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Drug intelligence / Profile preview
Org 249305-1
- Development stage
- Preclinical
- Lead developer
- Merck
- Modality
- Peptides
- Administration
- Subcutaneous
01
Overview
Org 249305-1 is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist developed for the treatment of type 2 diabetes. It is synthesized using CarboCarrier technology, which conjugates an antithrombin III (ATIII)-binding sulfated pentasaccharide (derived from idraparinux) to the Lys37 residue of a D-Ala8-GLP-1 amide analog via a tetraethylene glycol (TEG) linker. This conjugation allows the peptide to bind to plasma ATIII, significantly extending its circulating half-life and providing resistance to dipeptidyl peptidase-4 (DPP-IV) degradation. Org 249305-1 stimulates glucose-dependent insulin secretion, improves glucose tolerance, and reduces HbA1c levels, making it compatible with once-weekly subcutaneous dosing.
- Other names
- CarboCarrier D-Ala8GLP-1D-Ala8-GLP-1-pentasaccharide conjugateD-Ala-8-GLP-1-pentasaccharide conjugateD-Ala 8-GLP-1-pentasaccharide conjugateD-Ala8GLP-1-pentasaccharide conjugateD-Ala-8GLP-1-pentasaccharide conjugateD-Ala 8GLP-1-pentasaccharide conjugate
02
Targets
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