第一部分：PK/PD探索研究 1)评价甲磺酸雷沙吉兰透皮贴剂给药一周（4天/贴+3天/贴）的安全性。 2)评价甲磺酸雷沙吉兰透皮贴剂给药一周（4天/贴+3天/贴）的药代动力学和药效动力学特征。 3)比较甲磺酸雷沙吉兰透皮贴剂与甲磺酸雷沙吉兰片的药代动力学和药效动力学特征。 4)评价甲磺酸雷沙吉兰透皮贴剂给药后的黏附性、刺激性和致敏性。第二部分：多次给药生物利用度研究 1)比较甲磺酸雷沙吉兰透皮贴剂与甲磺酸雷沙吉兰片在健康人体内连续给药的相对生物利用度。 2)比较甲磺酸雷沙吉兰透皮贴剂与甲磺酸雷沙吉兰片多次给药的药效动力学特征。 3)评价甲磺酸雷沙吉兰透皮贴剂和甲磺酸雷沙吉兰片多次给药的安全性。 4)评价甲磺酸雷沙吉兰透皮贴剂多次给药的黏附性、刺激性和致敏性。第三部分：不同部位生物利用度研究 1)比较甲磺酸雷沙吉兰透皮贴剂不同部位给药的生物利用度。 2)评价甲磺酸雷沙吉兰透皮贴剂的安全性、黏附性、刺激性和致敏性。

开始日期2025-02-05

申办/合作机构

上海世领制药有限公司

[+1]

CTR20243770

/ Active, not recruitingN/A

甲磺酸雷沙吉兰片在健康受试者中空腹与餐后条件下开放、随机、单次给药、两制剂、两序列、四周期完全重复交叉设计生物等效性试验

研究空腹与餐后状态下单次口服受试制剂（甲磺酸雷沙吉兰片，规格1mg，浙江九洲生物医药有限公司持证）与参比制剂（甲磺酸雷沙吉兰片，规格1mg，商品名安齐来，Teva Pharmaceutical Industries Ltd.持证）在健康受试者体内的药代动力学特征，比较受试制剂与参比制剂的生物等效性，并研究药物在健康受试者体内的安全性。

开始日期2024-11-05

申办/合作机构

浙江九洲生物医药有限公司

CTIS2024-512311-41-00

/ Not yet recruiting临床1期

- UECHUP-RAS/24-2

开始日期2024-06-04

申办/合作机构-

100 项与甲磺酸雷沙吉兰相关的临床结果

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100 项与甲磺酸雷沙吉兰相关的转化医学

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100 项与甲磺酸雷沙吉兰相关的专利（医药）

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1,055

项与甲磺酸雷沙吉兰相关的文献（医药）

2025-12-01·MOLECULAR BIOLOGY REPORTS

Molecular pathways: the quest for effective MAO-B inhibitors in neurodegenerative therapy

Review

作者: Udi, Onoriode Andrew ; Ogbutor, Udoji Godsday ; Atere, Adedeji David ; Oyovwi, Mega Obukohwo ; Joseph, Gregory Uchechukwu

Neurodegenerative diseases like Parkinson's and Alzheimer's are a global health challenge due to their progressive degeneration, leading to cognitive decline and motor dysfunction. Monoamine oxidase B (MAO-B) enzyme is implicated in neurodegeneration, and developing inhibitors could be a promising therapeutic strategy. This review explores MAO-B activity molecular pathways, evaluates MAO-B inhibitors in neurodegenerative therapy, identifies challenges, and suggests future research directions. This review synthesizes findings from a range of scientific literature, including experimental studies, clinical trials, and biochemical analyses that focus on the role of MAO-B in neurodegeneration. Information was gathered from databases such as PubMed, Scopus, and Web of Science, ensuring a comprehensive overview of recent advancements in MAO-B inhibition strategies. The review reveals several promising MAO-B inhibitors that have demonstrated efficacy in preclinical models, as well as some that have progressed to clinical trials. Compounds such as rasagiline and selegiline have shown neuroprotective effects and benefits in symptom management in patients with Parkinson's disease. Furthermore, the review discusses novel inhibitors that target specific molecular pathways, enhancing the potential for improved therapeutic outcomes. However, several inhibitors also present challenges regarding their selectivity, side effects, and long-term efficacy. Research on MAO-B inhibitors for neurodegenerative diseases is crucial, with ongoing studies aiming for selective, potent molecules with fewer side effects and multimodal therapies.

2025-03-27·JOURNAL OF MEDICINAL CHEMISTRY

Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor

Article

作者: Basile, Lorenzo ; Lambona, Chiara ; Garofalo, Stefano ; Fioravanti, Rossella ; Mai, Antonello ; Massari, Marta ; Noce, Beatrice ; Gottinger, Andrea ; Fiorentino, Francesco ; Binda, Claudia ; Valente, Sergio ; Limatola, Cristina ; Castelôa, Mariana ; Mormino, Alessandro ; Marchese, Sara ; Reis, Joana ; Mattevi, Andrea ; Raucci, Alessia

NADPH oxidases (NOXs) are enzymes dedicated to reactive oxygen species (ROS) production and are implicated in cancer, neuroinflammation, and neurodegenerative diseases. VAS2870 is a covalent inhibitor of mainly NOX2 and NOX5. It alkylates a conserved active-site cysteine, blocking productive substrate binding. To enhance potency and selectivity toward NOXs, we conducted some chemical modifications, leading to the discovery of compound 9a that preferentially inhibits NOX2 with an IC₅₀ of 0.155 μM, and only upon its preactivation. We found that 9a, bearing a pargyline moiety, is also able to selectively inhibit MAOB over MAOA (465-fold) with an IC₅₀ of 0.182 μM, being the first-in-class dual NOX2/MAOB covalent inhibitor. Tested in the BV2 microglia neuroinflammation model, 9a decreased ROS production and downregulated proinflammatory cytokines as iNOS, IL-1β, and IL-6 expression more efficiently than the single target inhibitors (rasagiline for MAOB and VAS2870 for NOXs) but also, more importantly, than their combination.

