歌禮制藥-B(01672.HK)進軍肥胖藥物領域，宣佈其小分子GLP-1R激動劑ASC30正於美國進行每月一次皮下注射和每日一次口服片劑治療肥胖症的兩項I期臨牀試驗
格隆匯9月17日丨歌禮制藥-B(01672.HK)公吿，董事會宣佈其近期已在美國開展的ASC30兩項I期臨牀試驗均已完成首批患者給藥。ASC30是首款也是唯一一款既可每月一次皮下注射也可每日一次口服用於治療肥胖症的小分子GLP-1受體(GLP-1R)激動劑。歌禮ASC30片劑和ASC30注射劑分別於2024年7月和2024年9月獲得美國食品藥品監督管理局(FDA)的新藥臨牀試驗(IND)批准。公司預計將於2025年第一季度獲得上述兩項美國I期臨牀試驗的頂線數據。
ASC30是歌禮自主研發的不募集β-抑制蛋白(without β-arrestin recruitment)的小分子GLP-1R偏向激動劑(GLP-1 Rbiased small molecule agonist)。ASC30具有獨特和差異化性質，使以每月一次皮下注射和每日一次口服片劑的形式給藥成為可能。經過頭對頭比較，ASC30對GLP-1R的體外藥效比orforglipron高出2到3倍。在對非人靈長類動物(NHPs)進行的靜脈葡萄糖耐受實驗(IVGTT)中，經過頭對頭比較，與orforglipron(劑量：6毫克╱公斤)相比，ASC30(劑量：1.5毫克╱公斤)刺激分泌的胰島素更多，具有統計學顯著性差異。
在動物模型中，ASC30注射劑的半衰期長達25天，這為在人體中每月注射一次提供了支持。在NHPs中，與每週注射1次、共計6次的一種抗體多肽偶聯藥物相比，單次ASC30皮下注射可在一個月內持續有效地減輕體重。與每週注射一次的多肽GLP-1藥物和每月注射一次的抗體多肽偶聯候選藥物相比，每月皮下注射一次的ASC30具有潛在的強大競爭優勢(注射頻率更低和╱或成本更低)。
ASC30每日一次的片劑具有優越的藥代動力學(PK)特徵且對GLP-1R具有更強效的激動作用，使其有望成為同類最佳的GLP-1R小分子激動劑。在動物模型中，ASC30片劑的半衰期長達36小時，為每日口服一次提供了支持。在NHPs中，每日口服一次ASC30可顯著減輕體重。利用歌禮專有技術，在動物模型中，ASC30片劑穩態相對生物利用度達到了99%。
在肥胖症和糖尿病市場，每月一次的注射和每日一次的口服用藥對患者都很具吸引力。患者可能根據長期體重管理方法、生活方式和便利性選擇從注射轉為口服用藥，或口服轉註射用藥。ASC30作為一種小分子，可同時提供每月注射一次和每日口服一次兩種用藥選擇。此外，ASC30口服片劑和注射劑具有相同或相似的安全性，便於患者在兩種方案間切換。
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