Advancement in LC-MS to address DMPK challenges for novel modalities
Novel synthetic drug modalities, like macrocyclic peptides, GLP-1 receptor agonist and proteolysis targeting chimeras (PROTACs®) are rapidly emerging as novel drug modalities for challenging therapeutic targets. Although synthetic in nature, these modalities fall outside Lipinski’s rule of five, thus posing additional ADME challenges, requiring novel approaches for successful lead optimization programs. Recent advancement in Liquid Chromatography High Resolution Mass Spectrometry (LC-HRMS) technology have proven successful in increasing throughput for DMPK assays, as well as confidently identifying metabolic soft spots.
This webinar will showcase a novel approach developed by Merck & Co. on using the Thermo Scientific™ Orbitrap™ Astral™ mass spectrometer to increased throughput of combined stability testing and metabolite identification, enabling sample multiplexing to speed up the development of macrocyclic peptide drugs. Additionally, the benefit of intelligently acquired MSn fragmentation on the Thermo Scientific™ Orbitrap™ Ascend BioPharma Tribrid™ mass spectrometer for confident PROTACs® metabolite soft spot identification edition will be presented.
Key Learning Objectives:
- Recent advancement in liquid chromatography mass spectrometry to address DMPK challenges for compounds beyond Lipinski’s “rule of five”
- Strategies to increase throughput in the development of macrocyclic peptide drugs DMPK assays
- Benefits of multi-stage fragmentation techniques for confident PROTAC® metabolic soft spot identification
Who Should Attend:
- DMPK scientists working on peptide/cyclic peptide, PROTACs® and undruggable targets
- Researchers interested in strategies to improve ADME/DMPK properties of cyclic peptides and PROTACs®
- DMPK scientist interested novel LC-MS approach to speed DMPK assays
Presenter: Congliang Sun, Ph.D. (Sr. Scientist, Merck & Co.)
Presenter: Sven Hackbusch, Ph.D. (Senior Applications Scientist, Thermo Fisher Scientific)
Presenter: Melissa O'Meara (Forensic Science Consultant, C&EN Media Group)
