A Bond Worth Forming: The Rise of Targeted Covalent Inhibitors

Prior to 2000, many drugs that formed a covalent bond with targets did so non-selectively, which often led to undesired side effects when compared to non-covalent drugs. This led to the belief that covalent inhibitors were not ideal drug candidates resulting in limited development by the pharmaceutical industry. However, covalent drugs have experienced a remarkable resurgence in the last few years as evidenced by the growing number of approvals by the USFDA, including the 2021 approval of Sotorasib to treat lung cancer that was recently featured on ACS Webinars. In fact, from 2013-2021, eight drugs utilizing targeted covalent inhibitors (TCI) to treat lymphoma, lung cancer, and breast cancer have been approved.

Today, scientists have designed “warheads” with remarkable functionality that exhibit finely tuned reactivity, which only form covalent bonds when positioned at the desired target. Join a panel of experts as they explore the concept of targeted covalent inhibitors, their application in tackling previously unmanageable targets, and gain valuable insights into the covalent inhibitor landscape. Register now to discover current trends related to commonly employed warheads, their target proteins, and therapeutic indications.

This ACS Webinar is co-produced with National Chemsitry Week and CAS, a division of the American Chemical Society.

What You Will Learn

• The theory behind targeted covalent inhibitors and their use against undruggable targets
• Overview of the covalent inhibitor landscape based on data from the CAS Content Collection
• Trends as to the most frequently used warheads, the proteins they target and indications they address

Co-Produced With

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