Cenobamate (YKP3089) is a small molecule approved in the United States (US), Europe and several other countries around the world for the treatment of Partial-Onset (focal) seizures in adult subjects (≥18 years of age). In the US it is approved for use as monotherapy, however, there is little clinical data assessing its use as monotherapy in adults with POS. This study is designed to explore the effectiveness of doses of 100 mg/day and 200 mg/day as monotherapy in adult subjects with newly diagnosed or recurrent POS/focal onset epilepsy.

开始日期2024-10-14

申办/合作机构

SK Life Science, Inc.

NCT06352723 / Not yet recruiting早期临床1期IIT

Use of Cenobamate in the Intensive Care Unit for Acute Frequent Seizures and Status Epilepticus

The CENOBITE study will be conducted as a multi-center trial involving X leading centers from the Critical Care EEG Monitoring Consortium (CCEMRC). A total of 10 patients will be recruited over a period of one year, with each patient undergoing monitored treatment regimen. Each site will obtain its own approval from their institutional review board. Data will be shared through the MGB REDCap; raw EEG files will be shared through the MGB Dropbox and analyzed at the BWH.
Monitoring for the development of Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) syndrome, a potential adverse reaction, will be a key aspect of the study. Regular assessments, including RegiSCAR scoring (a validated scoring system for DREeSS5), daily serum cenobamate level measurements, and comprehensive lab tests, will be conducted to ensure patient safety and the effective management of any adverse reactions such as DRESS syndrome.

开始日期2024-04-01

申办/合作机构

The Brigham & Women's Hospital, Inc.

CTIS2023-506841-52-00 / Recruiting

Open-Label Safety and Efficacy Study of Cenobamate (YKP3089) in Pediatric Subjects with Partial-onset (Focal) Seizures - YKP3089C040

开始日期2023-04-19

申办/合作机构

SK Life Science, Inc.

100 项与 Cenobamate 相关的临床结果

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100 项与 Cenobamate 相关的转化医学

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100 项与 Cenobamate 相关的专利（医药）

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项与 Cenobamate 相关的文献（医药）

2024-12-01·Pediatric Neurology

Cenobamate's Efficacy for Seizure Treatment in Tuberous Sclerosis Complex

Article

作者: Franz, David N ; Horn, Paul ; Horn, Porn ; Krueger, Darcy ; Aungaroon, Gewalin ; Franz, David N. ; Cooke, Alexander ; Ritter, David

BACKGROUNDEpilepsy is prevalent, and seizure control is challenging in patients with tuberous sclerosis complex (TSC). Cenobamate (CBM) has proven efficacy in several studies; however, its benefit in the TSC population is not known.METHODSWe performed a retrospective review of patients with TSC who received adjunctive CBM for seizure treatments. We assessed treatment efficacy by comparing seizure frequencies three months before CBM (baseline) and those at 3-, 6-, 12-, and 18- month follow-ups.RESULTSWe identified 70 patients with TSC receiving CBM and excluded 16 with insufficient data. Fifty-four patients aged 2 to 39 years, with an average baseline seizure of 66.1 ± 88.9 per month, were analyzed. Treatment retention rates at 3, 6, 12, and 18 months were 94.4%, 79.6%, 66.7%, 44.4%, and responder rates (proportions of patients who remained on treatment and had ≥50% seizure reduction) were 38.1%, 51.7%, 53.1%, and 59.1%, respectively. Seizure-free rates at these respective follow-ups were 7.1%, 13.8%, 6.3%, and 9.1%. For patients experiencing reduced seizures, the mean percentage of change ranged from 61.5% to 74.6%. Side effects were common (64.8%), particularly sedation (42.6%), behavioral disturbance (24.1%), and gastrointestinal disturbance (22.2%).CONCLUSIONSMost patients in this study showed seizure reduction; however, the overall responder and seizure-free rates were lower than the literature, likely due to the unique underlying epileptogenesis in TSC and the challenges of tolerating CBM. The lower treatment retention rates signal areas for improvement in concurrent medication adjustment practices.