2025-02-28·JOURNAL OF ORGANIC CHEMISTRY

Copper-Catalyzed Domino Annulation of Isoselenocyanates: A Pathway to Structurally Diverse N, Se-Bis-Heterocyclic, and Fused Heterocyclic Compounds

Article

作者: He, Yan ; Fang, Yi-Ling ; Wang, Hai-Yang ; Wang, Ying-Chun

A copper-catalyzed domino addition/cyclization reaction was developed to synthesize novel benzoselenazole-linked 1,2,3-triazole and tetracyclic fused 12H-benzo[4,5]selenazole[2,3-b]quinazolin-12-one derivatives from isoselenocyanates. This domino reaction efficiently constructed multiple new chemical bonds in a single step, forming either four (one C-Se and three C-N) or three (one C-Se and two C-N) bonds. The reaction offers several key advantages, including mild conditions, broad substrate compatibility, and straightforward and safe operation. It presents a new method for synthesizing N, Se-containing polycyclic compounds, which have potential interest in medicinal chemistry. Notably, some of the synthesized compounds exhibited anticancer activity with IC₅₀ values below 20 μmol L^-1 against T24 human bladder cancer cells.

项与甲磺酸雷沙吉兰相关的新闻（医药）

2025-04-22

·PRNewswire

XADAGO/EQUFINA Set to Revolutionize Parkinson's Disease Treatment Landscape | DelveInsight

