A Randomized, Double-blind, Placebo-controlled Trial Comparing the Efficacy and Tolerance of Solriamfetol in Patients Affected with Idiopathic Hypersomnia.

This Phase II clinical trial is a monocenter, double-blind, randomized, placebo-controlled study aimed at evaluate the efficacy and safety of solriamfetol from 75 to 300 mg per day in IH patients.
Patients will be randomized (1:1) to receive either solriamfetol or placebo, with titration, every morning upon awakening during all treatment periods (Day 0 to Week 7).

开始日期2024-09-15

申办/合作机构

University Hospital of Montpellier

NCT06404099 / Recruiting临床2期IIT

RECOVER-SLEEP: A Platform Protocol for Evaluation of Interventions for Sleep Disturbances in Post-Acute Sequelae of SARS-CoV-2 Infection (PASC)

The platform protocol is designed to be flexible so that it is suitable for a range of study settings and intervention types. Therefore, the platform protocol provides a general protocol structure that can be shared by multiple interventions and allows comparative analysis across the interventions. For example, objectives, measures, and endpoints are generalized in the platform protocol, but intervention-specific features are detailed in separate appendices.
This platform protocol is a prospective, multi-center, multi-arm, randomized controlled platform trial evaluating potential interventions for PASC-mediated sleep disturbances. The hypothesis is that symptoms of sleep and circadian disorders that emerge in patients with PASC can be improved by phenotype-targeted interventions. Specific sleep and circadian disorders addressed in this protocol include sleep-related daytime impairment (referred to as hypersomnia) and complex PASC-related sleep disturbance (reflecting symptoms of insomnia and sleep-wake rhythm disturbance).

开始日期2024-08-12

申办/合作机构

Duke University

NCT06568367 / Recruiting临床3期

A Multi-center, Randomized, Double-blind, Placebo-controlled Trial to Assess the Efficacy and Safety of Solriamfetol in Excessive Sleepiness Associated With Shift Work Disorder

SUSTAIN (Studying Solriamfetol Modulation of TAAR-1, Dopamine, and Norepinephrine in Shift Work Disorder) is a Phase 3, multi-center, randomized, double-blind, placebo-controlled, parallel- group trial to assess the efficacy and safety of solriamfetol in adults with excessive sleepiness associated with shift work disorder (SWD).

开始日期2024-08-01

申办/合作机构

Axsome Therapeutics, Inc.

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100 项与索安非托相关的专利（医药）

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108

项与索安非托相关的文献（医药）

2024-12-01·Sleep Medicine: X

Comorbidity of obstructive sleep apnea and narcolepsy: A challenging diagnosis and complex management

Review

作者: Kheirandish-Gozal, Leila ; De Pieri, Marco ; Miano, Silvia

IntroductionNarcolepsy and obstructive sleep apnea syndrome (OSA) are relevant causes of excessive daytime sleepiness (EDS); although different for etiopathogenesis and symptoms, differential diagnosis is sometimes difficult, and guidelines are lacking concerning their management when coexisting in a same patient.MethodsA narrative review of the literature was realized including PubMed, Scopus and Embase, aimed to regroup studies and case reports evaluating epidemiology, clinical and instrumental features and treatment of patients presenting comorbid NT1 and OSA. Moreover, a snowball search on the pathophysiology underpinnings of the association of the two disorder was realized.ResultsFor adults, the prevalence of OSA in NT1 ranged from 24.8 % to 51.4 %. No studies were found concerning the treatment of EDS in double-diagnosis patients, but only case reports; these latter and the experience on patients with either NT or OSA suggest that modafinil, methylphenidate, pitolisant and solriamfetol are effective.DiscussionAdults with NT1 showed a higher prevalence of OSA compared to the general population, but the reach of the results reviewed here is limited by the retrospective design of most of the studies and by the inhomogeneous utilization of diagnostic criteria. The association with OSA is likely to be explained by the involvement of orexin in hypercapnic-hypoxic responses: a deficit of orexin may promote obstructive events during sleep. Open questions warrant further investigation, especially orexin's involvement in other sleep disorders associated with EDS, and the more appropriate treatment for the OSA-narcolepsy comorbidity.

2024-12-01·Sleep Medicine Reviews

Excessive daytime sleepiness in obstructive sleep apnea: Indirect treatment comparison of wake-promoting agents in patients adherent/nonadherent to primary OSA therapy

Review

作者: Zhang, Weijia ; Ye, Hui ; Xiao, Yi ; Wang, Yuxin

There remains an unmet need for a targeted treatment to address residual excessive daytime sleepiness (EDS) in patients with obstructive sleep apnea (OSA) after primary treatment. This network meta-analysis evaluated the efficacy and safety of wake-promoting agents (WPAs), namely solriamfetol, pitolisant, modafinil, and armodafinil, for treating residual EDS in patients with OSA. We conducted a comprehensive search which ultimately included 18 studies in the final analysis. All 4 WPAs demonstrated significant therapeutic benefits for the Epworth sleepiness scale (ESS) and maintenance of wakefulness test (MWT). Based on the surface under the cumulative ranking curve (SUCRA) score, solriamfetol, pitolisant, modafinil and armodafinil were ranked from highest to lowest for the ESS. A similar ranking was observed for MWT, where pitolisant was not included in the analysis. The subgroup analysis also evaluated the efficacy of WPAs in the primary treatment adherent and nonadherent subgroups. Regarding adverse reactions, solriamfetol demonstrated the lowest risk of all-cause discontinuation, whereas pitolisant exhibited minimal risks of adverse events leading to treatment discontinuation and treatment-emergent adverse events. Our analysis comprehensively compared the effects and adverse reactions of different WPAs in treating residual EDS in treated patients with OSA. This has significant implications for the practical clinical use of WPAs and future research.

