A Double Blind, Randomised, Placebo-controlled Trial Evaluating the Efficacy and Safety of Nerandomilast Over 26 Weeks in Patients With Systemic Autoimmune Rheumatic Diseases Associated Interstitial Lung Diseases (SARD-ILD)

Adults 18 years of age and older or above legal age with lung fibrosis related to systemic autoimmune rheumatic disease can participate in this study. People can only take part if they show no improvement in lung function after standard treatment with immunosuppressant medicine. The main purpose of this study is to find out how a medicine called nerandomilast affects the lungs in people with systemic autoimmune rheumatic disease.
Participants are put into 2 groups randomly, which means by chance. One group takes nerandomilast tablets and the other group takes placebo tablets. Placebo tablets look like nerandomilast tablets but do not contain any medicine. Participants take a tablet 2 times a day for 26 weeks. Participants continue immunosuppressant treatment for their underlying rheumatic disease.
Participants are in the study for about 7.5 months. During this time, they visit the study site 8 times. At study visits, participants have lung function tests. At select visits, chest imaging is performed. Participants fill in questionnaires about their symptoms and quality of life. The results between the 2 groups are compared to see whether the treatment works. The doctors also regularly check participants' health and take note of any unwanted effects.

开始日期2025-07-10

申办/合作机构

Boehringer Ingelheim GmbH

NCT06241560

/ Not yet recruiting临床2期

An Open-label, Single-group Trial to Evaluate the Effect of Pirfenidone on the Pharmacokinetics of a Single Oral Dose of BI 1015550

This study is open to adults with idiopathic pulmonary fibrosis (IPF) who are 40 years and older. The purpose of this study is to find out whether a medicine called pirfenidone changes the amount of a medicine called BI 1015550 in the blood. Some people may take more than one medicine at a time. Therefore, it is important to understand how different medicines influence one another.
Participants take one dose of BI 1015550 as a tablet. Participants then take one tablet of pirfenidone 3 times a day for one week. The dose is then increased to 2 tablets 3 times a day for the second week. In the third week the dose is increased further to 3 tablets 3 times a day. Participants then take another dose of BI 1015550 as a tablet.
Participants are in the study for a little over 1 month. During this time, they visit the study site 15 times. Two of the visits include overnight stays at the study site. The study staff also contacts the participants by phone. During the visits, the doctors collect information about participants' health and take blood samples from the participants. They compare the amount of pirfenidone and BI 1015550 in the blood. Doctors also regularly check participants' health and take note of any unwanted effects.

开始日期2025-03-31

申办/合作机构

Boehringer Ingelheim GmbH

NCT06624072

/ Completed临床1期

Relative Bioavailability of Two Different Formulations of Nerandomilast and Investigation of the Food Effect on New Formulation Following Oral Administration in Healthy Adult Male and Female Subjects (an Open-label, Randomised, Single-dose, Three-way Crossover Trial)

The main objective of this trial is to investigate two different formulations of nerandomilast and the effect of food on the pharmakokinetics of the new formulation following oral administration.

开始日期2024-10-15

申办/合作机构

Boehringer Ingelheim GmbH

100 项与那米司特相关的临床结果

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100 项与那米司特相关的转化医学

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100 项与那米司特相关的专利（医药）

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项与那米司特相关的文献（医药）

2025-01-01·JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Synthesis of Carbon 14 and Deuterium‐Labelled Nerandomilast (BI 1015550)

Article

作者: Latli, Bachir ; Hrapchak, Matt J. ; Frutos, Rogelio P.

ABSTRACT:

(R)‐2‐(4‐(5‐Chloropyrimidin‐2‐yl)piperidin‐1‐yl)‐4‐((1‐(hydroxymethyl)cyclobutyl)amino)‐6,7‐dihydrothieno[3,2‐d]pyrimidine 5‐oxide (BI 1015550, 1) is a potent and selective inhibitor of phosphodiesterase type 4 (PDE4) being developed for the treatment of idiopathic pulmonary fibrosis (IPF) and progressive pulmonary fibrosis (PPF). We report the synthesis of this drug candidate labelled with carbon 14 and deuterium. The carbon 14 synthesis was completed in three radioactive steps in 27% overall yield, with a specific activity of 52 mCi/mmol (1.92 GBq/mmol), radiochemical purity, and enantiomeric excess higher than 99%. The deuterium labelled compound was prepared in seven steps in 67% overall yield and with isotopic enrichment, chemical purity, and enantiomeric excess higher than 99%.

