Introduction and Objective: ASC30 is an oral GLP-1R biased small molecule agonist without β-arrestin recruitment, discovered and developed in-house at Ascletis. ASC30 has unique and differentiated properties that enable the administration of one small molecule as both a once-monthly subcutaneous injection and a once-daily oral tablet. The current study assessed safety, tolerability and pharmacokinetics of ASC30 oral tablet in a first-in-human single ascending dose study.Methods: This was a randomized, double-blind, placebo-controlled single ascending dose study in participants with a BMI of 30-40 kg/m². A total of 40 eligible participants were enrolled in a 6:2 ratio to receive ASC30 tablets at doses of 2 mg, 5 mg, 10 mg, 20 mg, or 40 mg, or matching placebo.Results: All AEs were mild (70.3%) to moderate (29.7%) in severity and consistent with GLP-1RA class. No SAEs or clinically significant changes in labs, including liver enzymes, due to study drug were observed. Table 1 shows preliminary pharmacokinetic analyses, which support once-daily oral dosing.Conclusion: ASC30 tablet exhibited a good safety and tolerability profile in this SAD study. Based on its superior PK profile, enhanced potency as a GLP-1 RA, and favorable safety profile, ASC30 tablet once-daily, has the potential to be the best-in-class oral GLP-1R small molecule agonist.
J. Wu: Employee; Ascletis Pharma (China) Co., Limited. V. Wang: None.
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