2024-11-01·Respiratory Medicine and Research

Guidelines for the assessment and management of residual sleepiness in obstructive apnea-hypopnea syndrome

Review

作者: Pépin, Jean-Louis ; Pilette, Charles ; Dauvilliers, Yves ; Boutouyrie, Pierre ; Bequignon, Émilie ; Philip, Pierre ; Gagnadoux, Frédéric ; Patout, Maxime ; Monaca, Christelle ; Geoffroy, Pierre-Alexis ; Baillieul, Sébastien ; Andrejak, Claire ; Barateau, Lucie ; Montani, David ; Tamisier, Renaud ; Trzepizur, Wojciech ; Arnulf, Isabelle ; Micoulaud-Franchi, Jean-Arthur ; Jaffuel, Dany

Excessive daytime sleepiness (EDS) is frequent among patients with obstructive sleep apnea hypopnea syndrome (OSAHS) and can persist despite the optimal correction of respiratory events (apnea, hypopnea and respiratory efforts), using continuous positive airway pressure (CPAP) or mandibular advancement device. Symptoms like apathy and fatigue may be mistaken for EDS. In addition, EDS has multi-factorial origin, which makes its evaluation complex. The marketing authorization [Autorisation de Mise sur le Marché (AMM)] for two wake-promoting agents (solriamfetol and pitolisant) raises several practical issues for clinicians. This consensus paper presents recommendations of good clinical practice to identify and evaluate EDS in this context, and to manage and follow-up the patients. It was conducted under the mandate of the French Societies for sleep medicine and for pneumology [Société Française de Recherche et de Médecine du Sommeil (SFRMS) and Société de Pneumologie de Langue Française (SPLF)]. A management algorithm is suggested, as well as a list of conditions during which the patient should be referred to a sleep center or a sleep specialist. The benefit/risk balance of a wake-promoting drug in residual EDS in OSAHS patients must be regularly reevaluated, especially in elderly patients with increased cardiovascular and psychiatric disorders risks. This consensus is based on the scientific knowledge at the time of the publication and may be revised according to their evolution.

项与索安非托相关的新闻（医药）

2024-10-29

·GlobeNewswire-Health Care

Axsome Therapeutics Presents Data from Multiple Programs Spanning Its Innovative Neuroscience Portfolio at Psych Congress 2024