2025-01-01·Therapeutic Advances in Respiratory Disease

Potential of phosphodiesterase 4B inhibition in the treatment of progressive pulmonary fibrosis

Review

作者: Keith, Rebecca ; Nambiar, Anoop M.

Idiopathic pulmonary fibrosis (IPF) is often regarded as the archetypal progressive fibrosing interstitial lung disease (ILD). The term “progressive pulmonary fibrosis” (PPF) generally describes progressive lung fibrosis in an individual with an ILD other than IPF. Both IPF and PPF are associated with loss of lung function, worsening dyspnea and quality of life, and premature death. Current treatments slow the decline in lung function but have side effects that may deter the initiation or continuation of treatment. There remains a high unmet need for additional therapies that can be used alone or in combination with current therapies to preserve lung function in patients with IPF and PPF. Phosphodiesterase-4 (PDE4) is an enzyme involved in the regulation of inflammatory processes. Pre-clinical studies have shown that preferential inhibition of PDE4B has anti-inflammatory and antifibrotic effects and a lower potential for gastrointestinal adverse events than pan-PDE4 inhibition. The preferential PDE4B inhibitor nerandomilast demonstrated efficacy in preserving lung function in a phase II trial in patients with IPF and is under investigation in phase III trials as a treatment for IPF and PPF.

2024-12-01·British Journal of Pharmacology

PDE4B inhibition by nerandomilast: Effects on lung fibrosis and transcriptome in fibrotic rats and on biomarkers in human lung epithelial cells

Article

作者: Quast, Karsten ; Nickolaus, Peter ; Herrmann, Franziska Elena ; Mayr, Christoph H. ; Reininger, Dennis ; Laemmle, Baerbel ; Fundel‐Clemens, Katrin ; Wollin, Lutz

Background and Purpose:

The PDE4 family is considered a prime target for therapeutic intervention in several fibro‐inflammatory diseases. We have investigated the molecular mechanisms of nerandomilast (BI 1015550), a preferential PDE4B inhibitor.

Experimental Approach:

In addition to clinically relevant parameters of idiopathic pulmonary fibrosis (IPF; lung function measurement/high‐resolution computed tomography scan/AI‐Ashcroft score), whole‐lung homogenates from a therapeutic male Wistar rat model of pulmonary fibrosis were analysed by next‐generation sequencing (NGS). Data were matched with public domain data derived from human IPF samples to investigate how well the rat model reflected human IPF. We scored the top counter‐regulated genes following treatment with nerandomilast in human single cells and validated disease markers discovered in the rat model using a human disease‐relevant in vitro assay of IPF.

Key Results:

Nerandomilast improved the decline of lung function parameters in bleomycin‐treated animals. In the NGS study, most transcripts deregulated by bleomycin treatment were normalised by nerandomilast treatment. Most notably, a significant number of deregulated transcripts that were identified in human IPF disease were also found in the animal model and reversed by nerandomilast. Mapping to single‐cell data revealed the strongest effects on mesenchymal, epithelial and endothelial cell populations. In a primary human epithelial cell culture system, several disease‐related (bio)markers were inhibited by nerandomilast in a concentration‐dependent manner.

Conclusions and Implications:

This study further supports the available knowledge about the anti‐inflammatory/antifibrotic mechanisms of nerandomilast and provides novel insights into the mode of action and signalling pathways influenced by nerandomilast treatment of lung fibrosis.

