Drug intelligence / Profile preview

exendin 9-39 + sitagliptin

Development stage
Preclinical
Lead developer
Eiger BioPharmaceuticals
Modality
Peptides, Small Molecules
Administration
Intravenous, Oral
01

Overview

Exendin 9-39 + sitagliptin is an experimental combination of two agents with distinct but related mechanisms in the incretin pathway. Exendin (9-39) is a peptide fragment that acts as a selective antagonist of the glucagon-like peptide 1 receptor (GLP-1R), thereby blocking GLP-1-mediated effects such as insulin secretion and glucose lowering[3][6][10]. Sitagliptin is a small molecule dipeptidyl peptidase 4 (DPP-4) inhibitor that increases endogenous levels of active incretins, including GLP-1 and GIP, by preventing their degradation[8]. The combination has been used in research to dissect the physiological roles of endogenous GLP-1 signaling and DPP-4 inhibition in glucose metabolism, insulin secretion, cholesterol efflux, and cardiovascular function[2][6][7]. This combination is not approved for clinical use but serves as a pharmacological tool to study incretin biology.

Other names
exendin-(9–39) + sitagliptinEx-9 + sitagliptin
02

Targets

GLP1R (GLP-1R)DPP-4 (Dipeptidyl Peptidase-IV)

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