NEW YORK, Oct. 29, 2024 (GLOBE NEWSWIRE) -- Axsome Therapeutics, Inc. (NASDAQ: AXSM), a biopharmaceutical company developing and delivering novel therapies for the management of central nervous system (CNS) disorders, today announced seven presentations from across its broad portfolio of innovative neuroscience products and product candidates at Psych Congress 2024, being held Oct. 29 - Nov. 2, 2024, in Boston, Massachusetts. Details for the presentations are as follows: Major Depressive Disorder Title: AXS-05 (Auvelity®) in Major Depressive Disorder: Pooled Data from Two Six-Week Controlled Trials (GEMINI and ASCEND)Presentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Craig Chepke, MD, SUNY Upstate Medical UniversityPoster Number: 171 Title: Effects of AXS-05 (Auvelity®) in Improving Anhedonia and Interest-Activity Symptoms of MDD and the Associated Improvements in Functional Impairment Presentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Roger McIntyre, MD, Professor of Psychiatry and Pharmacology at the University of TorontoPoster Number: 172 Title: Real-World Treatment Experiences and Expectations by Symptom Severity in Patients with Major Depressive DisorderPresentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Roger McIntyre, MD, Professor of Psychiatry and Pharmacology at the University of TorontoPoster Number: 198 Alzheimer’s Disease Agitation Title: Clinical Profile of AXS-05 in Treating Alzheimer’s Disease-Related Agitation: Results from The Phase 2/3 Development ProgramPresentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Jeffrey Cummings, MD, ScD, Vice Chair of Research, UNLV Department of Brain HealthPoster Number: 45 OSA and Narcolepsy Title: Solriamfetol for Excessive Daytime Sleepiness in Patients with Narcolepsy and OSA Reporting Anxiety and Depression in the Real-World SURWEY StudyPresentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Ulf Kallweit, MD, Assistant Professor of Neurology at the University Witten/Herdecke, GermanyPoster Number: 20 Cognition Title: Effects of Solriamfetol on Cognition in Obstructive Sleep Apnea with Excessive Daytime Sleepiness and Impaired Cognition in the SHARP Clinical TrialPresentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Yaroslav Winter, MD, Mainz Comprehensive Epilepsy and Sleep Medicine Center, department of neurology, Johannes Gutenberg-University, Mainz, GermanyPoster Number: 92 Title: Effects of Solriamfetol on Cognition in Patients with Excessive Daytime Sleepiness Associated with Narcolepsy in the Real-World SURWEY StudyPresentation Date and Time: Thursday, Oct. 31, 1:30 - 3 p.m. and Friday, Nov. 1, 1:30 - 3 p.m. ETLead Author: Yaroslav Winter, MD, Mainz Comprehensive Epilepsy and Sleep Medicine Center, department of neurology, Johannes Gutenberg-University, Mainz, GermanyPoster Number: 164 About Axsome Therapeutics Axsome Therapeutics, Inc. is a biopharmaceutical company developing and delivering novel therapies for central nervous system (CNS) conditions that have limited treatment options. Through development of therapeutic options with novel mechanisms of action, we are transforming the approach to treating CNS conditions. At Axsome, we are committed to developing products that meaningfully improve the lives of patients and provide new therapeutic options for physicians. For more information, please visit the Company’s website at www.axsome.com. Forward Looking Statements Certain matters discussed in this press release are “forward-looking statements”. The Company may, in some cases, use terms such as “predicts,” “believes,” “potential,” “continue,” “estimates,” “anticipates,” “expects,” “plans,” “intends,” “may,” “could,” “might,” “will,” “should” or other words that convey uncertainty of future events or outcomes to identify these forward-looking statements. In particular, the Company’s statements regarding trends and potential future results are examples of such forward-looking statements. The forward-looking statements include risks and uncertainties, including, but not limited to, the continued commercial success of the Company’s Sunosi® and Auvelity® products and the success of the Company’s efforts to obtain any additional indication(s) with respect to solriamfetol and/or AXS-05; the Company’s ability to maintain and expand payer coverage; the success, timing and cost of the Company’s ongoing clinical trials and anticipated clinical trials for the Company’s current product candidates, including statements regarding the timing of initiation, pace of enrollment and completion of the trials (including the Company’s ability to fully fund the Company’s disclosed clinical trials, which assumes no material changes to the Company’s currently projected revenues or expenses), futility analyses and receipt of interim results, which are not necessarily indicative of the final results of the Company’s ongoing clinical trials, and/or data readouts, and the number or type of studies or nature of results necessary to support the filing of a new drug application (“NDA”) for any of the Company’s current product candidates; the Company’s ability to fund additional clinical trials to continue the advancement of the Company’s product candidates; the timing of and the Company’s ability to obtain and maintain U.S. Food and Drug Administration (“FDA”) or other regulatory authority approval of, or other action with respect to, the Company’s product candidates, including statements regarding the timing of any NDA submission; whether issues identified by FDA in the complete response letter may impact the potential approvability of the Company’s NDA for AXS-07 for the acute treatment of migraine in adults with or without aura, pursuant to the Company’s special protocol assessment for the MOMENTUM clinical trial; the Company’s ability to successfully defend its intellectual property or obtain the necessary licenses at a cost acceptable to the Company, if at all; the successful implementation of the Company’s research and development programs and collaborations; the success of the Company’s license agreements; the acceptance by the market of the Company’s products and product candidates, if approved; the Company’s anticipated capital requirements, including the amount of capital required for the continued commercialization of Sunosi and Auvelity and for the Company’s commercial launch of its other product candidates, if approved, and the potential impact on the Company’s anticipated cash runway; the Company’s ability to convert sales to recognized revenue and maintain a favorable gross to net sales; unforeseen circumstances or other disruptions to normal business operations arising from or related to domestic political climate, geo-political conflicts or a global pandemic and other factors, including general economic conditions and regulatory developments, not within the Company’s control. The factors discussed herein could cause actual results and developments to be materially different from those expressed in or implied by such statements. The forward-looking statements are made only as of the date of this press release and the Company undertakes no obligation to publicly update such forward-looking statements to reflect subsequent events or circumstance. Investors:Mark JacobsonChief Operating Officer(212) 332-3243mjacobson@axsome.com Media:Darren OplandDirector, Corporate Communications(929) 837-1065dopland@axsome.com

