Core Insights - The article highlights the clinical development of ASC37, a novel oral GLP-1R/GIPR/GCGR triagonist peptide by Gilead Sciences, showcasing its significant pharmacokinetic advantages over existing treatments [5][7]. Group 1: Drug Development - ASC37 has entered clinical development as of November 30, with a notable oral bioavailability of 4.2%, which is approximately 9 times, 30 times, and 60 times higher than semaglutide, tirzepatide, and retatrutide, respectively [5]. - The drug's development leverages Gilead's two core technology platforms: AI-assisted drug discovery and enhanced oral peptide delivery technology [5]. - In non-human primate studies, ASC37 demonstrated an average apparent half-life of about 56 hours, supporting once-daily or even less frequent dosing [7]. Group 2: Efficacy and Exposure - ASC37 exhibited a drug exposure level (measured by area under the curve) approximately 57 times greater than that of retatrutide, indicating a higher amount of active substance entering systemic circulation for enhanced efficacy [7]. - The drug's activity levels in activating GLP-1R, GIPR, and GCGR receptors were approximately 5 times, 4 times, and 4 times higher than retatrutide, respectively [5]. Group 3: Regulatory Plans - Gilead plans to submit a new drug clinical trial application for ASC37 to the FDA for obesity treatment in the second quarter of 2026 [7].
速递｜超替尔泊肽30倍！新口服三靶点减重药进行临床开发