The effect of sulthiame on EEG has been studied in epilepsy syndromes of childhood with sleep activation by comparing sleep EEG obtained at baseline and after 4 weeks of treatment. The aim of the study is to know if an effect is still identifiable after 2 weeks of treatment by performing sleep EEG recordings after 2 and 4 weeks of treatment, respectively.

开始日期2023-10-17

申办/合作机构

Centre Hospitalier Universitaire d'Angers

EUCTR2017-004767-13-SE

/ Not yet recruiting临床2期

A randomized, placebo-controlled, multiple dose, double blind, phase IIb, dose guiding trial to explore safety and tolerability of four weeks treatment with sulthiame in patients with moderate to severe obstructive sleep apnea

开始日期2018-02-21

申办/合作机构

Desitin Arzneimittel GmbH

NCT03400189

/ Completed临床1期IIT

Preliminary Pilot Exploration of the Pharmacokinetic and Tolerability Profile of Sulthiame in Healthy Volunteers

This preliminary pilot exploration aims at specifying the pharmacokinetic parameters of sulthiame, formulated as an immediate release tablet, thus helping to design proper clinical trials for the future assessment of new paediatric formulations currently under development. The clinical tolerability to single doses of sulthiame will also be closely monitored to orient future trials.

开始日期2018-02-12

申办/合作机构

Centre Hospitalier Universitaire Vaudois

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100 项与舒噻美相关的临床结果

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100 项与舒噻美相关的转化医学

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100 项与舒噻美相关的专利（医药）

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项与舒噻美相关的文献（医药）

2025-08-01·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of isatin-functionalized benzenesulfonamides as novel carbonic anhydrase II and VII inhibitors with antiepileptic potential

Article

作者: Elnaggar, Yosra S R ; Eldehna, Wagdy M ; Giovannuzzi, Simone ; Abo-Ashour, Mahmoud F ; El-Hamaky, Anwar A ; Elsayed, Zainab M ; Al-Sanea, Mohammad M ; Alkabbani, Mahmoud Abdelrahman ; Tawfik, Haytham O ; Nocentini, Alessio ; Supuran, Claudiu T ; Khaleel, Eman F

Epilepsy continues to be a challenging neurological disorder with a partially understood etiology that necessitates novel therapeutic strategies. This study introduces isatin-functionalized benzenesulfonamides (5a-f and 7a-e) targeting carbonic anhydrase (CA) isoforms II and VII implicated in seizure mechanisms. The design exploits a one-tail approach, integrating a sulfonamide warhead for zinc coordination in the CA active site, a triazole linker (inspired by FDA-approved antiepileptic rufinamide), and an isatin-based tail. In vitro evaluation revealed potent inhibition of hCA II and VII, with sulfonamides 5c, 5e, 5f, 7a, and 7d showing notable activity. The anticonvulsant activity of five carbonic anhydrase inhibitors (5c, 5e, 5f, 7a, and 7d) was assessed using PTZ and pilocarpine-induced convulsions in mice. These compounds were selected based on their superior in vitro inhibitory potency against hCA II and VII isoforms, as reflected by their low nanomolar K_I values. Among them, 5e and 7a exhibited the highest efficacy, achieving 100 % protection in the PTZ model and significantly delaying seizure onset in the pilocarpine model. These compounds also reduced seizure severity and improved survival rates, surpassing valproic acid's effectiveness. Additionally, biochemical evaluation revealed that both compounds restored hippocampal KCC2 and mTOR levels, suggesting their role in modulating neuronal excitability and ionic balance. Safety assessments, including Rotarod and biochemical toxicity tests, confirmed their favorable safety profile, supporting their potential as promising anticonvulsant candidates.