2024-10-08

·精准药物

综述｜(2016–2020)上市药物中的分子手性中心构建

Asymmetric Synthesis of US - FDA Approved Drugs over Five Years (2016–2020): A Recapitulation of Chirality” 由 Rekha Tamatam 和 Dongyun Shin 撰写。论文强调了 2016 - 2020 年期间 FDA 批准的手性药物的合成方法，特别关注通过手性诱导、拆分或手性池进行的不对称合成。手性药物具有多种优势，包括：（1）由于更好的药代动力学和药效学性质，手性药物与非手性对应物相比可能具有更高的效力；（2）通过分离特定的对映体，手性药物可以减少不必要的副作用；（3）手性药物可以通过靶向特定的酶或受体来增强药物传递；（4）使用单一异构体可以降低生产成本，从而降低患者的药品价格。一个手性中心的药物的合成方法 1.1. Lifitegrast (2016) ： Lifitegrast 由美国加利福尼亚州布里斯班的 SARcode Bioscience 公司研发，用于治疗干眼症。Lifitegrast 的全合成从市售的手性底物3-溴-L-苯丙氨酸开始，经过10步反应完成，产率为 88%。 1.2. Acalabrutinib (2017)：阿卡拉布替尼由阿塞塔制药公司研发，用于治疗套细胞淋巴瘤（MCL）。从 4-溴苯甲酸（）出发，经过四步反应得到中间体。市售的手性脯氨酸衍生物与通过酰氯进行酰胺化反应，以 86% 的产率生成阿卡拉布替尼。 1.3. Pemafibrate (2017) ：培米贝特由兴和制药公司研发，用于治疗高脂血症。手性片段由对映体纯的（S）-2-羟基丁内酯（）在三甲基硅基碘存在下通过开环反应合成。的氢化还原以及使用2,6-二甲基吡啶进行的三氟甲磺酸酯加成生成。在碳酸钾和乙腈作用下发生构型翻转，以 75%的产率生成培米贝特。 1.4. Letermovir (2017) AiCuris公司开发了莱特莫韦用于治疗巨细胞病毒感染。在尿素环化步骤中，莱特莫韦中引入了一个手性中心。尿素在金鸡纳碱类相转移催化剂存在下，于磷酸钾水溶液和甲苯的双相混合物中发生环化反应，生成喹唑啉酮外消旋体（A12）。 1.5. Netarsudil(2017）艾尔建制药公司开发了奈他舒地尔用于治疗高眼压症。Evans噁唑烷酮（A15）作为手性助剂，随后在过氧化氢存在下被去除。二酯A14进行区域选择性水解，接着通过酰氯形成和酰胺化反应生成酯衍生物A16。用LiHMDS和Boc保护的苯并三唑基甲胺处理Evans噁唑烷酮化合物生成A17，奈他舒地尔的关键立体化学结构通过A17构建。 1.6. Niraparib (2017) 默克公司发现并由泰萨罗公司开发的尼拉帕利，通过酰氯形成和酰胺化反应生成酯衍生物A16。尼拉帕利用于治疗腹膜癌。具有一个手性中心的尼拉帕利从哌啶亚单元获得，由溴苯（A19）合成。亚硫酸氢盐加合物在ATA-302酶催化和吡哆醛-5-磷酸（PLP）共催化下进行转氨酶反应，生成手性哌啶A22。 1.7. Lorlatinib (2018）洛拉替尼由辉瑞公司研发，是一种肿瘤药物。洛拉替尼是一种大环化合物，由手性醇中间体A25构建而成。这个关键步骤涉及使用生物催化剂进行对映选择性还原。 1.8. Elobixibat Hydrate (2018) EA制药公司和持田制药公司开发了依洛昔巴特水合物，用于治疗慢性特发性便秘。在TBTU和甲基（R-2-氨基-2-苯基乙酸A28存在下，通过酸酯偶联生成单一手性碳。 1.9. Tezacaftor (2018) 由Vertex 制药公司发现和开发，特扎卡福是一种广泛作用的囊性纤维化跨膜传导调节因子（CFTR）。它的规模化合成（方案9）从3-氟-4-硝基苯胺A31开始。其区域选择性溴化从3-氟-4-硝基苯胺开始，与N-溴代琥珀酰亚胺（NBS）反应生成中间体A32。市售的（R）-缩水甘油基苄基醚A33通过酸催化开环在苯胺上诱导手性，接着还原硝基得到A34。后续步骤，包括Sonogashira偶联、Larock型环化和酸 - 胺偶联，以84%的产率得到特扎卡福。 1.10. Pyrotinib Maleate (2018) 恒瑞制药研发了马来酸吡咯替尼，它是一种泛ErbB受体酪氨酸激酶抑制剂，用于治疗转移性乳腺癌。马来酸吡咯替尼的千克级合成下图所示。手性片段A37由N-Boc-D-脯氨醇A36经过四步反应合成。 1.11. Encorafenib (2018) 康奈非尼与比美替尼（binimetinib）联合使用，用于治疗转移性黑色素瘤。目前，康奈非尼由辉瑞公司销售。手性的引入方式如下：在碱的存在下，用氯甲酸苄酯和氯甲酸甲酯处理(S)-(−)-1,2-二氨基丙烷二盐酸盐A39，生成氨基甲酸酯衍生物A40。经过氢化后，得到手性亚基A41。 1.12. Duvelisib Monohydrate (2018) Duvelisib一水合物最初由因泰利金（Intellikine）公司开发，后来授权给维瑞斯姆肿瘤公司（Verastem Oncology），用于治疗慢性淋巴细胞白血病和小淋巴细胞淋巴瘤。因泰利金公司公布的Duvelisib一水合物的千克级合成方法在方案12中进行了讨论。