Introduction and Objective: RDSY1801 is a novel GLP-1 peptide composed of a single mutation in Thr7→Pro and activates GLP-1R. This is the first-in human study of oral RDSY1801 capsules, designed to investigate its pharmacokinetics and safety in healthy adults.Methods: Total 54 healthy volunteers participated in the single escalation dose study. Participants were randomized into six groups to receive a single oral dose of RDSY1801 of 4, 10, 40, 80, 120 and 200 mg, respectively. Each dose group contained either 6 or 8 participants, with total 12 participants receiving placebo. Pharmacokinetic parameters were assessed within the dosage groups of 4, 40, 120 and 200mg.Results: Following oral administration of 4, 40, 120 and 200 mg doses of RDSY1801, pharmacokinetic studies showed that Tmax appeared consistently at approximately 3 hours for all dose groups, with Cmax of 2.56±0.29, 34.60±6.94, 137.25±18.78, and 242.00±25.52 ng/ml, respectively. Within the dose range of 4 to 200 mg, AUC increased in a dose-dependent manner, and T1/2 was about 0.5 hour. No deaths or SAEs occurred in this study. TEAEs were mild to moderate and transient. Specifically, regarding gastrointestinal adverse events, only one case of diarrhea (1/8) occurred in the dose group of 120 mg, and another case of nausea (1/8) occurred in the dose group of 200 mg. Unlike other GLP-1RAs, no increase in heart rates was observed in all participants treated with RDSY1801.Conclusion: RDSY1801 achieves effective plasma concentrations when administered orally. It was well tolerated in healthy volunteers, and no serious adverse events have been reported. Its clinical efficacies will be further studied.
W. Jia: None. F. Gao: None. J. Zhou: None. J. Liu: Advisory Panel; Current; Landing Laboratories.
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