2025-07-01·MICROBIOLOGICAL RESEARCH

Histone deacetylase Hos1 promotes the homeostasis of Candida albicans cell wall and membrane and its specific inhibitor has an antifungal activity in vivo

Article

作者: Wang, Yuchen ; Wang, Yanmei ; Bai, Wenhui ; Yang, Chen ; Zhang, Qiyue ; Li, Qingqing ; Ma, Jia ; Zhang, Peipei ; Zhang, Jiye ; Li, Guanglin

The rise of drug-resistant Candida albicans (C. albicans) has led to an urgent need for new therapeutic strategies. Histone deacetylases (HDACs) inhibition has been shown to limit fungal virulence while enhancing the efficacy of antifungal drugs against Candida. However, HDACs are highly conserved from yeast to humans, which has hindered the application of these inhibitors in the antifungal therapy. The aim of this study is to identify a suitable antifungal target and develop specific inhibitors targeting C. albicans HDACs. Based on sequence alignments, the HDAC Hos1 in C. albicans was proposed as a target for further investigation. We evaluated the impact of Hos1 on C. albicans pathogenicity using a murine model of disseminated candidiasis. Results showed that Hos1 null mutant caused less damage to mouse tissues. Additionally, we demonstrated that the reduced virulence was due to inhibition of cell wall O-mannan biosynthesis and altered metabolic flexibility, leading to decreased adaptability of C. albicans. Increased sensitivity of C. albicans to antifungal drugs was attributed to abnormal accumulation of ergosterol in the cell membrane. Furthermore, we identified Hos1 inhibitors from the ZINC database using molecular docking. These inhibitors exhibited highly specific inhibition of the deacetylation activity of C. albicans Hos1. Importantly, the inhibitors not only reduced colonization and invasion by C. albicans in vivo but also synergized with polyene drugs to combat C. albicans by causing abnormal accumulation of ergosterol. Our findings provide detailed insights into antifungal targets and a useful foundation for the discovery of antifungal drugs specifically targeting Candida.

2025-07-01·SEIZURE-EUROPEAN JOURNAL OF EPILEPSY

Loss-of-function variant in KCNH3 is associated with global developmental delay, autistic behavior, insomnia, and nocturnal seizures

Article

作者: Kortüm, Fanny ; Bauer, Christiane K ; Denecke, Jonas ; Möllring, Anna ; Alawi, Malik ; Bähring, Robert ; Harms, Frederike L ; Grinstein, Lev

INTRODUCTION:

The KCNH gene family encodes voltage-gated potassium (Kv) channels of the EAG subtype covering three subfamilies (Kv10-12). EAG channels are involved in the control of cardiac and neuronal excitation, and pathogenic variants in KCNH genes encoding Kv10 (eag) and Kv11 (erg) subfamily members cause a broad clinical spectrum ranging from cardiac arrhythmia to neurodevelopmental syndromes. However, no pathogenic variants have been hitherto reported for KCNH genes encoding Kv12 (elk) subfamily members.

METHODS:

Clinical, genomic, and functional studies were performed, including voltage-clamp experiments using heterologous channel expression in Xenopus oocytes.

RESULTS:

We examined an eight-year-old girl presenting with global developmental delay, intellectual disability, autistic and aggressive behavior, hyperactivity, insomnia, and nocturnal seizures. Focal seizures were successfully treated with sulthiame, which reduced the occurrence of temporo-parietal spike-wave paroxysms. Trio exome sequencing revealed a heterozygous de novo missense variant, NM_012284.3:c.1112C>T; p.(Ala371Val), in KCNH3, which encodes the Kv channel α-subunit Kv12.2. The amino acid substitution associated with the KCNH3 variant identified in the patient is located at a site highly conserved in EAG channels. The analogous variant in KCNH2 causes long-QT-syndrome 2, and has also been associated with epilepsy. Electrophysiological characterization of the KCNH3 p.(Ala371Val) variant demonstrated loss-of-function of the mutant Kv12.2 channels and strongly reduced current amplitudes upon co-expression of wildtype and mutant channel subunits in a dominant-negative manner.

CONCLUSION:

Our results propose KCNH3, which is primarily expressed in the nervous system, as a new disease gene associated with a neurodevelopmental phenotype including seizures.

