Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) represents the hemicalcium hydrate form of the calcium salt of Orforglipron, an orally active agonist targeting the Glucagon-like peptide-1 receptor (GLP-1R). This compound has demonstrated efficacy in mitigating type 2 diabetes [1].

在食蟹猴动物模型中，Orforglipron hemicalcium hydrate（血浆浓度0.94-4.8 nM，静脉注射30分钟；或0.05-0.1 mg/mL，灌胃，5天）剂量依赖性地抑制食物摄入，促进胰岛素分泌并降低血糖[1]。Orforglipron hemicalcium hydrate（0.05-1.35 mg/kg，灌胃）给药后2小时达到C max，血浆药物暴露量与剂量增加呈比例关系，显示其在胃肠道内呈剂量依赖性吸收[1]。Orforglipron hemicalcium hydrate在食蟹猴体内药代动力学分析[1]如下：route Dose (mg/kg) T max (h) C max (ng/mL) AUC 0-24h (ng·h/mL) i.g. 0.05 2.0 4.78 23.7 i.g. 0.15 2.0 20.7 135 i.g. 0.45 2.0 32.0 208 i.g. 1.35 2.0 148 1040。动物模型：食蟹猴模型[1]，剂量：0.9-4.8 nM；或0.05-0.1 mg/mL，给药方法：连续静脉注射30分钟使血浆浓度达到稳定状态的0.9-4.8 nM；灌胃给药5天，剂量0.05-0.1 mg/mL，结果：促进胰岛素分泌并降低血糖，剂量依赖性地抑制食物摄入。