2024-12-01·CNS Drugs

Recent Advances in Pharmacologic Treatments of Drug-Resistant Epilepsy: Breakthrough in Sight

Review

作者: Friedman, Daniel ; Klein, Pavel ; Kwan, Patrick

Epilepsy affects approximately 1% of the world population. Patients have recurrent seizures, increased physical and psychiatric comorbidities, and higher mortality rate than the general population. Over the last 40 years, research has resulted in 20 new antiseizure medications (ASMs) approved between 1990 and 2018. In spite of this, up to one-third of patients (~ 1 million patients in the USA) have drug-resistant epilepsy (DRE), with little change between 1982 and 2018, a period of intense new ASM development. A minority of patients with DRE may benefit from surgical treatment, but this specialized care remains challenging to scale. Therefore, the greatest hope for breakthroughs for patients with DRE is in pharmacologic therapies. Recently, several advances promise to change the outcomes for patients with DRE. Cenobamate, a drug with dual mechanisms of modulating sodium channel currents and GABA-A receptors, achieves 90-100% seizure reduction in 25-33% of patients with focal DRE, a response not observed with other ASMs. Fenfluramine, a serotonin-acting drug, dramatically reduces the frequency of convulsive seizures in Dravet syndrome, a devastating developmental epileptic encephalopathy with severe DRE. Both drugs reduce mortality. In addition, the possibility of DRE prevention was recently raised in patients with tuberous sclerosis complex, a relatively common genetic form of epilepsy. A paradigm shift is emerging in the treatment of epilepsy. Seizure freedom has become attainable in a significant proportion of patients with focal DRE, and dramatic seizure reduction has been achieved in a developmental encephalopathy. Coupled with a rich pipeline of new compounds under clinical development, the long sought-after breakthrough in the treatment of epilepsy may finally be in sight.

2024-12-01·Pediatric Neurology

Mammalian Target of Rapamycin Inhibitor Levels Decrease Under Cenobamate Treatment

Article

作者: Ritter, David M ; Ritter, David M. ; Franz, David Neal ; Agricola, Karen ; Becker, Lena-Luise ; Krueger, Darcy A ; Krueger, Darcy A.

BACKGROUNDEverolimus therapy has been approved in Tuberous Sclerosis Complex (TSC), for drug-resistant epilepsy as adjunctive therapy. A novel anti-seizure medication is cenobamate, which was approved for adults as adjunctive treatment for focal-onset seizures in drug-resistant epilepsy and is now commonly used in patients with TSC. Drug-drug interactions between cenobamate and mammalian target of rapamycin (mTORi) have not been prospectively evaluated, even though these agents are frequently administered together.METHODSWe performed a retrospective analysis of patients with TSC and compared mTORi drug levels before and after treatment initiation with cenobamate.RESULTSWe evaluated 20 patients with clinically diagnosed TSC (male: 55%, female: 45%) with a median current age at last visit of 17.0 years (range: 4-41 years, interquartile range [IQR]: 12.5 years). All patients received mTORi treatment of either everolimus (N = 12, 60%) or sirolimus (N = 8, 40%). Cenobamate treatment led to seizure freedom in 2 patients (10%), reduction of seizures in 9 patients (45%) and no change in seizure frequency in 9 patients (45%). Median maximal cenobamate dose was 200 mg (range: 100-500 mg, IQR: 262.5 mg), for example, 3.2 mg/kg/day (range: 0.8-9.5 mg/kg/day, IQR: 3.2 mg/kg/day). Median everolimus levels decreased significantly after cenobamate initiation from 5.1 ng/ml (range: 1.9-11.6 ng/ml, IQR: 3.8 ng/ml) to 3.4 ng/ml (range: 1-7.9 ng/ml, IQR: 1.7 ng/ml, P = 0.01221). The median sirolimus level did not decrease significantly (P = 0.3828).CONCLUSIONEverolimus levels decreased following cenobamate initiation. This is likely due to CYP3A4 induction of cenobamate. We recommend monitoring of serum plasma levels of mTORi co-administered with cenobamate and adjustment of mTORi doses accordingly.

项与 Cenobamate 相关的新闻（医药）

2024-11-19

·PRNewswire

SK Biopharmaceuticals Seals 1st Actinium-225-Based Collaborative Research Agreement with Korea Institute of Radiological and Medical Sciences as Steps Toward Becoming Global Radiopharmaceutical Therapy Player

