Optimizing Selectivity, Reactivity & Tolerability to Develop Safe, Potent & Clinically Successful Covalent Drugs for Oncology, Immunology & Beyond

2025 marked an exciting phase for covalent drugs, with the field doubling down on de-risked assets and tackling high-value targets in oncology, immunology, and beyond. With MOMA Therapeutics having recently dosed their first patient with a covalent Werner helicase inhibitor, and Novartis partnering with covalent pioneer Matchpoint Therapeutics in a $60 million deal, it was clear that the therapeutic potential of covalency was growing.

The 3rd Covalent Drug Discovery & Development Summit returned as the premier industry forum for experts to accelerate the discovery, translation and development of covalent drugs, driving the next wave of first- and best-in-class therapeutics against previously undruggable targets.

Uniting covalent drug leaders from the likes of Vividion Therapeutics, Pfizer, Revolution Medicines and Frontier Medicines, this three day deep-dive forum will focus on:

• Optimizing warhead selectivity, reactivity and durability to ensure the development of tolerable, potent covalent therapies
• Targeting non-cysteine residues and hard-to-drug proteins including transcription factors to expand the druggable proteome
• Elucidating PK/PD relationships and understanding ADME and target engagement to inform dosing and streamline clinical development
• Innovating advanced screening technologies and lead optimization strategies to rationally triage hits and progress covalent candidates efficiently

Over 3 days, attendees joined 80+ leaders in medicinal chemistry, biochemistry, structural biology and translation to uncover insights on overcoming key challenges in warhead design, lead optimization and preclinical to clinical development, ensuring that your pipeline is de-risked to reach patients in need.