As a selective monoamine oxidase B (MAO-B) inhibitor, XADAGO offers a unique mechanism of action that complements traditional therapies, potentially improving motor function and reducing "off" time in patients. The increasing prevalence of Parkinson's disease and the growing demand for effective therapies create a substantial market opportunity for XADAGO, particularly in regions with aging populations. LAS VEGAS, April 22, 2025 /PRNewswire/ -- DelveInsight's " XADAGO/EQUFINA Market Size, Forecast, and Market Insight Report" highlights the details around XADAGO/EQUFINA, an inhibitor of monoamine oxidase B (MAO-B) indicated as an adjunctive treatment to levodopa/carbidopa in patients with Parkinson's disease experiencing "off" episodes. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of XADAGO/EQUFINA. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. Newron Pharmaceuticals/Eisai/Meiji Seika Pharma's XADAGO/EQUFINA (safinamide) Overview XADAGO is a monoamine oxidase B (MAO-B) inhibitor used alongside levodopa/carbidopa to help manage "off" episodes in individuals with Parkinson's disease. While its exact mode of action in treating Parkinson's is not fully understood, it is thought to work by inhibiting MAO-B, thereby reducing dopamine breakdown. This leads to increased dopamine levels and enhanced dopaminergic activity in the brain. XADAGO contains the active ingredient safinamide in the form of a mesylate salt and is available in 50 mg and 100 mg film-coated oral tablets. Each tablet provides either 65.88 mg or 131.76 mg of safinamide mesylate, equivalent to 50 mg or 100 mg of the safinamide base. The medication is marketed as XADAGO in the United States and Europe and under the name EQUFINA in Japan. Learn more about XADAGO/EQUFINA projected market size for Parkinson's disease @ XADAGO/EQUFINA Market Potential Parkinson's disease is a progressive neurological disorder that mainly impairs movement control. It results from the slow degeneration of dopamine-producing neurons in the brain, especially in the substantia nigra, a region crucial for managing voluntary motor function. According to estimates by DelveInsight, there were 2.7 million diagnosed prevalent cases of Parkinson's disease in the 7MM in 2023, with the United States accounting for around 45% of these cases. While a cure for Parkinson's remains elusive, a combination of pharmacological and non-pharmacological therapies is used to manage symptoms. Physical, occupational, and speech therapies form key components of treatment, and surgical procedures may benefit select patients. Additionally, complementary therapies are sometimes employed to help address particular symptoms. Frequently prescribed medications for Parkinson's include levodopa, dopamine agonists, MAO-B inhibitors, COMT inhibitors, amantadine, anticholinergics, and adenosine A2A antagonists. These treatments primarily target motor symptoms, which are a major concern for those affected. DelveInsight reports that the Parkinson's disease market in the 7MM was valued at USD 3.2 billion in 2023. The market is expected to grow over the forecast period (2020–2034), fueled by the launch of new therapies, increasing prevalence, better access to healthcare, and rising demand for more advanced and effective treatment options. Discover more about the Parkinson's disease market in detail @ Parkinson's Disease Market Report Emerging Competitors of XADAGO/EQUFINA Some of the drugs in the pipeline include Solengepras (Cerevance), Minzasolmin (UCB Biopharma SRL/Novartis), Buntanetap (Annovis Bio), and others. Buntanetap has successfully completed Phase III trials for early-stage Parkinson's disease. Annovis Bio has scheduled a meeting with the FDA in Q1 2025 to determine the development path forward for Buntanetap in the treatment of Parkinson's disease. Buntanetap is also being developed for Alzheimer's disease, Lewy Body Dementia, and other neurodegenerative disorders. In November 2024, Cerevance announced the dosing of the first patient in its pivotal Phase III ARISE trial, evaluating solengepras as a potential adjunctive treatment for Parkinson's disease. Cerevance expects to report topline data in the first half of 2026. In December 2021, UCB partnered with Novartis to globally co-develop and co-commercialize UCB0599, a pioneering alpha-synuclein misfolding inhibitor currently in Phase II clinical trials for Parkinson's disease. To know more about the number of competing drugs in development, visit @ XADAGO/EQUFINA Market Positioning Compared to Other Drugs Key Milestones of XADAGO/EQUFINA In April 2020, Newron Pharmaceutical acknowledged that US WorldMeds, who held the US commercialization rights for the licensed drug, XADAGO, as a sub licensee of Zambon, had entered into a definitive agreement with Supernus Pharmaceuticals under which Supernus would acquire the CNS portfolio of US WorldMeds, including the US rights to XADAGO In November 2019, Eisai announced that it had launched the EQUFINA 50mg tablets for the indication of improvement of the wearing-off phenomenon in patients with Parkinson's disease under treatment with a drug containing levodopa in Japan. Manufacturing and marketing approval of EQUFINA was obtained in September 2019. In April 2017, Eisai Co., Ltd. and Meiji Seika Pharma announced entering into a license agreement for the commercialization of safinamide (development code: ME2125) to treat Parkinson's disease in Japan and Asia. In March 2017, Newron Pharmaceuticals announced the US FDA approval of XADAGO to treat Parkinson's disease as an add-on therapy to levodopa/carbidopa for patients experiencing "off" episodes. In March 2016, Zambon announced a strategic agreement with US WorldMeds to commercialize Newron's lead compound, XADAGO, to treat Parkinson's disease in the US. In February 2015, XADAGO was approved in the European Union as an add-on therapy to levodopa, alone or in combination with other Parkinson's medications, in mid-late stage PD patients with motor fluctuations. XADAGO/EQUFINA Patent Details XADAGO tablets are currently protected by three XADAGO patents with US patent numbers 8,076,515, 8,278,485, and 8,283,380, which expire between June 2027 and December 2028 and are listed in the FDA's publication, Approved Drug Products with Therapeutic Equivalence Evaluations, commonly referred to as the Orange Book. The company has a license agreement with Zambon S.p.A., Newron's partner, related to the XADAGO Patents, and as a new chemical entity, XADAGO is under the 5-year FDA exclusivity period that expires on March 21, 2022. In May 2017, Zambon filed a worldwide patent under the patent number WO2017207587A1. The invention relates to pharmaceutical compositions comprising safinamide and, more particularly, to taste-masked particles comprising said active ingredient or pharmaceutically acceptable salts thereof, oral dosage forms that include said particles, and a process for preparing them. Discover how XADAGO/EQUFINA is shaping the Parkinson's disease treatment landscape @ XADAGO 50mg XADAGO/EQUFINA Market Dynamics XADAGO, marketed as EQUFINA in some regions (notably in South Korea and Japan), is a once-daily oral selective MAO-B inhibitor used as an add-on treatment for Parkinson's disease patients experiencing "off" episodes while on a stable dose of levodopa. The drug's unique dual mechanism of action—MAO-B inhibition and modulation of glutamate release—offers both dopaminergic and non-dopaminergic effects, positioning it as a differentiated product in the PD adjunctive therapy landscape. This has helped it carve a niche in markets where patients are inadequately controlled by levodopa alone, particularly those in mid-to-late-stage PD. The global market dynamics for XADAGO/EQUFINA are shaped by a mix of competitive intensity, regional adoption trends, and payer dynamics. In the U.S. and Europe, the drug has faced stiff competition from generic MAO-B inhibitors (like selegiline and rasagiline) and newer Parkinson's disease therapies, including COMT inhibitors, dopamine agonists, and extended-release levodopa formulations. Despite this, its favorable safety profile and once-daily dosing have supported its uptake in certain patient segments, especially in Europe. Market penetration has been slower in the U.S. due to both reimbursement hurdles and physician preference for more established adjunctive treatments. In Asia, particularly Japan and South Korea, EQUFINA has demonstrated stronger market performance thanks to focused commercial strategies and a high unmet need for effective "off time" management. Meiji Seika Pharma and Eisai, the regional marketing partners, have successfully leveraged the drug's differentiated profile in clinician education, which has led to growing adoption among neurologists. In Japan, where the aging population is rapidly expanding and Parkinson's prevalence is rising, EQUFINA has benefited from both demographic tailwinds and formulary access. Looking ahead, the market outlook for XADAGO/EQUFINA depends on several strategic levers, including lifecycle management, regional partnerships, and real-world evidence generation. The manufacturer's ability to expand into new geographies, secure favorable reimbursement, and differentiate against both generics and newer entrants will be critical. Moreover, as Parkinson's disease treatment moves toward more personalized approaches, XADAGO/EQUFINA may find sustained relevance in specific subpopulations, particularly those requiring a balance of efficacy and tolerability. Dive deeper to get more insight into XADAGO/EQUFINA's strengths & weaknesses relative to competitors @ XADAGO/EQUFINA Market Drug Report Table of Contents Related Reports Parkinson's Disease Market Parkinson's Disease Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key Parkinson's disease companies, including UCB Biopharma SRL, Novartis, Annovis Bio, Supernus Pharmaceuticals, Inc., Britannia Pharmaceutical, Pharma Two B, Mitsubishi Tanabe Pharma (NeuroDerm), AbbVie, Cerevel Therapeutics, Cerevance, among others. Parkinson's Disease Pipeline Parkinson's Disease Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key Parkinson's disease companies, including Cerevel Therapeutics, Inhibikase Therapeutics, Neuraly, Peptron, Biogen, Roche, Brain Neurotherapy Bio, Inc., Modag, Annovis Bio Inc., BioVie Inc., United Neuroscience Ltd., Luye Pharma Group, AbbVie, UCB Biopharma SRL, InnoMedica Schweiz AG, Integrative Research Laboratories AB, H. Lundbeck A/S, Shanghai WD Pharmaceutical Co., Ltd., Cerevance Beta, Inc., Nobilis Therapeutics Inc., BlueRock Therapeutics, Taiwan Mitochondrion Applied Technology Co., Ltd., among others. Cell and Gene Therapy in Parkinson's Disease Market Cell and Gene Therapy in Parkinson's Disease Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key cell and gene therapy in Parkinson's disease companies including MeiraGTx, Hope Biosciences, Sumitomo Pharma, Prevail Therapeutics, BlueRock Therapeutics, Voyager Therapeutics, among others. Parkinson's Disease Psychosis Market Parkinson's Disease Psychosis Market Insights, Epidemiology, and Market Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key Parkinson's disease psychosis companies, including Sumitomo Pharma America Inc., Vanda Pharmaceuticals, Acadia Pharmaceuticals Inc., Otsuka America Pharmaceutical, Lundbeck LLC, Jazz Pharmaceuticals, Alkahest Inc., Sandoz, Sio Gene Therapies, Axovant Sciences Ltd, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床3期上市批准引进/卖出临床2期

