Product Description
A novel small molecule GLP-1R agonist (GS-4571) which stimulated a potent cAMP response in pancreatic beta-cells (EndoC-BH1) and selective agonism against human and monkey GLP-1R versus other class B GPCRs. In an intraperitoneal glucose tolerance test (IPGTT) it demonstrated improved glucose tolerance in humanized GLP-1R mice. Further studies, in obese cynomolgus monkeys, GS-4571 demonstrated similar improvements in glucose tolerance after a single dose treatment. Once-daily oral administration of GS-4571 in obese diabetic cynomolgus monkeys not only showed improved glycemic control but also showed a reduction in energy intake which led to an increase in weight loss over 36 days. Together these data support the continued development of GS-4571 into the clinic as a novel orally bioavailable GLP-1R small molecule agonist. (Sourced from: https://diabetesjournals.org/diabetes/article/73/Supplement_1/1625-P/155028/1625-P-GS-4571-an-Oral-Small-Molecule-GLP-1R)
Mechanisms of Action: GLP-1 Agonist
Novel Mechanism: No
Modality: Small Molecule
Route of Administration: Oral
FDA Designation: None *
Approval Status: Not Approved
Approved Countries: None
Approved Indications: None
Known Adverse Events: None
Company: Gilead Sciences
Company Location: FOSTER CITY CA 94404
Company CEO: Daniel P. O’Day
Additonal Commercial Interests: None
Clinical Description
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