Ascletis Selects for Clinical Development a Fixed-Dose Combination of First-in-Class Oral Small Molecule GIPR Agonist, ASC48, and Oral Small Molecule GLP-1R Agonist, ASC30

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- ASC48 is a potentially first-in-class oral small molecule GIPR agonist. - ASC48 demonstrated an EC 50 of 1 pM in the hGIPR cAMP activation assay, exhibiting greater potency than tirzepatide (EC 50 = 3 pM) and is a selective agonist for GIPR without activity for GLP-1R and GCGR. - ASC48 demonstrated excellent oral bioavailability and drug exposure as well as long half-life in rodents and non-human primates (NHPs), supporting once-daily oral dosing in humans. - Fixed dose combination of ASC30 and ASC48 (ASC30_48 FDC) is a potentially first-in-class oral one-pill, once-daily treatment for obesity, targeting both GLP-1R and GIPR. - ASC30_48 FDC demonstrated approximately 52% greater relative body weight reduction compared to ASC30 monotherapy in a head-to-head NHP study. - ASC30_48 FDC is a once-daily oral small molecule with the same mechanism of action as tirzepatide, the market leading GLP/GIP once weekly subcutaneous peptide with over $30 billion in sales in 2025. - Submission of an Investigational New Drug Application (IND) to the U.S. Food and Drug Administration (FDA) for ASC30_48 FDC oral tablets is expected in the fourth quarter of 2026. HONG KONG, July 15, 2026 /PRNewswire/ -- Ascletis Pharma Inc. (HKEX: 1672, "Ascletis") announces that it has selected a fixed-dose combination of ASC48, a potentially first-in-class oral small molecule GIPR agonist, and ASC30, an oral small molecule GLP-1R agonist, for clinical development. ASC30 and ASC48 fixed-dose combination (ASC30_48 FDC) is a potentially first-in-class oral one-pill, once-daily therapy for obesity, targeting GLP-1R and GIPR. ASC48 was discovered in-house utilizing Ascletis' Artificial Intelligence-assisted Structure-Based Drug Discovery (AISBDD) technology. In a head-to-head study, ASC48 demonstrated an EC50 of 1 pM in the hGIPR cAMP activation assay, exhibiting greater potency than tirzepatide (EC50 = 3 pM) and is a selective agonist for GIPR without activity for GLP-1R and GCGR. ASC48 demonstrated excellent oral bioavailability and drug exposure as well as long half-life in rodents and non-human primates (NHPs), supporting once-daily oral dosing in humans. ASC30_48 FDC demonstrated approximately 52% greater relative body weight reduction compared to ASC30 monotherapy in a head-to-head NHP study (Table 1). Table 1. Once-daily oral administration of ASC30_48 FDC for eight consecutive days produced 52% and 518% greater relative body weight reduction, respectively compared to ASC30 and ASC48 monotherapies

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