2025-04-14

·微信

2025 MDS 运动波动循证建议更新解读

帕金森病（PD）患者在长期使用左旋多巴治疗后，超过80%的患者最终会出现症状波动（如 “关期” 延长、“开期” 缩短、剂末现象等）1。在另一项国内的研究中，接受左旋多巴治疗的中国患者在近1年内有29.0%出现症状波动，而10年以上人群中症状波动的发生率则高达68.3%2。在一项针对帕金森患者的问卷调查中，高达66.3%的患者认为改善症状波动非常重要3。因此，对帕金森患者的症状波动现象进行更好的管理对改善患者的生活质量有很重要的意义。为了更好地协助医生们针对患者个体选择合适的治疗方案，MDS（International Parkinson and Movement Disorder Society，国际帕金森和运动障碍学会）在2002年第一次基于循证医学证据发表了选择治疗方法的建议，而且之后也在定期更新，最近一次的更新是在2018年。截至目前，针对帕金森病运动症状的治疗方案仍然在不断增加，多项临床试验结果也在陆续发表。因此在2025年，MDS基于102项随机对照试验（RCT，randomized controlled trial），采用了新的评估方法，系统评估了现有治疗手段（包括药物和手术）的有效性与安全性，为临床决策提供了重要参考（图1）4。图1在文章中，针对每一项干预措施的疗效评价都采用了两个维度：（1）结局的临床相关性（the clinical relevance of the outcome）；（2）证据质量（the quality of the evidence）。为了确定临床结局的相关性，如果有临床数据，就会使用相应量表上的最小临床重要差异（MCID，minimal clinically important differences）。对于 “开期” 时长、“关期” 时长以及无异动症的时间长度，最小临床重要差异为每天1小时5。而对于PDQ-39（帕金森病问卷 - 39 项，Parkinson's Disease Questionnaire - 39），最小临床重要差异为5分6。在证据质量方面，采用改良的GRADE方法（modified version of Grading of Recommendations, Assessment, Development, and Evaluations)，基于偏倚风险、不精确性、不一致性、间接性以及发表偏倚的可能性，对每一项干预措施有效性的证据质量进行评估（图2）。图2沙非胺（既往称沙芬酰胺，safinamide）是新一代的MAO-B（ B型单胺氧化酶，monoamine oxidase B）抑制剂，并且是所有药物中唯一的具有双重作用机制抗帕金森的药物。沙非胺除了通过抑制MAO-B对多巴胺递质的分解代谢外，还可以通过阻滞离子通道的途径来抑制过量谷氨酸的释放来改善帕金森患者的症状7。该篇文献经过筛查最终纳入了4项与沙非胺相关的RCT8-11。在4项RCT中，对比评估了沙非胺和安慰剂之间对于改善“开期”和“关期”时间的疗效。全部试验都观察到了具有临床意义的“关期”时间减少（相比安慰剂组减少约1h），并且增加了不伴有令人困扰的运动障碍的“开期”时间（相比安慰剂组增加约1h），显示了沙非胺对于症状波动者的优越疗效。在PDQ-39评分表方面，其中1项研究8显示沙非胺达到了改善日常生活质量的阈值，另一项研究9提示在沙非胺100mg组中，对于安慰剂，PDQ-39评分的改善也超过了5分的阈值均提示了其在改善帕金森病患者日常生活质量的作用。另一方面，值得注意的是MDS目前基于现有研究认为，沙非胺是唯一具有双重作用机制（MAO-B抑制和通道阻滞）的抗帕金森药物。而且在药物有效性方面，相比于前两代MAO-B阻滞剂司来吉兰和雷沙吉兰，其对于症状波动的改善有更高程度的证据支持（沙非胺为有效，司来吉兰为证据不足，雷沙吉兰为可能有效）。并且唑尼沙胺（zonisamide）不再被认为是双机制治疗药物，其对症状波动的有效性方面，MDS也基于最新证据也将其从有效调整为可能有效（图3）。图3此外，IPX 066, ER（卡比多巴 / 左旋多巴缓释剂，Levodopa Carbidopa Extended – Release，IPX 066为其研究代码）在治疗症状波动上也有令人满意的效果，而且是唯一被MDS认为有效的Levodopa/PDI（左旋多巴 / 外周脱羧酶抑制剂）类药物。文中参考了1篇发表于2013年的RCT12。该研究发现IPX 066相比对照组在减少“关期”时间上有明显优势（约1.2 h ，P < 0.0001），并且在“开期”时间上也有明确改善（不伴令人困扰的运动障碍的“开期”时间为0.9 h, P < 0.001；不伴任何运动障碍的“开期”时间为0.7 h, P < 0.05）（图4）。图4在外科治疗方面，MDS也对各种治疗方式的临床有效性做了较大的调整。当前，Bilateral STN DBS（Bilateral Subthalamic Nucleus Deep Brain Stimulation，双侧丘脑底核脑深部电刺激术）是唯一被MDS认为有效的术式。而在上一版推荐中同样被认为有效的Bilateral GPi DBS（Bilateral Globus Pallidus Internus Deep Brain Stimulation，双侧苍白球内侧部脑深部电刺激术）和Unilateral pallidotomy（单侧苍白球切开术）现已被调整为可能有效（图5）。图5时隔7年 MDS 从数据库中15485篇相关文章最终筛选了102项高质量 RCT，并且采用了新的方法来对所有纳入的文章进行治疗有效性分析和证据质量分级。随着时间推移、新药的开发和更多临床试验结果的发表，人们对于帕金森运动波动的理解和治疗观念也随之发生改变：IPX 066成为唯一达到有效级别的 Levodopa/PDI 类药物、普拉克索和罗替高汀的治疗地位仍然稳固、恩他卡朋和雷沙吉兰的有效性级别下降、沙非胺成为唯一有效的双机制药物、唑尼沙胺在有效性级别下降的同时也不再被认为具有通道阻滞的作用、 Bilateral STN DBS是当前证据最充分的针对运动波动症状的手术方案。未来随着更多新药的开发和临床试验的进行，治疗的选择仍然可能会出现变化。 MDS最新的循证医学建议确认了沙非胺对于帕金森病症状波动治疗的有效性。作为新一代的MAO-B抑制剂，沙非胺可以抑制MAO-B对于多巴胺递质的代谢，同时调节钠离子和钙离子通道抑制过量谷氨酸的释放，通过目前唯一的双重抗帕金森机制，可以明显减少“关期”时间并且增加不伴有令人困扰的运动障碍的“开期”时间，其在改善PDQ-39评分方面也有一定的优势，并且对于非运动症状也有明显的改善作用13-15。在帕金森病的治疗中，尤其是出现运动并发症的患者，沙非胺将会是很有优势的选择。参考文献1. Stocchi F, Antonini A, Barone P,et al. Early DEtection of wEaring off in Parkinson disease: the DEEP study. Parkinsonism Relat Disord. 2014 Feb;20(2):204-11. 2. Wan Y, Yuan C. Hou X, et al. Wearing-off Identification in Parkinson's Disease: The shapd-woq Study. Front Neurol. 