用正己基锂处理的韦恩瑞布酰胺（Weinreb amide）A44与苯甲酰胺A43结合，经过四步反应形成手性异喹啉A45。在最后一步中，在甲醇中用D-酒石酸进行盐析，然后用氨水提高A45的对映体纯度。 1.13. Elagolix sodium(2018) 艾拉戈利克斯钠用于治疗子宫内膜异位症女性患者，由艾伯维和神经分泌生物科学公司开发。与度维利塞一水合物类似，在尿嘧啶与甲磺酸酯衍生物进行烷基化的过程中引入手性；后者化合物是由(−)-N-叔丁氧羰基-D-α-苯甘氨醇与甲磺酰氯反应合成。 1.14. Tegoprazan (2018) 泰戈泊扎兰最初由辉瑞公司发现，后由乐化制药和CJ医疗进一步开发，用于治疗胃食管反流病（GERD）。泰戈泊扎兰的可扩展合成方法如方案14所示。在三正丁基膦和1,1′-(偶氮二甲酰)二哌啶（ADDP）存在下，在苯并咪唑环上引入对映纯的苯并二氢吡喃醇侧链A53是合成的关键步骤。然后，3,5-二氟苯酚（A50）与丙炔酸甲酯发生缩合反应，生成E式和Z式（1:1混合物）的烯醇醚（A51）。接着进行氢化，随后进行分子内傅克酰基化反应，并用硼杂噁唑烷催化剂（A52）进行不对称还原，生成苯并二氢吡喃醇（A53）。最后，对后者进行重结晶，得到对映纯的手性亚基A53。 1.15. Alpelisib (2019) 诺华制药开发了阿培利司。它用于治疗转移性乳腺癌。在合成的最后一步中，在三乙胺存在下，通过L-脯氨酸酰胺A56在A55的咪唑环上引入手性中心（方案15）。 1.16. Solriamfetol (2019) 索利氨酯由 SK 生物制药公司开发，用于治疗与阻塞性睡眠呼吸暂停（OSA）和发作性睡病相关的埃勒斯-当洛斯综合征（EDS）。索利氨酯的千克级合成如方案16所示。在酸的存在下，由D-苯丙氨醇（A58）和氰酸钠一步合成索利氨酯，产率为89%。 1.17. Pretomanid (2019) 普瑞玛尼是一种抗分枝杆菌药物，用于治疗结核病（TB）。它是结核病联盟开发的首个抗结核药物。环氧化物A61在二异丙基乙胺存在下与前手性硝基咪唑A60偶联，发挥其作为手性底物的作用，生成A62。 1.18. Zanubrutinib (2019) 百济神州开发了泽布替尼用于治疗套细胞淋巴瘤。与上述的手性库方法不同，泽布替尼是首个通过手性拆分方法生产的药物。泽布替尼通过用L-二苯甲酰酒石酸（LDBTA）处理，以拆分方法获得其纯对映体形式。 1.19. Darolutamide (2019) 达罗他胺用于治疗非转移性去势抵抗性前列腺癌。它由奥立安集团和拜耳医药保健有限公司开发。达罗他胺不对称合成的关键步骤是将手性异丙胺片段插入到的联芳基骨架中，然后通过酸介导脱除片段上的 Boc 保护基，生成中间体A68。 1.20. Cenobamate (2019) SK制药公司开发了西诺巴胺，用于治疗部分性发作癫痫。方案20中展示的酶催化过程概述了其在胶红酵母（一种氧化还原酶）存在下的不对称催化氢化。 1.21. Avapritinib (2020) 通过手性拆分（Chiralresolution）A73。Blueprint医药开发了阿伐替尼（avapritinib），用于治疗转移性胃肠道癌症。通过超临界流体色谱分离中间体A73进行手性拆分，以68%的产率生成对映纯的阿伐替尼。 1.22. Berotralstat (2020) 贝罗司他用于预防遗传性血管性水肿（HAE）发作。与阿伐替尼的合成方法相同，在最后一步通过超临界流体色谱法以纯对映体形式合成贝罗司他。 1.23. Lonafarnib (2020) 洛那法尼用于治疗哈钦森-吉尔福德早衰症综合征（HGPS）。与贝罗司他不同，洛那法尼的手性是通过手性分离获得的。中间体A77经二异丁基氢化铝（DIBAL）还原后进行手性分离，生成具有一个立体中心的手性亚基A78。这些连续的步骤产生洛那法尼。 1.24. Osilodrostat (2020）奥西卓司他用于治疗库欣病，是一种11β-羟化酶抑制剂。手性奥西卓司他的生成方式与贝罗司他类似。中间体A80通过手性高效液相色谱（HPLC）分离直接生成药物。 1.25. Oliceridine (2020) 奥利塞林，一种中枢神经系统（CNS）药物，用于治疗中度至重度急性疼痛。在奥利塞林的全合成中，手性中间体A83通过A82的脱羧反应获得，随后进行超临界流体色谱（SFC）手性分离。 1.26. Remimazolam (2020) Acacia制药公司开发了瑞马唑仑，一种超短效苯二氮䓬类药物。在氯仿中用手性底物A86处理A85，生成了取代产物，该产物经过碱促进的F-moc脱保护和乙酸促进的缩合反应，经过三步生成环化中间体A87。 1.27. Ozanimod (2020) 奥扎尼莫德用于治疗复发型多发性硬化症。手性亚磺酰胺片段A90作为手性辅助基团，通过在A91的茚上插入一个手性中心来发挥作用（方案27）。片段A90与茚衍生物A89作为手性辅助基团，通过在茚上插入一个手性中心来发挥作用。奥扎尼莫德由中间体通过连续步骤合成A91. 两个手性中心的药物的合成方法未完待续！声明：发表/转载本文仅仅是出于传播信息的需要，并不意味着代表本公众号观点或证实其内容的真实性。据此内容作出的任何判断，后果自负。若有侵权，告知必删！长按关注本公众号粉丝群/投稿/授权/广告等请联系公众号助手觉得本文好看，请点这里↓