101

项与那米司特相关的新闻（医药）

2025-04-15

·BioSpace

Boehringer Ingelheim Boosts I&I Portfolio With $357M in Biobucks for Cue

iStock, Mininyx Doodle At the heart of the licensing deal is CUE-501, a bispecific molecule that can selectively deplete B cells to address autoimmune and inflammatory conditions. Boehringer Ingelheim is fronting $12 million to license Cue Biopharma’s investigational B cell depletion therapy for autoimmune diseases, the German biopharma announced on Monday. The star of this back-heavy, multi-year deal is Cue’s CUE-501, a preclinical bispecific molecule that works by binding to a specific protein found on the surface of B cells. At the same time, CUE-501 also engages and activates a specific subset of killer T cells, selectively depleting B cells to suppress autoimmunity and inflammation. According to the biotech’s website , CUE-501 sidesteps the systemic activation of all T cells, which “may offer significant advantages over current cell therapy-based strategies.” For the right to develop and commercialize CUE-501, Boehringer Ingelheim is pledging up to $345 million in research, development and commercial milestones, on top of the $12 million upfront payment. Cue will also be entitled to royalties on net sales of CUE-501. In exchange for this investment, Cue will leverage its platform technologies to further develop CUE-501. Both parties may also expand the partnership to include other anti-B cell bispecifics for autoimmune indications, according to Monday’s release. Carine Boustany, Boehringer Ingelheim’s global head of Immunology and Respiratory Disease Research, said in a statement that Monday’s licensing deal is a “strategic expansion” of the company’s portfolio in the autoimmune and inflammatory space, allowing it to “deliver a more effective treatment option to patients earlier in their disease journey.” Boehringer’s immunology and inflammatory portfolio is anchored by the oral kinase inhibitor Ofev, indicated for idiopathic pulmonary fibrosis (IPF). In 2024, sales of Ofev jumped 7% to rake in approximately $4.26 billion. Meanwhile, the pharma’s asthma drug Spiriva remained one of its top sellers, with more than $1.8 billion in sales last year, despite dipping roughly 17% from the previous year. Additionally, in September 2024, Boehringer Ingelheim reported that its drug candidate nerandomilast aced the Phase III FIBRONEER-IPF study, showing significant lung function benefits in patients with IPF. At the time, the pharma revealed plans to approval application for the drug in this indication, though a specific timeline was not provided. Beyond I&I, Boehringer Ingelheim has also signed several deals in the past year. In January, the pharma entered two antibody-focused partnerships —one with Lonza’s Synaffix and another with Oxford BioTherapeutics—in oncology. In July 2024, Boehringer Ingelheim dropped $1.3 billion to acquire Nerio Therapeutics and its small molecule assets that can “reshape” the immune system to target tumors.