2020 Mar 13:11:116.3. Wüllner U, Fuchs G, Reketat N, et al. Requirements for Parkinson's disease pharmacotherapy from the patients' perspective: a questionnaire-based survey. Curr Med Res Opin. 2012 Jul;28(7):1239-46. study. Parkinsonism Relat Disord. 2014 Feb;20(2):204-11. 4. de Bie RMA, Katzenschlager R, Swinnen BEKS, Peball M, Lim SY, Mestre TA, Perez Lloret S, Coelho M, Aquino C, Tan AH, Bruno V, Dijk JM, Heim B, Lin CH, Kauppila LA, Litvan I, Spijker R, Seppi K, Costa J, Sampaio C, Fox SH, Silverdale MA. Update on Treatments for Parkinson's Disease Motor Fluctuations - An International Parkinson and Movement Disorder Society Evidence-Based Medicine Review. Mov Disord. 2025 Mar 8. doi: 10.1002/mds.30162. Epub ahead of print. PMID: 40055961. 5. Hauser RA, Gordon MF, Mizuno Y, et al. Minimal clinically important difference in Parkinson’s disease as assessed in pivotal trials of pramipexole extended release. Parkinsons Dis 2014;2014: 467131. 6. Horvath K, Aschermann Z, Kovacs M, et al. Changes in quality of life in Parkinson’s disease: how large must they be to be relevant Neuroepidemiology 2017;48(1–2):1–8. 7. Calabresi p, Kulisevsky J. Safinamide as Add-on Therapy - Moving Beyond Dopamine for a Multifaceted Approach in Parkinson's Disease.European Neurological Review,2017:12(Suppl. 5):2-6. 8. Borgohain R, Szasz J, Stanzione P, et al. Randomized trial of safinamide add-on to levodopa in Parkinson’s disease with motor fluctuations. Mov Disord 2014;29(2):229–237. 9. Hattori N, Tsuboi Y, Yamamoto A, Sasagawa Y, Nomoto M. Efficacy and safety of safinamide as an add-on therapy to L-DOPA for patients with Parkinson’s disease: a randomized, double-blind, placebo- controlled, phase II/III study. Parkinsonism Relat Disord 2020;75:17–23. 10. Schapira AHV, Fox SH, Hauser RA, et al. Assessment of safety and efficacy of safinamide as a levodopa adjunct in patients with Parkinson disease and motor fluctuations: a randomized clinical trial. JAMA Neurol 2017;74(2):216–224. 11. Wei Q, Tan Y, Xu P, et al. The XINDI study: a randomized phase III clinical trial evaluating the efficacy and safety of safinamide as add-on therapy to levodopa in Chinese patients with Parkinson’s disease with motor fluctuations. CNS Drugs 2022;36:1217–1227. 12. Hauser RA, Hsu A, Kell S, et al. Extended-release carbidopa-levodopa (IPX066) compared with immediate-release carbidopa-levodopa in patients with Parkinson’s disease and motor fluctuations: a phase 3 randomised, double-blind trial. Lancet Neurol 2013;12(4): 346–356. 13. Cattaneo C, M¨uller T, Bonizzoni E, et al. Long-Term Effects of Safinamide on Mood Fluctuations in Parkinson's Disease. J Parkinsons Dis. 2017;7(4):629-634. 14. Cattaneo C, Barone P, Bonizzoni E, et al. Effects of Safinamide on Pain in Fluctuating Parkinson's Disease Patients: A Post-Hoc Analysis. J Parkinsons Dis. 2017;7(1):95-101. 15. García DS, López IC, Guerra CL,et al. Safinamide improves sleep and daytime sleepiness in Parkinson's disease: results from the SAFINONMOTOR study. Neurol Sci. 2022 Apr;43(4):2537-2544. 提示：本材料仅供医疗卫生专业人士进行医学科学交流，不用于推广目的。

