Pharmacokinetic and dose‐finding studies on efpeglenatide in patients with type 2 diabetes
Diabetes, Obesity and Metabolism Apr 08, 2020
Yoon KH, Kang J, Kwon SC, et al. - In patients with type 2 diabetes (T2D), researchers evaluated the effectiveness, safety and pharmacokinetic/pharmacodynamic properties of efpeglenatide, a long‐acting glucagon‐like peptide‐1 receptor agonist. Two randomized, double‐blind, placebo‐controlled phase 2 trials have been performed. The single‐dose study (n = 48) was a first‐in‐patient, sequential dose‐escalation study and the repeated‐dose study (n = 71) was a multiple‐ascending‐dose trial. Both studies showed dose‐proportional increases in efpeglenatide serum concentrations. Both single and repeated doses of efpeglenatide have been effective and well tolerated throughout the doses and dosing regimens examined. The most frequently reported treatment‐emergent adverse events were gastrointestinal disorders in patients treated with efpeglenatide. The observed delayed tmax, long half‐life, and low peak‐to‐trough ratios indicate potential for enhanced effectiveness and dosing flexibility, with good tolerability of efpeglenatide in T2D patients.
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