申请上市上市批准

2024-09-24

·GlobeNewswire-Health Care

Axsome Therapeutics Presents Data from Multiple Programs at Sleep Europe 2024

Seven presentations highlight the Company’s growing CNS portfolio and commitment to improving treatment outcomes for patients with sleep disordersNEW YORK, Sept. 24, 2024 (GLOBE NEWSWIRE) -- Axsome Therapeutics, Inc. (NASDAQ: AXSM), a biopharmaceutical company developing and delivering novel therapies for the management of central nervous system (CNS) disorders, today announced seven presentations on AXS-12 and solriamfetol at Sleep Europe 2024, the 27th Congress of the European Sleep Research Society, being held September 24-27, 2024, in Seville, Spain. Featured presentations include data from the SYMPHONY Phase 3 trial of AXS-12 in narcolepsy, findings from the CRESCENDO patient survey underscoring the unmet needs of patients with type 1 narcolepsy, and previously reported data on solriamfetol demonstrating improvement in cognitive function in patients with excessive daytime sleepiness (EDS) associated with OSA and narcolepsy. Details for the presentations are as follows: AXS-12: Title: AXS-12 for the Treatment of Narcolepsy: Topline Results from the Phase 3 SYMPHONY TrialPoster Presentation Date and Time: Wednesday, September 25, 12:15 - 1:15 p.m. and 4:00 - 5:45 p.m. CESTLead Author: Michael Thorpy, MD, Director of the Sleep-Wake Disorders Center at the Montefiore Medical Center and Professor of Neurology at Albert Einstein College of Medicine, New York, NY, USAPoster Number: P254 Title: CRESCENDO: Results from a Survey of Symptom Burden and Quality of Life in Patients with Narcolepsy Type 1Poster Presentation Date and Time: Wednesday, September 25, 12:15 - 1:15 p.m. and 4:00 - 5:45 p.m. CESTLead Author: Michael Thorpy, MD, Director of the Sleep-Wake Disorders Center at the Montefiore Medical Center and Professor of Neurology at Albert Einstein College of Medicine, New York, NY, USAPoster Number: P265 Solriamfetol: Title: Solriamfetol and Maintenance of Wakefulness Outcomes in Patients with Narcolepsy and Obstructive Sleep ApneaOral Presentation Date and Time: Tuesday, September 24, 9:55 - 10:01 a.m. CEST Poster Presentation Date and Time: Wednesday, September 25, 12:15 - 1:15 p.m. and 4:00 - 5:45 p.m. CESTLead Author: Michael Thorpy, MD, Director of the Sleep-Wake Disorders Center at the Montefiore Medical Center and Professor of Neurology at Albert Einstein College of Medicine, New York, NY, USAPoster Number: P475 Title: Effects of Solriamfetol on Cognition in Patients with Excessive Daytime Sleepiness Associated with NarcolepsyPoster Presentation Date and Time: Wednesday, September 25, 12:15 - 1:15 p.m. and 4:00 - 5:45 p.m. CESTLead Author: Yaroslav Winter, MD, Mainz Comprehensive Epilepsy and Sleep Medicine Center, Department of Neurology, Johannes Gutenberg-University, Mainz, GermanyPoster Number: P197 Title: Real-world Use of Solriamfetol for Excessive Daytime Sleepiness in Patients Reporting Anxiety or DepressionPoster Presentation Date and Time: Friday, September 27, 10:45 a.m. - 1:30 p.m. CESTLead Author: Yaroslav Winter, MD, Mainz Comprehensive Epilepsy and Sleep Medicine Center, Department of Neurology, Johannes Gutenberg-University, Mainz, Germany Poster Number: P198 Title: SURWEY: Treatment of Excessive Daytime Sleepiness with Solriamfetol: Initiation, Titration, and OutcomePoster Presentation Date and Time: Thursday, September 26, 12:00 - 1:30 p.m. and 5:30 – 6:45 p.m. CESTLead Author: Samantha Floam, DMD, Axsome TherapeuticsPoster Number: P799 Title: Effects of Solriamfetol on Cognition in Obstructive Sleep Apnea with Excessive Daytime Sleepiness and Impaired CognitionPoster Presentation Date and Time: Friday, September 27, 10:45 a.m. - 1:30 p.m. CESTLead Author: Hans Van Dongen, PhD, Professor at Washington State University Poster Number: P1248 About Axsome Therapeutics Axsome Therapeutics, Inc. is a biopharmaceutical company developing and delivering novel therapies for central nervous system (CNS) conditions that have limited treatment options. Through development of therapeutic options with novel mechanisms of action, we are transforming the approach to treating CNS conditions. At Axsome, we are committed to developing products that meaningfully improve the lives of patients and provide new therapeutic options for physicians. For more information, please visit the Company’s website at www.axsome.com. Forward Looking Statements Certain matters discussed in this press release are “forward-looking statements”. The Company may, in some cases, use terms such as “predicts,” “believes,” “potential,” “continue,” “estimates,” “anticipates,” “expects,” “plans,” “intends,” “may,” “could,” “might,” “will,” “should” or other words that convey uncertainty of future events or outcomes to identify these forward-looking statements. In particular, the Company’s statements regarding trends and potential future results are examples of such forward-looking statements. The forward-looking statements include risks and uncertainties, including, but not limited to, the continued commercial success of the Company’s Sunosi® and Auvelity® products and the success of the Company’s efforts to obtain any additional indication(s) with respect to solriamfetol and/or AXS-05; the Company’s ability to maintain and expand payer coverage; the success, timing and cost of the Company’s ongoing clinical trials and anticipated clinical trials for the Company’s current product candidates, including statements regarding the timing of initiation, pace of enrollment and completion of the trials (including the Company’s ability to fully fund the Company’s disclosed clinical trials, which assumes no material changes to the Company’s currently projected revenues or expenses), futility analyses and receipt of interim results, which are not necessarily indicative of the final results of the Company’s ongoing clinical trials, and/or data readouts, and the number or type of studies or nature of results necessary to support the filing of a new drug application (“NDA”) for any of the Company’s current product candidates; the Company’s ability to fund additional clinical trials to continue the advancement of the Company’s product candidates; the timing of and the Company’s ability to obtain and maintain U.S. Food and Drug Administration (“FDA”) or other regulatory authority approval of, or other action with respect to, the Company’s product candidates, including statements regarding the timing of any NDA submission; whether issues identified by FDA in the complete response letter may impact the potential approvability of the Company’s NDA for AXS-07 for the acute treatment of migraine in adults with or without aura, pursuant to the Company’s special protocol assessment for the MOMENTUM clinical trial; the Company’s ability to successfully defend its intellectual property or obtain the necessary licenses at a cost acceptable to the Company, if at all; the successful implementation of the Company’s research and development programs and collaborations; the success of the Company’s license agreements; the acceptance by the market of the Company’s products and product candidates, if approved; the Company’s anticipated capital requirements, including the amount of capital required for the continued commercialization of Sunosi and Auvelity and for the Company’s commercial launch of its other product candidates, if approved, and the potential impact on the Company’s anticipated cash runway; the Company’s ability to convert sales to recognized revenue and maintain a favorable gross to net sales; unforeseen circumstances or other disruptions to normal business operations arising from or related to domestic political climate, geo-political conflicts or a global pandemic and other factors, including general economic conditions and regulatory developments, not within the Company’s control. The factors discussed herein could cause actual results and developments to be materially different from those expressed in or implied by such statements. The forward-looking statements are made only as of the date of this press release and the Company undertakes no obligation to publicly update such forward-looking statements to reflect subsequent events or circumstance. Investors:Mark JacobsonChief Operating Officer(212) 332-3243mjacobson@axsome.com Media:Darren OplandDirector, Corporate Communications(929) 837-1065dopland@axsome.com