临床研究临床结果

2025-04-11

·医药地理

世界帕金森日看用药市场变局：多巴丝肼领跑、罗替高汀微球入局

2025年4月11日是第29个世界帕金森日，今年的主题是“人工智能助力帕金森病管理”。帕金森病（Parkinson's Disease, PD）作为典型的神经系统退行性疾病，主要影响中老年人。其病理特征是大脑中产生多巴胺的神经元逐渐退化和死亡，导致多巴胺分泌不足，从而引发一系列运动和非运动症状。据悉，帕金森病是增长最快的神经系统疾病，目前全世界已有超过1000万帕金森病患者，预计到2050年全球帕金森病患者数量可达到2500万人。患者主要表现为静止性震颤、运动迟缓、肌强直、自主神经功能障碍等症状，给患者本人及家庭带来了较大负担。药物分类及作用机制按照作用靶点分类，帕金森病治疗药物主要可以分为以下几类：uDDC（DOPA脱羧酶）：DDC催化左旋多巴转化为多巴胺，是多巴胺合成的关键步骤。通过抑制DDC，可以减少外周左旋多巴的代谢，使其更多地进入中枢神经系统，从而提高左旋多巴的疗效。uHTR（5-羟色胺受体）：主要在调节情绪和认知功能方面发挥作用，通过与多巴胺能系统相互作用，调节基底神经节的活动，从而改善运动功能，不仅如此，HTR拮抗剂可以减少左旋多巴诱导的异动症。uCOMT（儿茶酚-O-甲基转移酶）：COMT抑制剂通过抑制COMT酶的活性，减少左旋多巴在外周的代谢，延长其进入中枢神经系统的时间，从而提高左旋多巴的生物利用度。uDAT（多巴胺转运体）：DAT负责多巴胺的再摄取，通过抑制DAT，可以增加突触间隙中的多巴胺浓度，从而延长多巴胺的作用时间。uMAOB（单胺氧化酶B）：MAOB抑制剂通过抑制MAOB酶的活性，减少多巴胺的分解，从而延长其在基底神经节中的作用时间。此外，MAOB抑制剂还具有抗氧化和神经保护作用。uDRD（多巴胺受体）：DRD激动剂可直接激活多巴胺受体，模拟多巴胺的作用，缓解运动症状。uADOR2a（腺苷A2A受体）：ADOR2a拮抗剂通过阻断A2A受体，减少间接通路的过度兴奋性，从而改善帕金森病的运动症状。Pharma ONE智能药物大数据分析平台显示，目前全球已有41款（按通用名计）治疗帕金森病的药物上市，具体品种如下：图：全球已上市的帕金森病治疗药物来源：Pharma ONE智能药物大数据分析平台，中国医药工业信息中心药物竞争市场格局基于PDB药物综合数据库展开分析，2020年至2024年，帕金森病治疗药物院端市场呈现先降后升的状态，2020年—2022年整个市场规模呈现缩减趋势，2022年缩减至27.33亿元，自2023年出现回升，2024年回升至28.78亿元，同比增长率达到6.80%。图：2020年—2024年帕金森病治疗药物市场规模来源：PDB药物综合数据库国内院端放大板块，中国医药工业信息中心近五年来，帕金森病治疗药物的市场格局也出现了巨大变化，其中，左旋多巴+苄丝肼，复方（多巴丝肼）的市场份额实现了大幅提升，从14.82%增长到23.65%，跃居市场首位，2024年销售额更是达到了6.80亿。雷沙吉兰的市场份额也实现了快速增长，2024年已占据13.01%的市场份额，成功跻身市场前三。相比较之下，普拉克索的市场份额出现了大幅缩减，降幅更是超过了10%，痛失榜一宝座，苯海索、吡贝地尔、溴隐亭、卡比多巴+左旋多巴，复方更是掉出了榜单前十，市场份额大幅减少。图：2020年、2024年帕金森病治疗药物市场竞争格局来源：PDB药物综合数据库国内院端放大板块，中国医药工业信息中心除此之外，PDB药物综合数据库数据显示，2024年有44款用于治疗帕金森病的药物进入了国家医保常规目录，其中浙江京新药业股份有限公司、齐鲁制药（海南）有限公司、石药集团欧意药业有限公司、海思科制药（眉山）有限公司、江苏恒瑞医药股份有限公司的盐酸普拉克索（缓释）片中标，被纳入第四批国采。图：2024年被纳入医保及国采的帕金森病治疗药物来源：PDB药物综合数据库国内院端放大板块，中国医药工业信息中心研发进程目前，全球各大药企都有布局帕金森病治疗，全球已有上百款帕金森病治疗药物进入临床。在中国，已有罗替高汀、雷沙吉兰、普拉克索在内的5个品种（按通用名计）获批上市，用于帕金森病的药物治疗，国内更是有数十款创新药处于积极的临床开发阶段。据不完全统计，这些新药包括COMT抑制剂、LRRK2靶向抑制剂、线粒体自噬诱导剂等多种类型，其中几个比较具有代表性的药物如下：2024年6月，绿叶制药宣布其自主研发的创新微球制剂——金悠平®（注射用罗替高汀微球），作为纳入优先审评审批程序的品种，已获得中国国家药品监督管理局的上市批准，用于帕金森病的治疗，金悠平®基于绿叶制药全球领先的微球技术平台开发，每周给药一次，是全球首个治疗帕金森病的长效缓释微球制剂，也是目前更符合“持续多巴胺能刺激（CDS）”理念的周制剂。复星医药与Bial公司合作的奥吡卡朋胶囊，作为一种第三代COMT抑制剂，已提交上市申请。该药物自2016年在欧盟首次获批，作为左旋多巴/多巴脱羧酶抑制剂（DDCIs）的辅助治疗手段，适用于帕金森病患者，尤其是那些因剂量末期运动波动而无法稳定病情的成年患者。左旋多巴是治疗帕金森病的常用药物，但随着疾病进展到中晚期，患者单独使用左旋多巴可能会遇到疗效减退的问题。奥吡卡朋作为COMT抑制剂，通过抑制左旋多巴的分解，使其更多地进入大脑，从而增强治疗效果，改善症状。XS-411是由士泽生物研发的通用型iPS衍生多巴胺能神经前体细胞注射液，分别于今年2月和4月在美国和中国获得IND许可，用于治疗帕金森病。根据士泽生物的公开资料，该公司与合作医院共同开展的国家级备案临床研究中，临床级iPSC衍生细胞在患者纹状体壳核区移植治疗中重度帕金森病的最长随访期已超过12个月，未出现与细胞疗法相关的不良事件。此外，多项关键疗效指标如开关期时间和MDS-UPDRS评分量表，以及多项非运动指标均显示出显著改善。这些积极结果为后续临床试验的开展提供了重要依据和验证。目前，该产品针对帕金森病的1期临床试验正在有序进行中。帕金森病的治疗是一个任重道远的过程，在各大药企的努力下，期待未来有越来越多的新药获批上市用于治疗帕金森病。想要了解更多帕金森病有关内容？欢迎点击下方医药地理药研科普数字人短视频查阅有关内容。想要获得更多医药相关的数据信息吗？欢迎扫码使用数据库，开启属于你的数据检索之旅！END如需获取更多数据洞察信息或公众号内容合作，请联系医药地理小助手微信号：pharmadl001