引进/卖出临床3期并购免疫疗法细胞疗法

2025-04-09

·药融圈

专利将到期，IPF新品续上：改写历史的FIC（附国内企业布局）

注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需得到授权。勃林格殷格翰/BI的第二大旗舰产品尼达尼布（Ofev）在2023财年业绩为35.10亿欧元，2024年为38亿欧元。特发性肺纤维化（IPF）的大品种。药融圈获悉：此前在2025年2月10日，勃林格殷格翰/BI宣布FIBRONEER™-ILD临床试验达到其主要终点，即与安慰剂相比，第52周时患者的用力肺活量（FVC,mL）较基线的绝对变化。FVC是衡量肺功能的指标。[2] FIBRONEER™系列试验的初步数据与其特发性肺纤维化（IPF）II期研究的安全性和耐受性数据基本一致，总体不良反应与安慰剂组相当。[3]Nerandomilast是一款在研的口服选择性磷酸二酯酶4B（PDE4B）抑制剂，[3]目前尚未获批，因此安全性和有效性有待验证。药融云数据，www.pharnexcloud.com；改名后为摩熵医药数据目前正在开展FIBRONEER™全球研发项目，该项目包含两项III期临床研究：针对特发性肺纤维化（IPF）患者的FIBRONEER™-IPF研究[4]，以及针对进展性肺纤维化（PPF）患者的FIBRONEER™-ILD[5]研究。基于这些研究结果，勃林格殷格翰将向美国食品药品监督管理局（FDA）及全球范围内的其他卫生监管机构递交nerandomilast用于治疗PPF的新药申请。关于FIBRONEER™-ILD (NCT05321082)[5]FIBRONEER™-ILD是一项双盲、随机、安慰剂对照试验，评估nerandomilast（BI 1015550）在PPF患者中至少治疗52周的疗效和安全性。主要终点：基线至第52周的FVC（mL）的绝对变化。关键次要终点：试验期间首次发生以下任一复合终点事件的时间：首次出现急性ILD加重、首次因呼吸系统原因住院、或死亡（以先发生者为准）。参与FIBRONEER™-ILD临床试验的患者，将接受至少52周内接受口服nerandomilast治疗，每日两次，剂量为9 毫克或18 毫克，或作为对照组接受安慰剂治疗。Nerandomilast每日两次，每次18毫克的剂量选择是基于II期临床试验的结果。[2]新增设的每日两次，每次9毫克的剂量，旨在评估较低剂量下的获益-风险情况，并提供进一步的剂量-效应及暴露-效应的数据。[2]该临床试验已在40多个国家的400多个研究中心开展，并招募了1178名患者。关于FIBRONEER™临床项目FIBRONEER™项目包括两项III期随机、双盲、安慰剂对照试验：FIBRONEER™-IPF（NCT05321069）[4]和FIBRONEER™-ILD（NCT05321082）[5]，旨在研究nerandomilast在IPF和PPF患者中治疗至少52周的疗效、安全性和耐受性。两项研究中，主要终点均为第52周时FVC较基线水平的绝对变化。关键次要终点为试验期间首次发生以下任一复合终点事件的时间：首次出现IPF/PPF急性加重、首次因呼吸系统原因住院、或死亡（以先发生者为准）。关于NerandomilastNerandomilast（BI 1015550）是一款在研的口服磷酸二酯酶4B（PDE4B）抑制剂，正被开发作为特发性肺纤维化（IPF）和进展性肺纤维化（PPF）的潜在治疗药物。[3],[4],[5]该化合物目前仍处于研发阶段，尚未获批，其疗效和安全性也有待验证。预计今年2025年将获批上市。Nerandomilast于2022年2月获得美国食品药品监督管理局（FDA）授予的特发性肺纤维化（IPF）突破性疗法认定。[6]一项针对147名IPF患者的II期随机、双盲、安慰剂对照临床试验，研究了nerandomilast的疗效、安全性及患者耐受性。[3]该研究的主要终点为12周治疗期间FVC（用力肺活量）相较于基线的变化水平。[3]关于特发性肺纤维化（IPF）和进展性肺纤维化（PPF）特发性肺纤维化（IPF）是一类较为常见的进行性纤维化间质性肺疾病（ILD）。[7]其临床症状包括：活动诱发的呼吸急促、持续干咳、胸部不适、疲劳和乏力。尽管被视为"罕见"病，但IPF影响了全球约三百万人。[8]该疾病主要影响50岁以上的人群，且男性患者多于女性。[8]患有某些非特发性肺纤维化 (IPF) 类型的 ILD 患者也可能出现进行性表型，称为进展性肺纤维化（PPF）。除特发性肺纤维化（IPF）以外的其他间质性肺疾病（ILD）中，进展性肺纤维化的定义为呼吸症状加重、生理监测中可观察到疾病恶化，以及影像学检查结果所证实的疾病进展。[9]药融圈监测显示：国内在本靶点PDE4B布局的企业有：海思科的HSK44459片，正在进行用于特发性肺纤维化受试者的有效性及安全性的多中心、随机、双盲、安慰剂对照的II期临床研究；石药集团的SYH2059片在今年初获准开展临床试验（相关专利CN118146236A）；恒瑞医药/瑞石，人福医药，东阳光等同样在布局。其他在做PDE4领域的还有苏州璞正等等。