開拓藥業-B(09939.HK):GT20029用於雄激素性脱髮及痤瘡適應症的新藥研究申請獲國家藥監局受理
格隆匯2月1日丨開拓藥業-B(09939.HK)發佈公吿,GT20029用於雄激素性脱髮及痤瘡適應症的新藥研究(IND)申請已獲中國國家藥品監督管理局藥品審評中心(CDE)受理。
GT20029是一種使用本集團內部的靶向蛋白降解嵌合體(PROTAC)平台開發的外用雄激素受體(AR)降解劑。PROTAC是一種小分子,其組成包括(i)靶蛋白(POI)的配體;(ii) E3泛素連接酶的配體;及(iii)結合(i)及(ii)的連接器。三元複合物形成後,通過縮小POI與E3泛素連接酶間的距離並使其貼近,PROTAC可引起POI的泛素化並進而降解POI。由於每個PROTAC分子可降解多個AR蛋白,低劑量的PROTAC藥物便可達到療效。此外,只要細胞中有少量的PROTAC分子,藥物療效便可維持,與其他小分子藥物相比可大幅減少給藥頻率。
GT20029是一種降解AR蛋白的AR降解劑。GT20029的作用機制為將AR蛋白招募至E3泛素連接酶進行降解。其作用於表層皮膚的局部組織及局部毛囊皮脂腺,可降低AR對雄激素的敏感性,而無需全身接觸藥物。
根據動物實驗,GT20029的有效性優於其他小分子AR抑制劑。此外,GT20029不會引起過度藥物蓄積及明顯的副作用。於達到療效的同時,GT20029能夠有效避免全身接觸藥物,以減少或避免口服雄激素信號通路抑制劑的副作用。與現有的口服抗雄激素療法相比,GT20029的優勢為見效快且副作用較少,併為雄激素性脱髮及痤瘡患者提供更多臨牀選擇。
據董事所知及所信,GT20029是全球首個進入臨牀階段的外用PROTAC藥物。集團亦正在準備GT20029於美國的IND申請。
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