SK Biopharmaceuticals, Korea Institute of Radiological and Medical Sciences collaborate on discovering and developing radiopharmaceutical drug candidates using an alpha-particle emitting radioisotope, actinium-225, for potential cancer treatments The two sides aim to submit an Investigational New Drug application by 2027, in line with SK Biopharmaceuticals' roadmap to strengthen its radiopharmaceutical therapy business SK Biopharmaceuticals further accelerates the expansion of its radiopharmaceutical therapy pipeline and capability, via strengthened internal resources and partnerships SEOUL, South Korea, Nov. 18, 2024 /PRNewswire/ -- SK Biopharmaceuticals, a biotech company, announced that it has entered into an agreement with the Korea Institute of Radiological and Medical Sciences (KIRAMS), Korea's premier research institution dedicated to the study and advancement of radiological and medical sciences, to collaborate on discovering and developing preclinical radiopharmaceutical drug candidates. This marks the first collaborative research agreement in which both sides will aim to discover radiopharmaceutical compounds and investigate novel oncological treatments, using actinium-225 (225Ac), an alpha-particle emitting radioisotope that selectively kills cancer cells. The research for radiopharmaceutical therapy (RPT) focuses on this application that has been gaining attention for its high potential in nuclear medicine. SK Biopharmaceuticals has already initiated its 225Ac-based research as it secured a supply of the radioisotope from TerraPower Isotopes, a subsidiary of TerraPower, a nuclear innovation company whose investors include SK Biopharmaceuticals' parent SK Inc. and Bill Gates. SK Biopharmaceuticals and KIRAMS will seek to submit an Investigational New Drug application by 2027, as they leverage each other's resources to optimize their drug discovery efforts. SK Biopharmaceuticals said it could significantly reduce the time and cost of new drug development, with KIRAMS' researchers, facilities and equipment using the radioisotope, enabling the company to further accelerate in securing and expanding its RPT pipeline and capability. The agreement is in line with SK Biopharmaceuticals' so-called "RPT Roadmap" recently introduced to become a global leading RPT player by 2027, as the company will fortify its RPT business by discovering new drug compounds, extending supply and production capacities, and developing a tech platform, via strengthened internal assets and strategic partnerships. In addition to the 225Ac supply agreement aligned with its roadmap, the company has in-licensed SKL35501 (FL-091) radiopharmaceutical compound targeting neurotensin receptor 1 (NTSR1) solid tumors. Jinkyung Lee, President of KIRAMS, stated, "Through this joint research agreement, we aim to take a leading role in developing innovative radiopharmaceutical therapeutics, in alignment with the Ministry of Science and ICT's strategic initiative to drive advancements in Radiation Biology. We look forward to contributing to the growth of the domestic radiopharmaceutical industry in close collaboration with SK Biopharmaceuticals." Donghoon Lee, CEO and President of SK Biopharmaceuticals, said "This agreement is one of key steps in enhancing SK Biopharmaceuticals' research capabilities. We will seek to spur SK Biopharmaceuticals to become a leading global RPT player through strengthened ties." About SK Biopharmaceuticals SK Biopharmaceuticals focuses on the research, development and commercialization of treatments for disorders of the central nervous system (CNS) and oncology. In 2017, SK Biopharmaceuticals established a research center to begin its expansion into oncology through research and development efforts. SK Biopharmaceuticals is the first and only Korean company to independently develop and commercialize an antiseizure medication, cenobamate (brand name: XCOPRI®) in the U.S. More than 100,000 patients have been treated globally with cenobamate, developed by SK Biopharmaceuticals and its U.S. subsidiary SK Life Science, Inc., since its launch in the U.S. in 2020. Cenobamate has successfully entered five major regions: North America, Europe, Asia, Central and South America, and the Middle East and North Africa. The company also has a pipeline of eight compounds in development in both CNS disorders and oncology. Additionally, SK Biopharmaceuticals is focused on the discovery of new treatments in oncology. For more information, visit SK Biopharmaceuticals' website at , and SK Life Science's website at . About Korea Institute of Radiological and Medical Sciences As a premier institution dedicated to the intersection of science, technology, and healthcare, the Korea Institute of Radiological and Medical Sciences (KIRAMS) is at the forefront of radiation medicine innovation. Ever since KIRAMS opened its doors as a radiation medicine research center in 1963, we have been contributing to the national development of science and technology, and to the promotion of the health of the people, based on our research in medical uses of radiation. By bringing the very first Cobalt-60 radiotherapy machine for cancer treatment to Korea in 1963, we were able to greatly increase the number of completely cured cancer patients. Following the restructuring of a cancer hospital in 1973, KIRAMS was leading domestic cancer treatment until the 1990s, by introducing diagnostic and treatment technologies that incorporated advanced science. In 2007, we became an independent institution, directly under the Ministry of Science and ICT, and since then we have established "Radiation Medicine" as a separate field of research and distinguished ourselves from other medical institutes by expanding the National Radiation Emergency Medical Center. And now, going beyond our original mission of defeating cancer, KIRAMS is evolving into a public institution committed to solving new problems for the country and for society, as well as for the benefit of the people. In other words, we are opening new horizons in radiation medicine by supporting specialized, research-centric hospitals engaged in advanced biomedical R&D, by consolidating research and detection of radiation in everyday life, which has recently become a social issue, and by establishing and operating the new Radioisotope Center for Pharmaceuticals to promote the research and use of radioisotopes for medical purposes. Leveraging our extensive experience and our accomplishments, we here at the Korea Institute of Radiological and Medical Sciences will not rest but continually develop into the number one specialist institute for radiotherapy trusted by the people. For more information, visit . SOURCE SK Biopharmaceuticals Co., Ltd WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

