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Symposium

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: 2019-02-07
Time: 8:45-17:00 Pacific Time
Registration fee: (USD): Regular: $195; Academic: $125; Students & Unemployed: $35
Location: Crowne Plaza, Foster City, CA
Major Sponsor: (1)Correlia Biosystems;(Major Sponsorship - Afternoon still open)
Vendor show vendors registered to date: (20)AIT Bioscience; Alturas Analytics; Averica Discovery Services; BioDuro; BioreclamationIVT; cgenetool; CMIC Inc.; Cytovier LLC; Intertek; MagArray; MedChemExpress; Medpace; MicroConstants; MRIGlobal; Nucleo Life Sciences; Q2 Solutions; Sekisui XenoTech, LLC; Selvita Inc.; Seventh Wave; WuXi AppTec
Registration: http://www.PBSS.org
Registration deadline:2019-02-04  (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


Agenda:

8:45-8:55           Welcome and overview - Richard Zang / Shichang Miao

8:55-9:40           Targeted Covalent Inhibitors for Drug Design - Tom Baillie

9:40-10:25         Kinetic selectivity with lysine-targeted kinase inhibitors - Jack Taunton

10:25-10:35       Major Sponsor's Presentation

10:35-10:50       Break

10:50-11:35       Covalent modification in drug discovery - a chemist's perspective - Joachim Rudolph

11:35-12:20       Safety Considerations for Covalent Inhibitors - Leah Schutt

12:20-13:20       Lunch

13:20-14:05       Preclinical challenges for reversible covalent inhibitors - Dane Karr

14:05-14:50       From bench to beside:  The story of a first-in-class covalent BTK inhibitor ibrutinib - Betty Chang

14:50-15:00       Major Sponsor's Presentation

15:00-15:15       Break

15:15-16:00       Benchmark for Selective Sustained Proteasome Inhibition - Shirin Kapur

16:00-16:45       Development of covalent proteasome inhibitors: DMPK and clinical pharmacology perspectives - Zhengping Wang

16:45-17:15       Panel Discussion


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