Topics

The conference will be centered around 8 topics. Some slots will be available for an oral communication to be selected out of the submitted abstracts.

Session 1 : Recent Developments in Synthetic Methodologies and their Impact

Session Chair : Dr Fabrice GALLOU, Novartis Pharma, Switzerland

Within the last decade, a variety of synthetic methodologies and technologies have significantly impacted the way to conduct chemistry. Most of these approaches, such bio- or chemo-catalysis, flow chemistry, photo-catalysis, chemistry in water, have been part of the toolbox of the chemists in the past. Recent developments have indeed made them reached high technology readiness, thus making them amenable for profound impact in almost all aspects of chemistry.

Session 2 : From Underground to Mainstream: Neglected and Novel, Emerging Functional Groups for Drug Discovery

Session Chair : Dr Ulrich LÜCKING, FoRx Therapeutics, Switzerland

Extension of the medicinal chemistry toolbox is in the vital interest of drug designers who are confronted with the task of finding molecular solutions for an ever-increasing biological target space in a timely manner. However, in the daily routine, medicinal chemists often tend to stick to the functional groups and structural elements they know and love.

This session intends to provide inspiration for the utilization of non-mainstream moieties in drug discovery to overcome optimization hurdles.

Session 3 : Human Dose Prediction in the Discovery Space

Session Chair : Dr Holger FISCHER, F. Hoffmann-La Roche, Switzerland

Human dose prediction for small molecules is mainly based on physiologically-based pharmacokinetic modeling (PBPK) to ensure the right exposure for a safe and effective treatment. This is typically done in late drug discovery before entry into human trials, but in recent years, simplified versions of human dose prediction are used for ranking lead optimization of compounds to judge the feasibility of a chemical series to reach the expected therapeutic dose, based on a limited number of molecular properties. In some cases, this is complemented with early PKPD modeling strategies to provide insights to the therapeutic window. The focus of the session will provide an overview and discussion on the benefits and risks of pre clinically used human dose predictions.

Session 4 : Radical Intermediates in Complex Molecule Synthesis

Session Chair : Prof. Nina HARTRAMPF, University of Zurich, Switzerland

Reactions proceeding through radical intermediates, such as electrochemical and photochemical reactions, are becoming increasingly popular in organic chemistry. New synthetic methods have significantly improved the selectivity and efficiency of these reactions, making them valuable tools for the synthesis of natural products and other complex, highly functionalized molecules. This session intends to showcase state-of-the-art methods that enable novel disconnections in target molecule synthesis that were unattainable with classic methods.

Session 5 : Antiviral Drug Discovery

Session Chair : Dr Michael SOFIA, Arbutus Biopharma, United States

Viral diseases have had a profound impact on human health. Since the beginning of the 21^st century the World Health Organization has declared fourteen infectious disease related public health emergencies eight of which are viral in origin and include SARS, Influenza H1N1, Ebola, MERS, Zika, SARS-CoV-2 and Monkeypox. In addition, chronic viral diseases such as HIV, HCV, HBV, HSV and HPV continue to burden both the developed and underdeveloped regions of the world. To compound the situation, there is a growing concern around the emergence of resistant variants of known viral pathogens and the potential for the emergence of new viruses. These heightened concerns are fueled by an increase in population density and urbanization, increases in global travel and migration and the impact of climate change.

To counter the continual threat of viral diseases, it is imperative that focus be maintained not only on the development of vaccines to control the emergence of viral diseases within a population but also on the development of novel antiviral drugs to combat these infections once they take hold within a population. The success of antiviral drugs in combating global public health challenges can be seen in the treatments developed to combat HIV infection and the cures developed for HCV. To achieve such success, required that all available tools in the drug discovery toolbox including genomics, structural biology, computational chemistry, high throughput screening and modern chemical synthetic methods be leveraged. This session on Antiviral Drug Discovery will highlight progress in the discovery of novel agents to treat viral infections, and the strategies and methods used to deliver these agents to the clinic.

Session 6 : Latest Advances and Approaches in Bioconjugation Drug Discovery

Session Chair : Dr Natalia CHERNYAK, Merck, Sharp & Dohme, United States

Safety and efficacy constitute the major criteria governing regulatory approval of any new drug. Bioconjugates, where a proven therapeutic agent connected to a targeting ligand, represent a powerful approach to safer medicines. In the last decade the field of bioconjugates has witnessed major breakthroughs in selective delivery of small molecules, radiotherapeutics, as well as complex biomolecules such as oligonucleotides and protein degraders. Notable achievements in the field are FDA approvals of 14 antibody drug conjugates with many more entering clinical trials, as well as success of much smaller formats with approvals of peptide drug conjugates, Lutatera, Pepaxto, and Pluvicto. With this excitement we would like to invite you to hear on recent developments in the field of bioconjugates for drug delivery.

Session 7 : Drug Discovery Tales 1 & 2

Session Chair : Dr Scott WOLKENBERG, Janssen Pharmaceutical Companies of Johnson & Johnson, United States

This session will be put together by selected proposals out of the abstract submissions.

Session 8 : Cryo-EM: Applications for Structure-Based Drug Discovery

Session Chair : Dr Katharina DÜRR, OMass Therapeutics, United Kingdom

In recent years, cryo-electron microscopy (cryo-EM) has become a key technology for the structure-based design of drugs targeting disease-relevant macromolecules. This has been particularly transformative for drug targets which are not suitable for other structural methods (X-ray crystallography or NMR), such as integral membrane proteins. Advances in detector technology and image processing software have made this technique now broadly applicable for routine high-resolution structure determination of GPCR/G protein complexes, ion channels, solute carriers and other challenging targets.

In this session, speakers from academia and industry will present examples of how cryo-EM has contributed to small molecule design and how it can be even implemented for high-throughput approaches such as fragment-based screening pipelines.