綠葉製藥(02186.HK)：1類化學新藥LY03012完成中國I期臨牀試驗
格隆匯 12 月 23日丨綠葉製藥(02186.HK)公告，集團創新產品，1類化學新藥LY03012緩釋片("LY03012")已於中國完成I期臨牀。
該臨牀試驗採用隨機、雙盲、安慰劑對照、單次和多次劑量遞增的試驗設計，旨在評估健康受試者服用LY03012後的安全性、耐受性和藥代動力學(PK)特徵，60例受試者進入單次服藥研究(第一階段)，48例受試者進入每天一次、連續7天的多次服藥研究(第二階段)。
在該臨牀試驗中，健康受試者單次服用80–400mg、七天內每天服用80–320mg後，整體安全耐受性良好，常見不良事件主要是噁心、嘔吐、睏倦等。不良事件大多為輕度，少部分為中度，均預後良好，無受試者因不良事件退出研究，亦無非預期不良事件發生。
LY03012為一種口服的小分子化合物，非臨牀研究顯示，作為一種全新的腦內單胺類神經遞質轉運體抑制劑，可以入腦並抑制突觸前膜5-羥基色胺轉運體(serotonin transporter,SERT)、去甲腎上腺素轉運體(noradrenaline transporter,NET)和多巴胺轉運體(dopamine transporter,DAT)，從而增加突觸間隙的去甲腎上腺素、5-羥基色胺和多巴胺濃度，進而通過增強疼痛調節的下行抑制通路發揮鎮痛作用。
此外，LY03012還能調節機體的睡眠–覺醒週期，在發揮鎮痛作用的劑量下，預期不引起明顯的鎮靜和嗜睡等不良反應。過度的鎮靜和嗜睡一直是慢性疼痛治療的缺陷，嚴重影響工作和生活，如駕駛、機械操作，以及包括溝通交流在內的絕大部分社會活動，也導致用藥劑量無法進一步提升，因此不能取得更好的療效，成為目前慢性疼痛臨牀治療有效性不足的重要原因。
集團已經為LY03012申請了化合物專利、晶型專利和緩釋片劑型專利。化合物及晶型專利已在中國、美國、歐洲、日及韓國等國家取得。LY03012申報的適應症為糖尿病周圍神經痛、纖維肌痛和骨關節炎等慢性疼痛的治療。
除中國外，集團亦致力於在美國、歐洲、日及其他國家和地區註冊和上市LY03012。根據IQIVA資料，鎮痛藥在2019年於中國市場規模達到人民幣158.2億元，從2017年至2019年以17.4%的年複合增長率上升。集團已在全球上市丁丙諾啡貼劑、芬太尼貼劑等鎮痛藥物。
此外，集團還有1類新藥LPM3480392注射液(LY03014)等多個創新鎮痛藥物在研。董事會相信，LY03012將有力豐富集團鎮痛領域的產品線，從而持續推進集團在鎮痛領域的發展。
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