放射疗法上市批准临床研究

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

2024-07-17

·FierceBiotech

SK inks $572M deal for Full-Life prospect, advancing push to become Asia’s radiopharma leader

The deal is part of a broader expansion into radiopharmaceuticals. SK Biopharmaceuticals has followed through on its promise to place big bets in a bid to become Asia’s radiopharma leader. The Korean biotech got the ball rolling by striking a $571.5 million biobucks deal to license a drug candidate in development at Full-Life Technologies. Today, SK’s pipeline and portfolio is focused on central nervous system disorders, with the epilepsy drug Xcopri leading the charge. But the biotech is making a concerted effort to branch out. One year ago, SK outlined plans to expand in oncology and identified radiopharmaceuticals as one of the modalities at the heart of the push. SK is joining a who’s who of Big Pharma companies on the hunt for radiopharma deals. The expansion plan led SK to Full-Life, a radiotherapeutics biotech with operations in Belgium, Germany and China. Specifically, SK has plucked the NTSR1-directed radionuclide drug conjugate program FL-091 from Full-Life’s pipeline. NTSR1 is overexpressed in tumors including colorectal, breast, pancreatic, and head and neck cancers, leading Full-Life to identify the neurotensin receptor as a potential target for a radioligand. The biotech recently published preclinical data on FL-091. The public pipeline of Full-Life, which has a PSMA program in human testing, puts FL-091 on the cusp of clinical development. SK has secured global rights to take FL-091 forward through a deal worth up to $571.5 million in upfront and milestone payments. Neither party has disclosed the size of the upfront payment. The deal gives SK the right of first negotiation to license other pre-selected Full-Life programs. The deal is part of a broader expansion into radiopharmaceuticals. SK CEO Donghoon Lee used the press release about the deal to tease the unveiling and implementation of radiopharmaceutical business plans later this year. The company put another piece of its oncology strategy in place in 2023 when it bought a 60% stake in Proteovant Therapeutics to add protein degradation capabilities and a cancer R&D center.

并购蛋白降解靶向嵌合体引进/卖出

100 项与 Cenobamate 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11150	Cenobamate	N03A	DB06119

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
癫痫	挪威	Angelini Pharma, Inc.	2021-03-26
癫痫	欧盟	Angelini Pharma, Inc.	2021-03-26
癫痫	冰岛	Angelini Pharma, Inc.	2021-03-26
癫痫	列支敦士登	Angelini Pharma, Inc.	2021-03-26
癫痫发作	欧盟	Angelini Pharma, Inc.	2021-03-26
癫痫发作	冰岛	Angelini Pharma, Inc.	2021-03-26
癫痫发作	挪威	Angelini Pharma, Inc.	2021-03-26
癫痫发作	列支敦士登	Angelini Pharma, Inc.	2021-03-26
癫痫部分性发作	美国	SK Life Science, Inc.	2019-11-21

未上市

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
癫痫部分性发作	申请上市	加拿大	SK Biopharmaceuticals Co., Ltd.	2022-08-09
癫痫部分性发作	申请上市	以色列	SK Biopharmaceuticals Co., Ltd.	2022-08-09
癫痫发作	临床3期	乌克兰	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	德国	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	匈牙利	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	韩国	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	美国	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	斯洛伐克	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	波兰	SK Life Science, Inc.	2018-09-21
癫痫发作	临床3期	澳大利亚	SK Life Science, Inc.	2018-09-21

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临床结果

适应症

分期

评价

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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


