathepsin. This final scientific case brought together many of the themes from the week.
To bring all the learning together, participants worked in teams on their own drug development proposal. Using the knowledge gained throughout the course, they developed and presented a proposal that combined a scientific rationale, a chosen treatment approach, development considerations, potential risks and ways to mitigate them. This final assignment helped participants bring the different sessions together and gain a broader view of how a drug discovery project takes shape.
We look back on the Summer Course at Pivot Park with great appreciation and enthusiasm. The week showed how broad, complex and inspiring drug discovery is, and how many different areas of expertise are needed to bring new therapeutic ideas to patients. We especially appreciate that experts from both the field and education took the time to share their knowledge, experience and insights with the participants and the Pivot Park community. Their contributions made the programme not only highly informative, but also engaging, practical and inspiring!
With thanks to Rutger Folmer, Aloys Sesink, Mike Ruth, Hans van Eenennaam, Sander van Berkel, Iwan de Esch, Christian Ottmann, Joost Uitdehaag, Leendert van den Bos, Sander Nabuurs, David Lutje Hulsik, Laura Heitman, Jan Spanholtz, Roland Brock, Henk Jan van den Ham, Jerre Edens, Miriam Porzberg, Pedro Hermkens, Dennis Löwik and Floris Rutjes.
