Title: “ Discovery and characterization of IRAKIMiDs: degraders targeting both IRAK4 and IMiD substrates for oncology indications.“
By Matthew Weiss
Organized by the Medicinal Chemistry Section
of the Northeastern Section, American Chemical Society (NESACS)
Thursday – March 17th, 2022
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|Biography: Matt earned his BA from Bowdoin College in 1997 before moving to Yale University where he worked on the total synthesis of the welwitindolinone family of alkaloids in the lab of Prof. John Wood. Subsequent to his PhD, Matt conducted an NIH post-doctoral fellowship at the University of California, Irvine with Prof. Larry Overman working on the synthesis of polypyrroloindolines. Matt Spent 13 years at Amgen in Cambridge, MA where he focused primarily in the areas of Oncology and Neuroscience, delivering development candidates within both. In 2018, he moved to Kymera Therapeutics, where he now serves as Head of Medicinal Chemistry. In his time at Kymera, he has been involved with numerous development candidates, a subset of which are currently being evaluated clinically.
|Abstract: Targeted protein degradation (TPD) is a new powerful therapeutic modality which harnesses the body’s natural cellular recycling machinery – the ubiquitin proteasome system (UPS) – to break down or degrade unwanted proteins. This presentation will highlight the discovery and medicinal chemistry optimization of a series of novel orally bioavailable degraders that target the simultaneous degradation of both IRAK4 and IMiD substrates, including Ikaros and Aiolos. These efforts culminated in the identification of KT-413, a heterobifunctional degrader currently being evaluated in Phase I clinical trials. A detailed description of the preclinical pharmacokinetic/pharmacodynamic/efficacy relationships associated with KT-413 will also be described.
Symposium Organizing Committee: Brian Aquila, Mark Ashwell, Scott Edmondson, Dan Elbaum, Jeremy Green, Paul Greenspan, Adrian Hobson, Blaise Lippa, Lisa Marcaurelle, Min Lu, Kap-Sun Yeung, Andrew Scholte, Mala Gopalsamy, Raj (SB) Rajur (Chair)