The DMPK Challenges and Strategies for Developing Protein Degrader Compounds
Recorded: July 2023
This webinar showed challenges and complexities of working with protein degraders and how these can be overcome to allow DMPK data to be incorporated in medicinal chemistry design.
Agenda
- What are the challenges in assessing DMPK properties for protein degraders?
- The characteristics of protein degraders and the challenges in assessing their DMPK properties
- How do we assess ADME properties for protein degraders?
- in vitro methods to assess ADME properties for protein degraders in discovery projects – theoretical and practical aspects of the methods
- How do we use DMPK data to guide structure optimization for protein degraders?
- General principals of using DMPK data to optimize structure for protein degraders to improve their DMPK properties
Moderated by:
Chris Bode, Ph.D. – VP of Scientific Affairs at Pharmaron
Speakers
Andy Pike, Ph.D. – Senior DMPK Discovery and Development Lead at AstraZeneca
Andy Pike is a DMPK specialist with 30 years of experience in drug discovery with the pharmaceutical industry. Having previously worked for Merck Sharp & Dohme, Astex and Pfizer, currently Andy is a DMPK project lead within AstraZeneca Oncology R&D. Andy has worked across a range of therapeutic areas, target classes and drug modalities and in recent years has begun working with heterobifunctional degraders, applying his experience to understanding the specific ADME challenges they present compared to traditional small molecule drugs.
Yu Wang, Ph.D. – Senior Director, in vitro ADME at Pharmaron
Dr. Wang joined Pharmaron in 2012 and is the senior director of in vitro ADME department in Beijing. He worked on the CYP induction and cell-based transporter studies in his first 3 years of career. He has been leading an experienced team since 2015 to support drug discovery projects for biotech and big pharma clients across the world. He serves as a study director and scientific leader to oversee various in vitro ADME and in vitro toxicity assays. He also led the capability development by establishing high throughput ADME screening platform and in vitro liver tox screening platform at Pharmaron. Before joining Pharmaron, he obtained his Ph.D. in pharmacology from China Agricultural University, and B.Sc. in biology from Beijing Normal University.
Ben Rahemtulla – Associate Principal Scientist, Drug Discovery at Pharmaron
Ben joined the Drug Discovery group at Pharmaron in 2019 and since then has been involved in as a synthetic and medicinal chemist on numerous projects on small-molecules and targeted protein degraders. Prior to this, he worked as a Postdoctoral Researcher in Medicinal Chemistry at Theravance Biopharma, San Francisco, working on exploratory kinase projects, and targeted protein degraders. He received both his DPhil and MChem from the University of Oxford and his DPhil research was carried out under the supervision of Professor Martin Smith in the field of asymmetric organocatalysis, sponsored by GSK through a CASE award. From his time at Pharmaron he is co-author/co-inventor on 2 peer-reviewed publications and 4 patents.