临床3期

100 项与索安非托相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11328	索安非托	N06BA14	DB14754

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
发作性睡病	美国	Axsome Malta Ltd.	2019-03-20
阻塞性睡眠呼吸暂停综合征	美国	Axsome Malta Ltd.	2019-03-20
白天过度嗜睡	加拿大	Jazz Pharmaceuticals Ireland Ltd.	-

未上市

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适应症	最高研发状态	国家/地区	公司	日期
特发性睡眠过度	临床2期	德国	Jazz Pharmaceuticals Plc	2015-05-01
特发性睡眠过度	临床2期	瑞典	Jazz Pharmaceuticals Plc	2015-05-01
特发性睡眠过度	临床前	美国	Jazz Pharmaceuticals Plc	2015-05-01
特发性睡眠过度	临床前	芬兰	Jazz Pharmaceuticals Plc	2015-05-01
特发性睡眠过度	临床前	法国	Jazz Pharmaceuticals Plc	2015-05-01
特发性睡眠过度	药物发现	加拿大	Jazz Pharmaceuticals Plc	2015-05-01
特发性睡眠过度	药物发现	荷兰	Jazz Pharmaceuticals Plc	2015-05-01
发作性睡病	药物发现	加拿大	Jazz Pharmaceuticals Plc	2015-05-01
发作性睡病	药物发现	芬兰	Jazz Pharmaceuticals Plc	2015-05-01
发作性睡病	药物发现	荷兰	Jazz Pharmaceuticals Plc	2015-05-01

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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


