Carbachol

▎药明康德内容团队编辑 今日，Tenpoint Therapeutics公布其第二项3期关键试验BRIO-II的积极顶线结果。分析显示，该试验达到了与美国FDA、欧洲药品管理局（EMA）和英国药品和健康产品管理局（MHRA）商定的预设主要终点，其所开发的Brimochol PF滴眼液相较于对照组可显著改善患者的近视力，维持时间最长达8小时。这表示患者只要在早上滴几滴眼药水，几乎整个白天的近视力都得到提高！此积极结果支持该公司预定在2025年上半年递交该疗法的上市申请。 BRIO-II是一项包含3个队列、多中心、随机、双盲的安全性和疗效研究，评估Brimochol PF滴眼液与卡巴胆碱单药滴眼液和安慰剂滴眼液相比，在视力正常（无近视眼或远视眼）的老花眼患者中的疗效与安全性，该研究共招募了629名受试者。 分析显示， 相较于对照组，Brimochol PF在所有时间点（最长至8小时）显著改善患者的近视力（p<0.008）。Brimochol PF还在所有时间点显示出临床和统计学显著的瞳孔缩小效果。瞳孔缩小是缩瞳药物类别疗法的关键作用机制，通过形成针孔效应，矫正近视力丧失并增加景深。Brimochol PF在实现这一效果的同时，还改善了远距离视力，并在10小时内逐渐消除了瞳孔缩小。随着白天后期瞳孔缩小的减少，可能降低夜间视力困难的风险。在为期12个月的在家用药阶段中，研究未观察到对视力或瞳孔作用的快速耐药现象。 图片来源：123RF Brimochol PF在为期12个月的每日用药期间耐受性良好，无治疗相关的严重不良事件。额外分析显示，Brimochol PF显著改善了患者的阅读速度和基于NEI屈光误差生活质量问卷的患者报告的生活质量结果。 Brimochol PF结合了卡巴胆碱和溴莫尼定两种获批药物。缩瞳剂卡巴胆碱在缩小瞳孔的同时，可能刺激控制晶状体形状的睫状体肌肉的收缩，改变晶状体的形状，导致它的屈光特征发生变化和引起远视力下降。经常接受治疗的患者还会出现头痛、近视移位、眼睛发红等副作用。溴莫尼定是一种α2受体激动剂，它可以起到抑制睫状体肌肉收缩和减少红眼的作用，还可以提高卡巴胆碱的半衰期，让它的效果可以持续8-12个小时，这意味着早上滴一次眼药水可能管用一整天。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放 参考资料： [1] Tenpoint Therapeutics Announces Positive Topline Data from Phase 3 Pivotal Study, BRIO-II, of BRIMOCHOL™ PF for the Treatment of Presbyopia. Retrieved January 9, 2025 from https://www.businesswire.com/news/home/20250109824922/en 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。 版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。 分享，点赞，在看，聚焦全球生物医药健康创新

LONDON--( BUSINESS WIRE )--Tenpoint Therapeutics, Inc., a global, clinical-stage biotech company developing groundbreaking treatments to rejuvenate vision in the aging eye, today reported positive topline results from BRIO-II, the company’s second Phase 3 pivotal trial. BRIO-II met the pre-specified primary endpoints agreed upon with the U.S. FDA, and European Medicines Agency (EMA), and the UK Medicines and Healthcare products Regulatory Agency (MHRA), demonstrating statistically significant improvements in near vision versus vehicle at all timepoints out to 8 hours (p<0.008). BRIMOCHOL™ PF also demonstrated clinically and statistically significant reductions in pupil size at all timepoints. The reduction in pupil size is the key mechanism of action for the miotic class of therapies creating a pinhole effect that corrects for the loss of near vision and increases depth of focus. BRIMOCHOL™ PF accomplishes this while improving distance vision and providing a gradual resolution of miosis over 10 hours. Less miosis later in the day may minimize difficulties with night-time vision. No tachyphylaxis was observed in either vision or pupil effects over the duration of the 12-month at-home dosing phase of the study. BRIMOCHOL™ PF was well-tolerated over a 12-month daily dosing period with no treatment-related serious adverse events. In additional analysis, BRIMOCHOL™ PF significantly improved reading speed and patient-reported quality of life outcomes based on the NEI-Refractive Error Quality of Life questionnaire. Further details will be presented at upcoming scientific meetings. “Tenpoint Therapeutics is the only company in the presbyopia category to demonstrate contribution of elements with BRIMOCHOL™ PF, paving the way for a combination drug approval that offers the additional benefits of brimonidine,” said Rhett Schiffman, M.D., M.S., M.H.S.A., Chief Medical Officer and Head of Research and Development. “In our studies, brimonidine increased the magnitude and duration of action of carbachol and reduced the incidence of hyperemia (eye redness) over carbachol alone. BRIMOCHOL™ PF is the only presbyopia correcting eyedrop to have gone through a 12-month safety study. It was very well-tolerated over 12 months of continuous dosing and subjects in the study reported very high compliance during the study and a strong willingness to use the drug. We are very grateful to the investigators, their staff, and the study participants for their enormous efforts in this groundbreaking trial.” BRIO-II is a 3-arm, multicenter, randomized, double-masked, safety and efficacy study of BRIMOCHOL™ PF (carbachol/brimonidine tartrate fixed-dose combination) topical ophthalmic solution vs. carbachol monotherapy topical ophthalmic solution vs. a vehicle topical ophthalmic solution in subjects with emmetropic phakic or pseudophakic presbyopia ( NCT05135286 ). The study enrolled 629 subjects across 47 sites in the United States. “I am very pleased to see that BRIMOCHOL™ PF was not only well-tolerated over a 12-month dosing study but also achieved a functional improvement in reading speed, something that patients really care about,” said John Hovanesian, M.D., a member of Company’s Medical Advisory Board. “BRIMOCHOL™ PF has demonstrated a profile that, if approved, will meet the needs for a large proportion of presbyopes and I’m excited for the product to become a reality for patients.” About Tenpoint Therapeutics Tenpoint Therapeutics Limited is a global, clinical-stage biotech company developing groundbreaking treatments to rejuvenate vision in the aging eye. Its pipeline includes paradigm-shifting treatments for ophthalmic indications with the greatest need and global market potential, including presbyopia, cataracts and geographic atrophy. Its lead asset, BRIMOCHOL™ PF, is a novel, pupil-modulating therapeutic designed to correct the loss of near vision associated with presbyopia, a condition that afflicts approximately 2 billion people globally. BRIMOCHOL™ PF has completed two large phase 3 pivotal trials (BRIO-I and BRIO-II) and the company plans to file the US NDA, in the first half of 2025. This topical ophthalmic is poised for launch in 2026. Tenpoint’s leadership team includes ophthalmic industry luminaries with track records of successful approvals and commercialization of blockbuster drugs. A privately held company, Tenpoint Therapeutics is backed by AdBio Partners, British Patient Capital, Eight Roads, EQT Life Sciences, F-Prime Capital, Hillhouse Capital Management, Qiming Venture Partners USA, Sofinnova Partners, and UCL Technology Fund. To learn more, visit tenpointtherapeutics.com and connect on LinkedIn .