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Non‐clinical and first‐in‐human characterization of ECC5004 / AZD5004 , a novel once‐daily, oral small‐molecule GLP ‐1 receptor agonist
Early testing of ECC5004/AZD5004, a new once-a-day pill that activates the GLP-1 receptor
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Abstract
ECC5004 demonstrated an IC of 2.4 nM for binding to the human GLP-1 receptor.
- ECC5004 augmented signaling without causing receptor internalization or recruitment of β-arrestin-2.
- Increased glucose-stimulated insulin secretion was observed in both human cell lines and non-human primates.
- Body weight changes were noted in a 9-month toxicity study in non-human primates.
- The first-in-human study indicated that ECC5004 was well tolerated with no serious adverse events.
- Dose-dependent reductions in glucose and body weight were recorded at doses of 25 mg and above.
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Key numbers
2.4 nM
IC for GLP-1R Binding
Potency of ECC5004 binding to the human .
36.5%
Body Weight Change in NHPs
Decrease in body weight gain at 50 mg/kg/day compared to control in male NHPs.
48 of 52
Participants Completing FIH Study
Completion rate in the first-in-human study of ECC5004.