Drug intelligence / Profile preview

[Aib35]hGLP-1(7-36)NH2

Development stage
Unknown
Lead developer
Ipsen
Modality
Peptides
Administration
Subcutaneous
01

Overview

[Aib35]hGLP-1(7-36)NH2 is a synthetic peptide analogue of human glucagon-like peptide-1 (hGLP-1) featuring a substitution of the glycine at position 35 with alpha-aminoisobutyric acid (Aib). This modification is specifically designed to enhance the peptide's metabolic stability by protecting the C-terminal region from protease cleavage, notably by enzymes such as human plasma kallikrein and plasmin. Structural analysis using circular dichroism (CD) has demonstrated that the Aib35 substitution increases the alpha-helicity of the C-terminus compared to native hGLP-1(7-36)NH2. While this analogue retains high binding affinity and potency at the GLP-1 receptor, it was primarily studied as a research intermediate in the development of taspoglutide (BIM-51077), which incorporates an additional Aib substitution at position 8 to achieve comprehensive resistance to dipeptidyl peptidase-4 (DPP-4) and other enzymes for the treatment of type 2 diabetes.

Other names
Aib35-hGLP-1(7-36)NH2Aib35-substituted human GLP-1(7-36) amide
02

Targets

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