Nintedanib esylate

新“马甲”，很神奇 同一种药，换个“马甲”就能更有效、更长效、副作用更小，真有这么神奇吗？创新给药剂型让这件事成真。药物新剂型是在传统药物剂型基础上，通过创新技术或方法研发出的新型药物形态。制成新剂型，好比穿上不同的“马甲”，实现长效、靶向以及副作用最小化，提高药物临床依从性。 从长效缓释制剂微球、微晶到“精准投放”的靶向制剂脂质体、纳米粒，从薄如糯米纸的口溶膜到快速起效的软胶囊，近年来，齐鲁制药构建起多个高端复杂制剂技术平台，突破“卡脖子”关键技术，解决未满足的临床需求，不断惠及广大患者。 一天三次变一月一针 在齐鲁制药布局的新剂型产品里，微球的技术难度最大，也是最具价值的制剂之一。微球制剂是由包裹着药物、粒径为1到250微米的球状实体组成，大多数上市的微球产品的粒径从十几微米到几十微米不等。微球到底有多“微”？1微米只有头发丝的1/50。 微球肉眼看起来就是一堆粉末，本领却大得不得了，精确控制药物的释放速率，可持续平稳释放药物几周至数月，最长可实现6个月给药一次，不用老跑医院打针，大大提高患者的用药依从性，并减轻用药经济负担。2023年8月，齐鲁制药注射用醋酸奥曲肽微球获得国家药监局批准上市，为该产品国内首家获批，同时，也是国内首个按照仿制药一致性评价要求批准上市的长效微球制剂。奥曲肽微球一个月只需给药一次，相比于每日注射三次的普通剂型，它显著降低了注射频率和不良反应。 微晶/纳米晶制剂是将原料药粉碎或研磨成微米晶体（粒径1-100微米）或纳米晶体（粒径100-1000纳米）并悬浮于水溶液或油溶液中，也能持续、缓慢释放药物，用药一次能管1个月甚至6个月，口服、注射、透皮、眼部给药统统涵盖。 2023年10月，齐鲁制药长效微晶制剂棕榈酸帕利哌酮注射液获得国家药监局批准上市，为国内首家，同时，也是首个批准上市的国产月度给药长效微晶制剂。该产品每月仅需给药1次，兼具急性期快速起效，维持期持续改善症状的作用。此外，棕榈酸帕利哌酮注射液获美国FDA临时性批准。 精准靶向出击，副作用更小 复杂制剂军团中除了超长待机的“长效缓释战士”，还有专攻病灶的“特种兵”，脂质体、纳米粒等纳米制剂就是典型代表。纳米制剂靶向出击，能让药物精准到达病灶，提高药物有效浓度，疗效更佳，降低药物全身毒性和不良反应。 脂质体是用脂质分子包封住药物，形成一个微型胶囊，就像一个“泡泡”，把药物精准投放到身体需要的地方。脂质体制剂能加强药物利用度和稳定性，同时降低对正常组织的损害，降低毒性，减少不良反应。2024年5月，齐鲁制药盐酸多柔比星脂质体注射液获批上市，因其强大的抗肿瘤活性、较同类抗肿瘤抗生素高出数倍的成药性，广泛用于乳腺癌、卵巢癌、多发性骨髓瘤等肿瘤治疗。此外，另一款脂质体药物两性霉素B脂质体已在中国、美国和欧洲申报上市。 纳米粒制剂是以纳米级颗粒（10-100纳米）为载体，包裹着药物，保护药物不被分解或失活。纳米粒能精准锁定肿瘤组织，到达病灶部位后药物分子缓慢释放，既提高打击精度，又减少对健康细胞的伤害，提升患者生活质量。2019年，齐鲁制药纳米粒制剂注射用紫杉醇（白蛋白结合型）获批上市，白蛋白作为载体，利用纳米技术把白蛋白与不溶于水的紫杉醇结合，相较于传统溶剂，避免了多种不良反应。与传统紫杉醇制剂相比，纳米粒剂型高疗效，低毒性，使用方便。 软雾吸入剂则是通过局部给药实现“靶向”，高效递送的软雾剂装置让药液雾化，形成细腻、缓慢移动的药雾，直接递送到肺部，相比于传统气雾剂，到达肺部的药物剂量高得多。软雾剂实现快速起效与精准治疗的双重优势，而且全身不良反应少。今年齐鲁制药两个软雾剂产品噻托溴铵奥达特罗吸入喷雾剂和噻托溴铵吸入喷雾剂国内申报上市，主要用于慢性阻塞性肺疾病（包括慢性支气管炎和肺气肿）的长期维持治疗。 让吃药难变为吃药易 一个生病的孩子哭闹着不肯吃药，一个哮喘患者半天不会用干粉吸入剂，一个精神病患者把药吐出来……很多时候，用药难成为治疗“拦路虎”，而剂型的改进和给药方式创新轻松化解难题。 软雾剂的一大优势就是便携易用，相比要精确配合吸气和按压的传统吸入剂，患者可自然吸气，无需吸气配合，操作简单，难度低，对儿童、老年人和肺功能降低或呼吸困难的患者非常友好。 口溶膜则让吃药变得像“吃糖”般轻松，口溶膜是含药聚合物薄膜，看起来像一张小小糯米纸，入口是水果味，不用水送服，在口中十几秒溶解。而且口溶膜易吸收、起效快、副作用小，尤其适用于儿童、老年、吞咽困难的患者，大大提高用药依从性。 2013年，齐鲁制药开始布局口溶膜制剂研发，是国内最早进行此类改良型剂型研究的药企。2021年，公司首个口溶膜产品奥氮平口溶膜获批上市，为精神疾病患者提供全新、更便捷的用药选择。今年7月，又有一款抗精神病药物利培酮口溶膜获批上市。目前齐鲁制药已有6个口溶膜产品上市，5个为国内首家，包括适用于儿童哮喘的孟鲁司特钠口溶膜、适用于阿尔茨海默症的盐酸美金刚口溶膜等。 软胶囊也是一款让吃药变得更容易的新剂型，把液状油性物完全气密封装于软质囊材中，能掩盖药物不良气味、方便服药。服用后软胶囊能够在胃部迅速溶解，释放出药物，从而有利于药物的快速吸收。齐鲁制药已上市乙磺酸尼达尼布软胶囊、二十碳五烯酸乙酯软胶囊等7个软胶囊产品，覆盖心血管、呼吸、泌尿、免疫系统等多个治疗领域。 “高精尖”复杂制剂不断“上新” 如今，高技术壁垒的复杂注射剂研发已成为药物创新的热点，其临床价值明显、安全性好等特点为临床需求提供“更优解”。早在2007年，齐鲁制药就开始创新布局，搭建多个高端复杂制剂技术平台，开发高技术壁垒复杂制剂和新型给药技术药物，不断突破技术壁垒，实现多款首仿药和改良型创新药快速上市，用更多新药、好药。 目前，齐鲁制药已有微球、微晶、纳米粒、脂质体、口溶膜、软胶囊、亚微乳、渗透泵控释片等30多项复杂制剂产品获批上市，其中10余项为国内首家或独家获批上市，为临床医生和患者提供更贴合个体需求、具有临床实用性的用药新选择。 点击下方关键词 获取更多资讯  ↓↓ | 李燕总裁 | 全国人大代表 |  | 中国医药百强 | 伊鲁阿克 | 患者招募 |  | 雷珠单抗 | 全球首创艾托组合抗体 | 曲帕双靶组合 |  | 董事长的二十万个蛋糕 | 社会责任企业 |