项与舒噻美相关的新闻（医药）

2025-04-25

·shionogi.com

Shionogi Announces Further Agreement with Apnimed for Sleep Disorder Treatments - Introduction of New Assets to Joint Venture Shionogi-Apnimed Sleep Science – (SASS)

OSAKA, Japan, April 25, 2025 - Shionogi & Co., Ltd. (Head Office: Osaka, Japan; Chief Executive Officer: Isao Teshirogi, Ph.D.; hereafter "Shionogi") announced that it has entered into an agreement with Apnimed, Inc. (Head Office: Massachusetts, USA; Chief Executive Officer: Lawrence G. Miller, MD; hereafter "Apnimed") for the introduction of sulthiame* and a new drug development program. * Sulthiame: A carbonic anhydrase inhibitor approved as an antiepileptic drug in certain regions. Sulthiame has successfully completed two Phase 2 trials in over 300 obstructive sleep apnea (OSA) patients studied for up to 3 months in Europe.1 With the conclusion of this agreement, Shionogi acquired a joint ownership interest in the intellectual property rights related to the use of sulthiame in the field of sleep apnea and also in other intellectual property rights related to a different drug development program of Apnimed by paying a one-time fee to Apnimed.※ Furthermore, Shionogi and Apnimed have already equally contributed this intellectual property to SASS, which will now conduct thefuture research and development of sulthiame and the other drug development program. ※ Note: Shionogi retains exclusive negotiation rights for the development and sales rights in Japan, Korea, Taiwan, and China. “We are pleased to add new assets to the SASS OSA pipeline,” said John Keller, Ph.D., Senior Executive Officer, Senior Vice President, R&D Supervisory Unit at Shionogi. “Our joint venture, combining the scientific and medical resources of Apnimed and Shionogi, represents the most robust global effort to bring new pharmacologic treatments for people with sleep apnea and related disorders.” “We are delighted to announce that this transaction further strengthened our SASS pipeline,” commented Larry Miller, MD, Chief Executive Officer of Apnimed. “The 80 million people with OSA in the US, and hundreds of millions more around the globe, need more convenient options that directly treat the root causes of OSA.” Shionogi has identified Contributing to a Healthy and Prosperous Life as one of our material focus area. We are committed to creating a society where everyone can lead a longer, more vibrant life, realizing their goals. Through the partnership with Apnimed, Shionogi continues to strive to deliver innovative treatments for diseases with high unmet medical needs, including sleep apnea and related disorders, to patients as quickly as possible. About Apnimed Apnimed, based in Cambridge, Massachusetts, is a pharmaceutical company with exceptional expertise in sleep disorders. The company is building a portfolio of novel drug treatments for sleep-related breathing disorders, including Sleep Apnea Syndrome (SAS). Apnimed's lead development candidate, AD109, aims to maintain upper airway patency during sleep with a once-daily oral medication for the treatment of OSA, which, if approved, could bring a dramatic change to conventional therapies for OSA. For more details, please visit apnimed.com, X, or LinkedIn. About Shionogi-Apnimed Sleep Science, LLC In November 2023, Shionogi and Apnimed established a joint venture, Shionogi-Apnimed Sleep Science, LLC, with each company holding a 50% stake. 2 The aim of SASS is to provide promising solutions to meet the unmet needs in the field of sleep disorders. SASS combines Shionogi's capabilities in small molecule drug discovery, first-in-class and best-in-class compound creation with Apnimed's advanced expertise in the field of sleep disorders, including a highly experienced clinical-stage drug development team and a strong network with clinical facilities. This collaboration leverages superior translational research to create promising solutions in the field of sleep disorders more rapidly than either company could achieve alone. References: 1. Hedner et al. Efficacy, Safety, and Tolerability of Three Doses of Sulthiame in Patients With Obstructive Sleep Apnea. A Randomized, Double-blind, Placebo Controlled, Dose-ranging Study (STM-042/K). B14. American Thoracic Society Annual Meeting 2024. 2. Press Release: November 1, 2023 - Establishment of a Joint Venture Company with Apnimed for Solving Challenges in Sleep Disorders Forward-Looking Statements This announcement contains forward-looking statements. These statements are based on expectations in light of the information currently available, assumptions that are subject to risks and uncertainties which could cause actual results to differ materially from these statements. Risks and uncertainties include general domestic and international economic conditions such as general industry and market conditions, and changes of interest rate and currency exchange rate. These risks and uncertainties particularly apply with respect to product-related forward-looking statements. Product risks and uncertainties include, but are not limited to, completion and discontinuation of clinical trials; obtaining regulatory approvals; claims and concerns about product safety and efficacy; technological advances; adverse outcome of important litigation; domestic and foreign healthcare reforms and changes of laws and regulations. Also for existing products, there are manufacturing and marketing risks, which include, but are not limited to, inability to build production capacity to meet demand, lack of availability of raw materials and entry of competitive products. The company disclaims any intention or obligation to update or revise any forward-looking statements whether as a result of new information, future events or otherwise. For Further Information, Contact: SHIONOGI Website Inquiry Form: https://www.shionogi.com/global/en/contact.html

