Aceclidine

盐酸毛果芸香碱滴眼液的仿制，近年非常受业内关注。 盐酸毛果芸香碱滴眼液自23年开始，累计批了14张仿制临床批件，对一个较为小众的眼科领域，属实罕见。 图源：摩熵医药 盐酸毛果芸香碱滴眼液算得上一款眼科神药，这是FDA批准的第一款用于治疗老花眼的眼药水，由艾伯维旗下艾尔建研发。 2021年，艾尔建宣布，FDA批准了Vuity（盐酸毛果芸香碱眼用溶液）1.25%，用于治疗成人老视（老花眼）。 其实毛果芸香碱眼用最开始用于治疗青光眼，即硝酸毛果芸香碱滴眼液，艾尔建在其基础上改动了酸根，以505(b)(2)改良上市。 彼时资本市场非常看好艾伯维这款滴眼液以及老花眼药物市场，多家国外证券机构预测老花眼市场至少能达到年30-50亿美元。 但从实际销售情况来看，艾伯维这款神药较预期存在很大差距，截至2025年艾伯维发布三个季度的销售数据，Vuity并未被单独列出，而是与Xen凝胶支架等设备合并算入“其他眼部护理”，这部分产品合计总销售额才仅达到2.48亿美元。 2023年，全球第二款老花眼药物上市，由ORASIS公司研发的0.4%浓度毛果芸香碱滴眼液Qlosi在FDA获批，Vuity是多剂量包装，需要防腐剂，而Qlosi是单剂量包装，不含防腐剂，且低浓度使不良反应发生概率减少，因此ORASIS公司凭着一款产品在2024年融资7800W。 目前这两款产品均已被纳入参比目录，从目前有临床进度的企业来看，因单剂量不含防腐剂，技术要求更高，大部分都选择了艾尔建的1.25%含量进行仿制。 其中很多眼科龙头企业，比如国内“OK镜一哥”欧普康、眼科王牌莎普爱思等均获批了临床。 其中莎普爱思的临床批件是2023年从南京恒道花费952万元买入，发布公告后莎普爱思连日涨停，足见资本市场多看好此品种，目前山东华铂凯盛和南京正科已完成Ⅲ期临床提交了上市申请。 此品种上市需要相当长的时间和精力，至今首仿未出。进度最快的是山东华铂凯盛和南京正科医药，已在2025年提交上市申请，正在等待评审中。 放眼全球，目前已上市的老花眼药物并不多，仅4款，除了上文提到的Vuity和Qlosi外，还有两款分别是： VIZZ（2025年7月FDA批准）： 由LENZ THERAP公司研发，含1.44%醋克利定，为首款醋克利定类眼药水，每日用药1次，30分钟起效，维持显著改善视力效果长达10小时。 YUVEZZI（2026年1月FDA批准）： Tenpoint公司研发，是含卡巴胆碱与溴莫尼定的复方制剂，这是FDA批准的首款用于治疗老花眼的复方滴眼液。Yuvezzi同样采用每日一滴给药方案，可在30分钟内起效，持续长达10小时，从而改善近视力。 与盐酸毛果芸香碱成分滴眼液原研未在国内上市不同，这两款药物原研均已选择跟国内企业达成合作，不日就将进入国内。 2022年4月，箕星获得醋克利定滴眼液的大中华区权益，包括港澳台。根据协议，箕星支付首付款1500万美元，1500万美元开发里程碑付款，8000万美元销售里程碑付款，以及基于净销售额5%到15%分级销售分成或者在产品批准前再授权收入15%到5%。 目前盐酸醋克利定滴眼液的上市申请已于25年7月获CDE受理。 图源：摩熵医药 另一款2022年5月，兆科眼科与Tenpoint签订独家许可协议，获得Yuvezzi在大中华区、韩国及指定东南亚地区的开发与商业生产权；2024年2月，双方进一步扩大合作，将授权区域拓展至更多市场。 在国内， 兆科眼科正在开展 Yuvezzi用于治疗老花眼的Ⅱ期临床。 这一小众领域用药，要卷起来了！ ↓⭐关注药通社，洞见行业趋势↓ 投稿/企业合作/内容沟通： 药通社总编—华籍美人（Ww_150525） *添加请注明备注及来意

Tenpoint Therapeutics' newly approved Yuvezzi can improve the up-close vision of patients with presbyopia, potentially allowing them to discard their reading glasses. Combining two eye drops that have been on the market for at least 30 years each has earned Tenpoint Therapeutics an FDA approval (PDF) for Yuvezzi, a treatment for presbyopia, a common, age-related condition that makes it difficult to focus on nearby objects.Yuvezzi, which is a solution of 2.75% carbachol and 0.1% brimonidine tartrate, becomes the first combination treatment for presbyopia, which affects roughly 2 billion around the world and 128 million in the United States.Carbachol reached the market in 1972 as Alcon’s Miostat to dilate pupils during cataract surgeries. Brimonidine tartrate was commercialized in 1996 by Allergan as an ocular hypertension eye drop and most recently by Bausch+Lomb as Lumify, a treatment to reduce eye redness.Along with the approval, London-based Tenpoint raised (PDF) a Series B round of $85 million led by Janus Henderson, EQT Nexus, Hillhouse and the British Business Bank. Additionally, Tenpoint has secured a $150 million debt facility from Hercules Capital, which the company will pull down in installments.The funding will facilitate Yuvezzi’s launch, which Tenpoint expects to kick off early in the second quarter of this year.Yuvezzi—also known as Brimochol PF—was originally developed by Visus Therapeutics, a seven-year-old Seattle company, which merged 13 months ago with Tenpoint. Forging the partnership was the chairman of both biotechs, David Guyer, M.D.