参考：[1] Boehringer Ingelheim (2024) Boehringer's nerandomilast meets primary endpoint in pivotal phase-III FIBRONEER™-IPF study. January 2025. https://www.boehringer-ingelheim.com/us/topline-results-boehringers-phase-iii-ipf-study[2] Maher TM, et al. (2023) Design of a phase III, double-blind, randomised, placebo-controlled trial of BI 1015550 in patients with progressive pulmonary fibrosis (FIBRONEER-ILD). In: BMJ Open Respir Res 2023;10:e001580.[3] Richeldi L, et al. (2022) Trial of a Preferential Phosphodiesterase 4B Inhibitor for Idiopathic Pulmonary Fibrosis. In: N Engl J Med 2022;386:2178-2187.[4] Boehringer Ingelheim (2024) A Study to Find Out Whether BI 1015550 Improves Lung Function in People With Idiopathic Pulmonary Fibrosis (IPF). Accessed January 2025. https://clinicaltrials.gov/study/NCT05321069[5] Boehringer Ingelheim (2024) A Study to Find Out Whether BI 1015550 Improves Lung Function in People With Progressive Fibrosing Interstitial Lung Diseases (PF-ILDs). Accessed January 2025. https://clinicaltrials.gov/study/NCT05321082?tab=results.[6] Boehringer Ingelheim (2022) FDA Grants BI 1015550 Breakthrough Therapy Designation for Idiopathic Pulmonary Fibrosis. https://www.boehringer-ingelheim.com/us/human-health/lung-diseases/pulmonary-fibrosis/fda-grants-bi-1015550-breakthrough-therapy.[7] Sauleda J, et al. Idiopathic Pulmonary Fibrosis: Epidemiology, Natural History, Phenotypes. Med Sci (Basel). 2018 Nov 29;6(4):110. doi: 10.3390/medsci6040110. PMID: 30501130; PMCID: PMC6313500.[8] Koudstaal T, et al. (2023) Idiopathic pulmonary fibrosis. In: Presse Med 2023; 52(3):104166[9] Cottin, V. et al. (2023) Criteria for Progressive Pulmonary Fibrosis: Getting the Horse Ready for the Cart. In: Am J Respir Crit Care Med 2023; 207(1):11-13；[10] 药融云数据，www.pharnexcloud.com；改名后为摩熵医药数据；FDA/EMA/PMDA；www.boehringer-ingelheim.com；相关公司公开披露，https://www.boehringer-ingelheim.com；[11] 海思科，https://pharma.bcpmdata.com/database/1/detail/210/e5fZjpUBqEcAI374eYZi；石药CN118146236A；[12] https://mp.weixin.qq.com/s/hE9LH0W7jz5MBSE-g_SF1g；等等。此文仅用于向医疗卫生专业人士提供科学信息，不代表平台立场，不作任何用药推荐。更多药企信息交流可后台留下名片。会议推荐 | 点击查看详情植根上海、辐射全球,药融圈作为生物医药产业级战略平台,以"让智慧与人脉无界流动"为使命,构建覆盖药物研发、生产、流通、商业化的全产业链赋能体系。通过智能化云服务、精准资源链接、产业智库与生态社群四大核心引擎,打造中国医药价值流动的基础设施。在全球化与数字化双重浪潮下,药融圈正重新定义医药资源的流通范式--这里不仅是信息与人脉的枢纽站,更是催生产业变革的化学反应器。我们以中国为原点,编织全球医药智慧网络,让每一次精准链接都成为企业跨越式增长的催化剂。点点赞点分享点推荐