临床2期引进/卖出上市批准

2024-09-13

·drugs

Sulthiame Beneficial for Symptoms of Obstructive Sleep Apnea

FRIDAY, Sept. 13, 2024 -- Sulthiame (STM) is beneficial for improving symptoms of obstructive sleep apnea (OSA), according to a study presented at the European Respiratory Society Congress, held from Sept. 7 to 11 in Vienna. Jan A. Hedner, M.D., Ph.D., from Sahlgrenska Academy in Sweden, and colleagues conducted a double-blind, randomized, placebo-controlled trial involving OSA patients not accepting or tolerating continuous positive airway pressure or oral splints. Polysomnography was used to evaluate three doses of STM and placebo. Overall, 298 participants were randomly allocated to 100 mg, 200 mg, and 300 mg STM or placebo (74, 74, 75, and 75, respectively). The researchers found that the primary efficacy end point of change in the apnea/hypopnea index during sleep associated with a ≥3 percent decrease in oxygen levels or an arousal from sleep from baseline to week 15 was met for –17.8, –34.8, and –39.9 percent, respectively, with 100 mg, 200 mg, and 300 mg STM. A placebo-adjusted, dose-dependent reduction of 47.1 percent in apnea/hypopnea with ≥4 percent oxygen desaturation was seen at week 15. Improvement in mean overnight oxygen desaturation of 0.95 and 0.87 percent was seen at week 15 for 200 mg and 300 mg STM, respectively. There was improvement in the total arousal index and sleep quality; effects on sleep macrostructure were neutral. For sleepy patients (Epworth Sleepiness Scale ≥11), the scale score was reduced. "People taking sulthiame in the trial had a reduction in OSA symptoms such as stopping breathing during the night and feeling sleepy during the day. Their average levels of oxygen in the blood were also improved with the treatment," Hedner said in a statement. Abstract More Information Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果

2024-09-10

·drugs

Could a Pill Help Ease Sleep Apnea?

TUESDAY, Sept. 10, 2024 -- A European epilepsy drug could be an effective treatment for sleep apnea, a new study suggests. Patients who took sulthiame had few pauses in their breathing while asleep, as well as higher levels of blood oxygen, according to clinical trial results presented Tuesday at the European Respiratory Society annual meeting in Vienna. “This suggests that sulthiame could be an effective treatment for obstructive sleep apnea, especially for those who find they cannot use the existing mechanical treatments” like a CPAP machine , said researcher Jan Hedner from Sahlgrenska University Hospital and the University of Gothenburg in Sweden. Sulthiame has never been approved for use in the United States, but it is used in Europe to treat epilepsy. It appears to quell seizures by increasing blood levels of an established anticonvulsant called phenytoin. The drug also targets the respiratory system by inhibiting an enzyme called carbonic anhydrase, which stimulates upper airway muscles, researchers explained. For the study, researchers recruited nearly 300 people being treated for sleep apnea at hospitals in Spain, France, Belgium, Germany and the Czech Republic. None of the patients were using CPAP machines or mouthpieces to keep their airways open during sleep. Three-fourths of the participants were prescribed sulthiame at different dosage levels, and the remaining quarter took a placebo pill. Those taking the highest dose of sulthiame had 40% to 50% better breathing at night than those on placebo, based on different measures of sleep apnea, researchers said. Sulthaime patients also felt less sleepy during the daytime, researchers said. The drug produced mild to moderate side effects like pins and needles, headache, fatigue and nausea. “People taking sulthiame in the trial had a reduction in obstructive sleep apnea symptoms such as stopping breathing during the night and feeling sleepy during the day,” Hedner said in a meeting news release. “Their average levels of oxygen in the blood were also improved with the treatment.” However, Hedner said further clinical trials are needed to confirm these benefits before sulthaime can be widely adopted as a treatment for sleep apnea. Head of the ERS meeting, Sophia Schiza , noted this is one of the first studies to suggest that a drug could help with sleep apnea. Schiza was not involved in the research. “The results are promising,” Schiza, a professor of respiratory and sleep medicine at the University of Crete in Greece, said in a news release. “We need to continue testing sulthiame and other treatments to understand their long-term effects, including any side effects.” Because these findings were presented at a medical meeting, they should be considered preliminary until published in a peer-reviewed journal. Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果上市批准

