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Covalent Inhibitor Drug Discovery & Development: Biology, Chemistry, PK, Safety and Case Studies (Jointly with Bay Area PKPD Network)

Speakers: Tom Baillie (Univ Washington), Jack Taunton (UCSF), Joachim Rudolph (Genentech), Dane Karr (Nurix), Zhengping Wang (Revolution Medicine), Shirin Kapur (ex-Onyx), Leah Schutt- (Genentech), Betty Chang (ex-Pharmacyclics)
Organizers: Xu (Richard) Zang, PhD (Genentech)
Date: 2/7/2019
Time: 8:45-17:00
Registration fee (USD): Regular: $195; Academic: $125; Students & Unemployed: $35;
Location: Crowne Plaza, Foster City, CA
Major Sponsor:
Vendor show vendors registered to date: (4)BioreclamationIVT; MedChemExpress; MicroConstants; Seventh Wave
Registration deadline:2/7/2019  (it will close sooner if the seating cap is reached)

About the Topic

In recent years, there has been a renewed interest in drug development of covalent inhibitors.  Several of these inhibitors have been approved by the FDA and EMA and more covalent inhibitors are in early and late stage development.  Covalent inhibitors can have superior affinity towards target proteins compared to their non-covalent counterparts, potentially resulting in improved therapeutic benefit.  This symposium will cover a wide range topics pertaining to covalent inhibitors discovery and development

Key Topics:

  • Targeted Covalent Inhibitors for Drug Design – Tom Baillie (UW)
  • Kinetic selectivity with lysine-targeted kinase inhibitors – Jack Taunton (UCSF)
  • Covalent modification in drug discovery - a chemist's perspective – Joachim Rudolph (Genentech)
  • Preclinical challenges for reversible covalent inhibitors – Dane Karr (Principia)
  • Development of covalent proteosome inhibitors: DMPK and clinical pharmacology perspectives – Zhengping Wang (Revolution Medicine)
  • Benchmark for Selective Sustained Proteasome Inhibition – Shirin Kapur (Cortexyme)
  • Safety Considerations for Covalent Inhibitors - Leah Schutt- (Genentech)
  • From bench to bedside: The story of a first-in-class covalent BTK inhibitor ibrutinib– Betty Chang

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