临床3期专利到期临床2期

2025-04-02

·FiercePharma

Amid uncertainty in the US, Boehringer Ingelheim projects 'slight' revenue increase for '25

Boehringer Ingelheim is projecting a "slight" revenue increase in 2025 but admitted its estimates are clouded by uncertainty over the U.S. regulatory environment and potential U.S. tariffs for pharmaceutical products. Boehringer Ingelheim picked a challenging day to reveal its 2024 financial results and guidance for this year.With President Donald Trump announcing his plan on tariffs on Wednesday and uncertainty surrounding if and how they will affect the export of pharmaceutical products to the U.S., the German company is treading lightly with its projection of a “slight year-on-year increase” in revenue.“We don't even know whether there are going to be tariffs,” Chairman Hubertus von Baumbach said on Wednesday morning during the company’s annual press conference.There are other uncertainties in the U.S. for Boehringer, which is the largest privately-owned company in the industry and has overtaken Bayer as Germany’s top seller of pharmaceuticals.For one, the drugmaker has two key products under review by the FDA, both of which Boehringer hopes to launch in the second half of this year. But with the U.S. regulator in a state of flux, von Baumbach said he isn’t sure “to what extent it will impact our ability to register products.”“All we have is the information that people are being laid off,” he added. “Like in the case of tariffs, let’s wait and see.” As for 2024, Boehringer’s revenue reached 26.8 billion euros ($29 billion), which was a 4.7% increase and a 6.1% bump at constant exchange rates.Jardiance continued as Boehringer’s top product, generating revenue of 8.4 billion euros ($9.1 billion), which was up by 15%. Sales of the aging diabetes medicine have been boosted in recent years by its approval to treat heart failure. However, that momentum is slowing after Boehringer reported increases for Jardiance of 39% in 2022 and 30% in 2023.Boehringer’s second-leading product, Ofev saw a 9% bump in sales to 3.8 billion euros ($4.1 billion). With the company losing patent protection for the idiopathic pulmonary fibrosis treatment by the end of this decade, it is banking on follow-on nerandomilast, which is under review in the U.S. and Europe. Boehringer also hopes to launch zongertinib this year. It would be the first orally administered, targeted therapy for previously treated HER2-mutated lung cancer patients.“As our current pipeline continues to mature and more products come closer to a potential market introduction, we have entered a pivotal phase of high investments,” von Baumbach said in a release, referring to Boehringer’s pharma R&D investment figure of 5.7 billion euros ($6.2 billion), which was 28% of the division’s sales.

100 项与那米司特相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
特发性肺纤维化	申请上市	中国	Boehringer Ingelheim International GmbH	2025-02-25
特发性肺纤维化	申请上市	中国	Boehringer Ingelheim Pharma GmbH & Co., KG	2025-02-25
风湿性疾病	临床3期	美国	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	中国	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	日本	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	澳大利亚	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	奥地利	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	法国	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	德国	Boehringer Ingelheim GmbH	2025-07-10
风湿性疾病	临床3期	意大利	Boehringer Ingelheim GmbH	2025-07-10

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05321082 (FIBRONEER-ILD, NEWS) 人工标引	临床3期	纤维化	1,178	nerandomilast 9 mg or 18 mg dose	網鏇廠鏇積蓋淵簾衊選(繭糧鹽鑰製鏇觸製觸願) = The study hit its primary endpoint. 壓顧鹹艱鹹遞選艱獵製 (遞鹽糧廠淵鏇獵憲鹹淵 ) 达到更多	积极	2025-02-10
				placebo
NCT04419506 (Phase 2 \| 1305-0013, CTgov)	临床2期	特发性肺纤维化	147	Placebo (Placebo - Antifibrotics at Baseline)	鏇襯鬱獵艱夢獵積壓顧(蓋膚窪窪衊鹹廠鏇構膚) = 選獵艱顧鑰膚鑰鏇廠廠齋願壓網齋觸夢構膚願 (壓網餘醖艱鹹築憲憲鬱, 壓廠選鹹繭願憲鏇獵觸 ~ 構範夢獵襯遞窪鹹繭簾) 更多	-	2022-11-01
				prifenidone+pirfenidone+BI 1015550+nintedanib (BI 1015550 - Antifibrotics at Baseline)	鏇襯鬱獵艱夢獵積壓顧(蓋膚窪窪衊鹹廠鏇構膚) = 選膚淵範製醖網艱範艱齋願壓網齋觸夢構膚願 (壓網餘醖艱鹹築憲憲鬱, 繭蓋襯製網淵選築簾選 ~ 鬱膚願壓鏇餘淵餘艱鑰) 更多
NCT01835899 (CTgov)	临床1期	-	24	Placebo	憲繭構憲觸積醖觸鏇獵 = 齋餘淵膚願衊簾壓鹽積網膚網築廠糧願鬱窪齋 (窪鹽製憲鑰繭願壓網繭, 膚淵遞窪積獵醖願顧膚 ~ 衊壓鏇簾鬱夢襯顧製願) 更多	-	2016-01-22