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外链

KEGG	Wiki	ATC	Drug Bank
D02562	甲磺酸雷沙吉兰	N04BD02	DB01367

研发状态

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10 条最早获批的记录,

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适应症	国家/地区	公司	日期
帕金森病	欧盟	Teva Pharmaceuticals Europe BV	2005-02-21
帕金森病	冰岛	Teva Pharmaceuticals Europe BV	2005-02-21
帕金森病	列支敦士登	Teva Pharmaceuticals Europe BV	2005-02-21
帕金森病	挪威	Teva Pharmaceuticals Europe BV	2005-02-21

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适应症	最高研发状态	国家/地区	公司	日期
精神运动障碍	临床3期	-	H. Lundbeck A/S	2011-01-01
不宁腿综合征	临床3期	美国	Teva Neuroscience, Inc.	2010-09-01
帕金森病（青年型、早发型）	临床3期	-	Teva Neuroscience, Inc.	1997-07-01
多系统萎缩	临床2期	美国	H. Lundbeck A/S	2009-12-01
多系统萎缩	临床2期	奥地利	H. Lundbeck A/S	2009-12-01
多系统萎缩	临床2期	加拿大	H. Lundbeck A/S	2009-12-01
多系统萎缩	临床2期	法国	H. Lundbeck A/S	2009-12-01
多系统萎缩	临床2期	德国	H. Lundbeck A/S	2009-12-01
多系统萎缩	临床2期	匈牙利	H. Lundbeck A/S	2009-12-01
多系统萎缩	临床2期	以色列	H. Lundbeck A/S	2009-12-01

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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