Peer-reviewed publication highlights potential breakthrough anti-fibrotic properties of LTI-03 in lung tissue from IPF patientsAUSTIN, Texas, Sept. 17, 2025 (GLOBE NEWSWIRE) -- Rein Therapeutics ("Rein") (NASDAQ: RNTX), a biopharmaceutical company advancing a novel pipeline of first-in-class medicines to address significant unmet medical needs in orphan pulmonary and fibrosis indications, today announced the publication of novel data on its lead drug candidate, LTI-03, in iScience, a peer-reviewed, open-access journal published by Cell Press. The paper, titled “LTI-03 peptide demonstrates anti-fibrotic activity in ex vivo lung slices from IPF patients,” reports how LTI-03 was tested directly on lung tissue donated by patients with idiopathic pulmonary fibrosis (IPF) who underwent lung transplant. In this model, LTI-03 showed signs of reducing scarring and protecting lung cells, reinforcing its potential as an important new therapy. Key Highlights The study used real lung tissue donated by IPF patients. These samples continued to show scarring activity for several days, making them a highly relevant way to test new therapies.LTI-03 reduced multiple scarring pathways (including TGFβ, VEGF, PDGF, and FGF), while also lowering collagen production and inflammatory signals in diseased lung tissue.Unlike nintedanib, the FDA-approved standard-of-care drug, LTI-03 achieved these effects without causing cell damage or death in patient samples, reinforcing the drug’s strong safety profile.The findings add to the growing body of evidence that LTI-03 has the potential to become a meaningful new therapy for IPF. Brian Windsor, PhD, Chief Executive Officer of Rein Therapeutics, commented, “Using a highly relevant translational model, this peer-reviewed publication provides further validation of LTI-03’s broad anti-fibrotic effects in IPF lung tissue. These data support our ongoing Phase 2 RENEW trial, where we are evaluating LTI-03 in patients living with IPF, a disease with very limited treatment options and high unmet need.” Urgent Need IPF is a progressive fibrotic lung disease that affects approximately 100,000 people in the U.S. and more than 70,000 in the U.K. Median survival is just 3–5 years from diagnosis, even with currently approved therapies. The global market for IPF treatments is projected to exceed $11 billion by 2031, underscoring the urgent need for more effective approaches. Next Steps Rein recently announced regulatory