Oral Macrocyclic Peptides: Merck’s Enlicitide Breakthrough & Novartis Deals

A deep dive into the recent technical milestones in oral macrocyclic peptides, featuring Merck’s Phase 2 results for Enlicitide and the billion-dollar collaboration between Novartis and Unnatural Products.

In this session, we discuss why macrocyclic peptides are becoming the "Goldilocks" modality—combining the tissue penetration of small molecules with the high potency and selectivity of monoclonal antibodies. We break down the medicinal chemistry hurdles, specifically focusing on how macrocyclization and N-methylation solve the "baggage" of poor metabolic stability and permeability.

Key Discussion Points:
- Merck’s Clinical Success: A review of the CORALreef Lipids trial where the oral PCSK9 inhibitor, Enlicitide, achieved antibody-level efficacy with a 57% reduction in LDL.
- The Novartis x Unnatural Products Deal: Analyzing the $1.7 billion collaboration focused on programmable synthetic macrocycle platforms.
- The "Chameleonic" Mechanism: How molecules like Cyclosporine A use intramolecular hydrogen bonding to "mask" polar surfaces for better cell permeability.
- Future Frontiers: The role of AI in drug design, stapled peptides for intracellular targets, and the development of peptide-based degraders.

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Видео Oral Macrocyclic Peptides: Merck’s Enlicitide Breakthrough & Novartis Deals канала BioSpark Group