Thursday, February 26, 2026 | 11am EST / 4pm GMT (UK) / 5pm CET (EU-Central)
Metabolic instability is a key challenge in developing peptide therapeutics, and factors like rapid clearance and complex, multi-pathway biotransformation can further limit their effectiveness. Understanding and addressing these hurdles can unlock the full potential of peptide drugs, enabling them to reach challenging biological targets, support rational chemical design, and achieve clinical success. This webinar presents an integrated mechanism–analytics–design perspective to tackle these challenges and accelerate peptide drug discovery.
Dr. Lionel Cheruzel will review common metabolic pathways for peptide therapeutics and evaluate the in vitro systems used to characterize instability. He will discuss chemical modifications—including noncanonical amino acid incorporation, cyclization, lipidation, and conjugation—to enhance metabolic stability and pharmacokinetics. Case studies of clinical-stage molecules such as semaglutide, tirzepatide, and MK-0616 (enlicitide) will demonstrate how rational design supports clinical success. featured speaker will highlight key development risks and practical approaches to mitigate them. Case studies will demonstrate how integrating early formulation planning with DMPK insights and milligram-scale API data supports data-driven decisions and accelerates clinical entry within a structured timeline. Attendees will gain insights into how a systematic approach can streamline early development and help promising candidates to reach the clinic faster.
Dr. Mingshe Zhu will focus on analytical challenges that limit mechanistic understanding of peptide metabolism. He will explain why conventional LC–HRMS workflows often fail to capture the full peptide metabolite landscape and introduce a universal LC–HRMS approach for comprehensive profiling across proteolytic and non-proteolytic pathways. Case studies with clinically relevant peptides (e.g., semaglutide, cyclosporine A, tirzepatide) will show how advanced analytics reveals uncover metabolic soft spots and supports structure–metabolism understanding.
What you will learn:
· In vitro systems and experimental strategies to characterize peptide instability
· Medicinal chemistry and conjugation approaches that improve peptide stability and PK
· Limitations of conventional LC–HRMS methods for peptide metabolite profiling
· How an advanced LC–HRMS workflow enables comprehensive biotransformation and soft-spot analysis
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