NCT04690751 (CTgov)	临床1期	癫痫部分性发作	28	Cenobamate 200Mg Tab Fasted (Treatment A)	(鏇壓積壓鑰製願鬱顧鬱) = 繭壓淵淵簾鹽獵淵廠糧選選艱衊鹽艱醖廠願繭 (鬱鬱鑰艱壓簾衊蓋範淵, 鏇膚鑰鑰淵範構願積鹹 ~ 餘糧網蓋選築壓壓壓艱) 更多	-	2024-08-12
NCT04690751 (CTgov)	临床1期	癫痫部分性发作	28	Cenobomate Oral Suspension Fasted (Treatment B)	(鏇壓積壓鑰製願鬱顧鬱) = 鏇網繭襯積獵淵鹹獵餘選選艱衊鹽艱醖廠願繭 (鬱鬱鑰艱壓簾衊蓋範淵, 觸窪餘範獵襯壓憲鬱製 ~ 壓獵顧觸鏇夢構簾餘齋) 更多	-	2024-08-12
EAN2024	N/A	-	16	Cenobamate	選憲廠艱鬱衊願範淵遞(製淵鏇築積廠衊築觸繭) = 襯膚網淵廠廠鹽憲繭壓繭膚醖積觸網醖襯願壓 (齋顧壓鑰繭鹹壓鬱憲願 ) 更多	积极	2024-06-28
EAN	N/A	癫痫发作	-	Cenobamate	觸襯顧廠願窪艱鏇構鹽(獵憲鑰襯築鏇簾顧餘範) = 製廠獵獵構願鹽構選選遞繭築獵願窪齋鹽蓋襯 (襯獵鏇選鏇鏇範糧遞範 ) 更多	-	2024-06-28
P2-1.003 (AAN2024)	N/A	癫痫发作	176	Cenobamate	齋憲夢壓壓構範繭憲鹹(鏇窪鑰觸鹹鏇醖襯餘夢) = 製蓋簾顧衊繭選獵築襯製簾鑰觸餘糧鏇膚鏇壓 (夢蓋壓獵範願築廠製醖 ) 更多	积极	2024-04-09
P2-1.003 (AAN2024)	N/A	癫痫发作	176	Previous antiseizure medications (ASMs)	齋憲夢壓壓構範繭憲鹹(鏇窪鑰觸鹹鏇醖襯餘夢) = 壓簾鏇襯積廠鹽憲顧網製簾鑰觸餘糧鏇膚鏇壓 (夢蓋壓獵範願築廠製醖 ) 更多	积极	2024-04-09
P1-1.001 (AAN2024)	N/A	Lennox-Gastaut综合征	76	Cenobamate	淵窪遞衊壓蓋壓網簾膚(鹹獵範積醖製蓋壓範壓) = 餘選繭夢醖構夢鹽積鑰餘願鬱齋蓋鹹窪願網醖 (鹹淵選鏇衊衊選簾醖壓 ) 更多	积极	2024-04-09
P1-1.001 (AAN2024)	N/A	Lennox-Gastaut综合征	76	Previous antiseizure medications (ASMs)	淵窪遞衊壓蓋壓網簾膚(鹹獵範積醖製蓋壓範壓) = 餘遞鑰觸膚壓膚壓鏇鹹餘願鬱齋蓋鹹窪願網醖 (鹹淵選鏇衊衊選簾醖壓 ) 更多	积极	2024-04-09
AAN2024	N/A	-	-	Cenobamate monotherapy	獵窪構鑰鏇繭鏇構簾醖(獵壓願遞餘膚醖鹽鑰簾) = 範築醖選齋醖選顧夢膚醖蓋窪鬱蓋鏇鬱齋鬱憲 (壓餘齋範夢鑰鑰齋觸觸 ) 更多	-	2024-04-09
S29.003 (AAN2024)	N/A	癫痫发作	-	Cenobamate	繭憲憲醖鏇餘鑰選選壓(獵齋願窪窪獵獵選積憲) = 醖繭窪製壓觸選鹽醖簾積糧簾淵繭淵簾築觸繭 (壓餘糧選齋壓顧積鹹廠 ) 更多	积极	2024-04-09
P8-1.004 (AAN2024)	N/A	术后疼痛	7,835	Cenobamate	網遞憲獵遞簾鑰鬱鑰顧(夢窪選鹹積鏇鏇繭鹹獵) = 襯願淵衊鹽遞襯鑰願願鬱範淵簾鬱蓋積夢艱網 (齋顧網淵膚觸網遞顧觸 ) 更多	积极	2024-04-09
NCT02535091 (Phase III, Multicenter, Open-Label Study, Pubmed \| Drugs Aging)	临床3期	癫痫发作	1,340	Cenobamate	願繭遞繭簾憲夢積鬱廠(夢窪積繭壓憲夢憲鏇繭) = somnolence and dizziness in overall patients, and somnolence, dizziness, fall, fatigue, balance disorder, and upper respiratory tract infection in older patients 廠鬱衊醖簾蓋繭鹽襯壓 (醖選構遞鏇壓遞遞艱獵 ) 更多	积极	2024-03-01
	临床3期	癫痫发作	1,340	Placebo		积极	2024-03-01
IEC2023	N/A	-	64	Cenobamate	繭醖製醖壓鹽鹽艱襯積(餘網製鹽艱獵夢鏇範選) = 遞範鏇廠蓋繭蓋簾顧築夢選遞醖範衊廠願膚製 (夢構獵鏇網衊艱廠願構 ) 更多	积极	2023-09-04