NCT03727139 (JapicCTI-184181, Pubmed \| Expert Opin Drug Saf)	N/A	帕金森病	961	Rasagiline 1 mg once daily	顧遞蓋網衊蓋淵壓遞範(築夢鹽繭膚顧餘夢齋夢) = 製鹽糧夢網鏇築築壓顧願獵鹽積顧齋獵衊窪範 (蓋衊餘壓餘選鏇觸網廠 )	积极	2024-01-02
NCT02789020 (CTgov)	临床2期	帕金森病	96	functional Magnetic Resonance Imaging+Rasagiline (Rasagiline)	憲餘鹹廠積範壓網網顧(鬱壓製觸膚壓艱鏇齋獵) = 觸夢淵鏇簾鹹襯鏇觸積製壓壓壓鹽構選廠願蓋 (廠鹹膚鬱顧憲鬱衊淵繭, 0.01) 更多	-	2023-09-06
				functional Magnetic Resonance Imaging (Placebo)	憲餘鹹廠積範壓網網顧(鬱壓製觸膚壓艱鏇齋獵) = 範艱選遞餘遞壓顧選鹽製壓壓壓鹽構選廠願蓋 (廠鹹膚鬱顧憲鬱衊淵繭, 0.01) 更多
NCT02359552 (R2, CTgov)	临床2期	阿尔茨海默症	50	Placebo (Placebo)	製廠積願齋艱獵齋觸築(夢遞範構選鏇餘鑰衊夢) = 獵願廠蓋衊夢壓艱膚鏇選願獵繭繭鬱衊餘淵襯 (遞醖蓋鏇製築艱築範觸, 0.030) 更多	-	2020-10-20
				Rasagiline (Rasagiline)	製廠積願齋艱獵齋觸築(夢遞範構選鏇餘鑰衊夢) = 願積顧築鏇蓋願壓憲廠選願獵繭繭鬱衊餘淵襯 (遞醖蓋鏇製築艱築範觸, 0.030) 更多
NCT01786603 (CTgov)	临床2期	肌萎缩侧索硬化	80	Rasagiline (Rasagiline)	蓋鏇憲壓鏇淵獵簾構艱(鏇醖網夢選鹹鬱夢糧簾) = 遞鏇鏇糧鹹夢遞衊範顧衊顧壓餘鬱齋願窪範遞 (製鬱製襯餘選簾鑰鬱蓋, 選憲製餘衊襯鬱網網鬱 ~ 襯窪膚艱夢願繭網顧觸) 更多	-	2020-01-27
				Placebo (Placebo)	蓋鏇憲壓鏇淵獵簾構艱(鏇醖網夢選鹹鬱夢糧簾) = 壓鏇鹽淵鏇遞遞襯醖獵衊顧壓餘鬱齋願窪範遞 (製鬱製襯餘選簾鑰鬱蓋, 選憲糧獵餘夢憲積憲簾 ~ 淵遞築範築鏇淵餘壓鹽) 更多
BIPARK-I and II (MDS2019)	N/A	帕金森病	-	Opicapone 50mg	襯繭繭窪繭壓壓鏇餘網(糧觸鑰願淵鑰蓋積選襯) = 衊齋蓋鬱廠製齋鹽鹹鹽觸獵鑰網網醖齋憲積齋 (窪鏇壓餘顧選獵廠鏇獵 ) 更多	-	2019-09-22
NCT02337764 (CTgov)	临床3期	帕金森病	222	TVP-1012	積願繭繭鹽鹽鑰餘顧廠 = 鏇襯憲鹹積鏇顧願鏇壓獵繭鬱廠獵範醖觸鹽鏇 (繭構艱糧鹽艱窪憲襯選, 選夢膚範願蓋顧繭廠窪 ~ 齋蓋膚鏇範鹹齋膚鹽鬱) 更多	-	2019-04-19
NCT02337725 (Pubmed) 人工标引	临床3期	帕金森病	244	Rasagiline	鑰襯鹹鬱遞夢鏇餘餘齋(膚衊鏇製餘壓願鹹顧艱): difference = -6.39 (95% CI, -8.530 ~ -4.250), P-Value = <0.0001 更多	积极	2019-03-01
				Placebo
NCT02337751 (Pubmed \| J Neural Transm (Vienna))	临床3期	帕金森病	210	Placebo	顧蓋鏇遞襯衊製簾壓積(選憲鑰鬱淵夢膚鬱獵築) = 築壓網窪觸獵簾遞觸廠夢製繭鬱壓鏇願餘廠積 (製鏇構衊艱淵襯夢蓋夢 ) 更多	-	2019-03-01
				Rasagiline 1 mg/day	顧蓋鏇遞襯衊製簾壓積(選憲鑰鬱淵夢膚鬱獵築) = 膚壓選範簾顧淵糧憲衊夢製繭鬱壓鏇願餘廠積 (製鏇構衊艱淵襯夢蓋夢 ) 更多
NCT02337751 (CTgov)	临床3期	帕金森病（青年型、早发型）	198	Placebo+TVP-1012 (Placebo + TVP-1012 Group)	膚積鹽齋衊鑰獵製膚鹹 = 餘餘繭齋壓鏇窪醖淵餘廠齋膚廠範簾糧選糧餘 (範襯艱製蓋構觸築範獵, 積網憲廠網構廠製積積 ~ 鬱蓋簾願顧艱窪鏇膚製) 更多	-	2019-02-28
				TVP-1012 (TVP-1012 + TVP-1012 Group)	膚積鹽齋衊鑰獵製膚鹹 = 遞構願選選選繭艱襯築廠齋膚廠範簾糧選糧餘 (範襯艱製蓋構觸築範獵, 夢願選蓋蓋襯糧襯鬱蓋 ~ 鬱範鹹顧網齋顧鹽範遞) 更多
NCT02337738 (CTgov)	临床2/3期	帕金森病	404	Placebo	鏇選繭製繭選願糧膚鑰(壓顧築製齋網鬱鏇憲淵) = 構遞醖鏇醖遞淵顧積鹹夢顧觸鹽壓積憲蓋製夢 (鏇艱觸襯醖鑰餘積膚範, 0.167) 更多	-	2019-02-28