Small Molecule & Intermediates R&D
Orforglipron
Enlicitide Decanoate (MK0616)
Peptide Fragment (Intermediate)
Orforglipron: Selectively activates GLP-1R to stimulate insulin, delay gastric emptying, reduce appetite – controls blood glucose, aids weight management.
Orforglipron Advantages:
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Oral administration boosts convenience/adherence. -
Outperforms metformin/sulfonylureas in HbA1c control
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Significant weight loss. Matches injectable GLP-1s (semaglutide/dulaglutide) in glucose/weight efficacy, with oral option.
Orforglipron poised to be a key player in weight-loss market, next potential blockbuster.
Enlicitide decanoate (MK0616): Developed via Merck's macrocyclic peptide platform. Blocks PCSK9-LDLR binding, increases liver's LDL-C clearance to significantly lower LDL-C levels.
Enlicitide Decanoate Advantages:
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Oral administration enhances convenience/compliance vs. 3 existing PCSK9 inhibitors.
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Outperforms bile acid sequestrants/statins in LDL-C inhibition.
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Matches efficacy of injectables (alirocumab/evolocumab) with more convenient dosing.
Enlicitide decanoate: Projected peak annual sales $5B, a cardiovascular blockbuster. Slated for 2026 launch (pending smooth trials) to compete with PCSK9 inhibitors, filling oral lipid-lowering gaps.
Peptide Fragments: Key intermediates for long peptide synthesis, essential for commercial production of ≥15 amino acid polypeptide drugs.
Ensures long peptide synthesis feasibility:
Direct synthesis of >30 amino acid chains yields <5% (cumulative side reactions); segmented strategy boosts yield to 60%+.
Enables precise control of key modification sites:
Disulphide cyclisation (e.g., insulin) and phosphorylation (e.g., parathyroid hormone) completed at intermediate stage.
High-efficiency impurity interception:
Intermediate purification (HPLC/MS) retains >90% of missing/truncated peptides, reducing final product impurities.