NCT04839562 (CTgov)	临床2/3期	注意缺陷障碍伴多动	66	Solriamfetol 75 MG (Solriamfetol)	鏇淵鹽鬱築願蓋鬱鬱製(顧廠衊顧鏇製鏇廠蓋壓) = 構壓醖鑰襯壓艱壓製糧夢構齋繭糧艱鬱壓艱積 (衊憲衊鏇窪夢齋顧糧獵, 夢遞餘願壓製憲蓋構艱 ~ 顧齋繭艱積糧鹽襯廠齋) 更多	-	2024-03-04
				Placebo (Placebo)	鏇淵鹽鬱築願蓋鬱鬱製(顧廠衊顧鏇製鏇廠蓋壓) = 築積窪艱醖艱膚壓鏇艱夢構齋繭糧艱鬱壓艱積 (衊憲衊鏇窪夢齋顧糧獵, 夢壓艱蓋艱淵遞繭簾簾 ~ 鏇簾範鑰願淵廠膚鹽窪) 更多
WSC2023	N/A	白天过度嗜睡	-	Solriamfetol 150 mg/day	(衊鹹餘繭餘願齋憲襯艱) = 3.4% 鑰積壓觸鹹糧顧築蓋鬱 (艱蓋齋製襯選獵遞鬱衊 ) 更多	-	2023-10-25
				Placebo
WSC2023	N/A	阻塞性睡眠呼吸暂停综合征	-	Solriamfetol 37.5 mg/day	(構築鹽醖鏇襯願蓋鏇窪) = Common adverse effects were headache 餘夢範觸獵選齋醖築窪 (壓構壓餘夢構鹹壓餘築 ) 更多	-	2023-10-24
				Solriamfetol 75 mg/day
Pubmed	N/A	发作性睡病 \| 阻塞性睡眠呼吸暂停综合征	-	Solriamfetol 37.5 mg	(遞簾製構鑰製糧簾鹹鬱) = No weight-related treatment-emergent adverse events were serious 醖範窪積襯廠製艱觸壓 (積製製淵鬱鏇糧衊鏇繭 )	-	2022-08-14
				Solriamfetol 75 mg
NCT02348593 \| NCT02348606 (Pubmed \| J Clin Sleep Med)	N/A	发作性睡病 \| 白天过度嗜睡	-	Solriamfetol 37.5 mg	(鏇鹽獵鹹窪艱衊窪淵構) = 願壓憲壓壓艱糧憲顧築簾構艱獵糧醖夢憲構夢 (鬱齋簾鏇醖繭夢遞顧廠 ) 更多	-	2021-07-20
				Solriamfetol 150 mg	(簾衊壓鏇艱鬱積廠鏇製) = 淵鏇積築積鬱繭網範顧簾襯鹹壓顧衊遞獵鬱繭 (願觸積衊範夢壓觸範齋 )
NCT03037203 (Pubmed \| Mov Disord)	临床2期	白天过度嗜睡	66	Solriamfetol 300 mg/d	(願糧夢鏇鹹鑰選鏇廠遞) = 5.4% 鬱願醖淵膚夢壓窪衊鬱 (構蓋蓋窪鹽鏇鏇壓製網 ) 更多	-	2021-06-30
NCT02348606 (Pubmed)	临床3期	白天过度嗜睡	476	Solriamfetol 37.5 mg/d	憲積糧憲鬱鏇構膚鏇憲(願簾膚艱窪顧築網簾觸) = 願膚鏇築淵鏇觸夢鹹窪構醖廠鏇顧選製鬱淵餘 (鑰齋獵鑰獵鏇齋觸繭窪, 0.6 ~ 9.0)	-	2021-02-22
				Solriamfetol 75 mg/d	憲積糧憲鬱鏇構膚鏇憲(願簾膚艱窪顧築網簾觸) = 衊夢夢餘積鏇顧蓋範築構醖廠鏇顧選製鬱淵餘 (鑰齋獵鑰獵鏇齋觸繭窪, 4.3 ~ 12.5)
NCT02806908 (2274, CTgov)	临床2期	发作性睡病 \| 特发性睡眠过度	24	Placebo (Placebo)	築蓋衊夢觸夢廠選顧淵(齋膚衊觸廠鹽範蓋膚獵) = 膚糧壓範衊製餘顧衊壓構壓網壓繭襯鹹壓積蓋 (遞鹹網築淵蓋築遞醖鬱, 網窪製範窪壓鑰窪獵淵 ~ 憲壓繭襯遞製鑰淵觸顧) 更多	-	2021-01-13
				JZP-110 (JZP-110)	築蓋衊夢觸夢廠選顧淵(齋膚衊觸廠鹽範蓋膚獵) = 鹹鹹鹹繭襯壓壓願醖遞構壓網壓繭襯鹹壓積蓋 (遞鹹網築淵蓋築遞醖鬱, 鹹積餘廠蓋夢鬱襯遞廠 ~ 繭襯醖選遞觸醖糧蓋糧) 更多
NCT02348593 \| NCT02348606 (TONES 3, Pubmed \| J Clin Sleep Med)	临床3期	发作性睡病 \| 阻塞性睡眠呼吸暂停综合征	-	Solriamfetol 37.5 mg	壓鬱鏇願網構壓製鬱齋(簾鏇積艱遞蓋艱齋鏇築) = 壓鏇願繭壓餘壓遞齋夢選願餘鏇簾鏇願鹽製餘 (衊鏇築鏇鏇鑰網餘積衊 )	-	2020-11-23
				Solriamfetol 75 mg	壓鬱鏇願網構壓製鬱齋(簾鏇積艱遞蓋艱齋鏇築) = 積築蓋壓餘鹽觸蓋積夢選願餘鏇簾鏇願鹽製餘 (衊鏇築鏇鏇鑰網餘積衊 )