“(Visus) had a pretty narrow group of key investors, but they had a really exciting pipeline,” Tenpoint CEO Henric Bjarke said in an interview with Fierce. “And then you had Tenpoint, which had a very exciting but early-stage pipeline. And they had a broad base of investors.”Bjarke, who took over in December of 2024, was brought in for his experience launching ophthalmic drugs. He said Tenpoint recently reached a headcount of 100 and has hired two-thirds of its sales force, which will eventually include 76 sales reps targeting 12,200 physicians across 8,800 offices. By the end of this year, Bjarke expects to have 180 to 200 employees on board.The approval was backed by two phase 3 trials. The first study demonstrated Yuvezzi’s superiority over its individual components, which is a requirement the FDA imposes on fixed-dose combo treatments. The vehicle-controlled second study achieved all vision improvement endpoints and sustained efficacy measures over eight hours. With participants receiving treatments for 12 months, which is the longest safety study ever conducted for presbyopia, there were no serious adverse treatment effects.The dual action provided by Yuvezzi includes carbachol to constrict the eye’s pupil and brimonidine to stop it from dilating. Keeping the pupil small creates a pinhole effect, improving visual acuity and depth of focus.“Carbachol is the drug that creates the miotic effect, or the reduction of the size of your pupil,” Bjarke explained. “And brimonidine increases the amount of carbachol that reaches the target tissue, so you get better effect and longer duration.” The approval of Yuvezzi comes just six months after the FDA signed off on another presbyopia treatment, Lenz Therapeutics’ eye drop Vizz. Analysts at William Blair have pegged Vizz, which has a unique mechanism of action, as a potential blockbuster.Other presbyopia drugs have had difficulty gaining a foothold in the market. Much was expected of AbbVie’s Vuity, which was approved in 2021, but the product hasn’t generated enough revenue to appear in the company’s quarterly financial reports. Orasis Pharmaceuticals scored a 2023 FDA approval for presbyopia drug Qlosi but the company didn’t launch the eye drop until April of 2025.“We have a competitive product. We have an innovative product and we have a strong story to tell around it,” Bjarke said when asked about other competition.Bjarke calls the market “enormous” and believes there is room for multiple products.“If you are an individual who’s had glasses all your life, this might not be something for you,” Bjarke said. “But people who live an active life—either through work or through hobbies—where they go to their activity and it forces them to put on and take off their glass, it’s very frustrating.” In his practice in Laguna Hills, California, John Hovanesian, M.D., of Harvard Eye Associates, sees many patients who are looking for another alternative.“The impact of presbyopia is often underestimated and current solutions like glasses, contacts or surgery have fallen short in meeting the real-world needs of people who struggle with close-up tasks,” Hovanesian said in the release.