approval from the U.K.’s MHRA to initiate the Phase 2 RENEW trial of LTI-03. The trial will evaluate safety, tolerability, and changes in lung function in up to 120 patients, with initial data expected in 2026. The full article can be found here: https://www-cell-com.libproxy1.nus.edu.sg/iscience/fulltext/S2589-0042(25)01698-0 About Rein Therapeutics Rein Therapeutics is a clinical-stage biopharmaceutical company advancing a novel pipeline of first-in-class therapies to address significant unmet medical needs in orphan pulmonary and fibrosis indications. Rein's lead product candidate, LTI-03, is a novel, synthetic peptide with a dual mechanism targeting alveolar epithelial cell survival as well as inhibition of profibrotic signaling. LTI-03 has received Orphan Drug Designation in the U.S. and is in clinical development. Rein's second product candidate, LTI-01, is a proenzyme that has completed Phase 1b and Phase 2a clinical trials for the treatment of loculated pleural effusions. LTI-01 has received Orphan Drug Designation in the U.S. and E.U. and Fast Track Designation in the U.S. Forward-Looking Statements This press release may contain forward-looking statements of Rein Therapeutics, Inc. ("Rein", the "Company", "we", "our" or "us") within the meaning of the Private Securities Litigation Reform Act of 1995, including statements with respect to expectations for the Company’s LTI-03 product candidate. We use words such as "anticipate," "believe," "estimate," "expect," "hope," "intend," "may," "plan," "predict," "project," "target," "potential," "would," "can," "could," "should," "continue," and other words and terms of similar meaning to help identify forward-looking statements, although not all forward-looking statements contain these identifying words. Actual results may differ materially from those indicated by such forward-looking statements as a result of various important factors as well as the risks disclosed in the "Risk Factors" section of the Company's Annual Report on Form 10-K for the year ended December 31, 2024, which is on file with the United States Securities and Exchange Commission (the "SEC") and in subsequent filings that the Company files with the SEC. These forward-looking statements should not be relied upon as representing the Company's view as of any date after the date of this press release, and we expressly disclaim any obligation to update any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. Rein Investor Relations & Media Contact: Investor Relations IR@ReinTx.com