100 项与舒噻美相关的药物交易

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KEGG	Wiki	ATC	Drug Bank
D01787	舒噻美	N03AX03	DB08329

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适应症	国家/地区	公司	日期
癫痫发作	日本	Kyowa Pharmaceutical Industry Co., Ltd.	2001-09-28

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适应症	最高研发状态	国家/地区	公司	日期
阻塞性睡眠呼吸暂停综合征	临床2期	比利时	Desitin Arzneimittel GmbH	2021-11-23

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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


Drugs 人工标引	N/A	阻塞性睡眠呼吸暂停综合征	298	Sulthiame 100 mg	齋積艱獵繭壓觸選膚獵(衊憲淵製夢鹹憲製鏇鑰) = 齋選膚積鹽繭鏇繭衊餘顧願選糧鬱壓襯鏇積製 (衊餘選廠構鑰襯廠衊鹽 )	积极	2024-09-13
				Sulthiame 200 mg	齋積艱獵繭壓觸選膚獵(衊憲淵製夢鹹憲製鏇鑰) = 鏇顧窪蓋襯鏇鹽積觸夢顧願選糧鬱壓襯鏇積製 (衊餘選廠構鑰襯廠衊鹽 ) 更多
ERS2022	N/A	阻塞性睡眠呼吸暂停综合征 hemoglobin-adjusted blood CA activity	-	STM 200 mg	遞夢襯範製蓋襯願窪窪(簾範膚壓齋膚窪襯鏇簾) = 鏇製齋鏇窪鹽鹹夢選願構醖築鏇襯糧築糧壓構 (鑰獵鬱壓衊夢選遞壓夢 )	积极	2022-09-04
				Placebo	遞夢襯範製蓋襯願窪窪(簾範膚壓齋膚窪襯鏇簾) = 願餘襯醖襯鏇廠艱鏇願構醖築鏇襯糧築糧壓構 (鑰獵鬱壓衊夢選遞壓夢 )
ERS2022	N/A	阻塞性睡眠呼吸暂停综合征	58	Sulthiame 200mg	憲壓範願衊衊繭糧鏇壓(簾衊遞壓壓範獵夢鹽繭) = 繭繭艱選製艱糧衊顧憲艱簾鬱膚夢積網夢艱膚 (襯齋獵鑰壓獵窪淵壓膚 ) 更多	积极	2022-09-04
				Sulthiame 400mg	憲壓範願衊衊繭糧鏇壓(簾衊遞壓壓範獵夢鹽繭) = 鏇鑰構鏇鹽網鹽壓廠願艱簾鬱膚夢積網夢艱膚 (襯齋獵鑰壓獵窪淵壓膚 ) 更多
EUCTR2017-004767-13-SE (not available, WSC2022)	临床2期	睡眠呼吸暂停综合征	-	Sulthiame 200 mg	築願獵醖餘繭繭製夢製(醖簾醖願憲餘醖壓願醖) = 鹽獵憲構鹽憲簾鬱獵壓範壓積廠膚醖艱艱鏇壓 (膚糧獵繭膚窪積鏇築鬱 ) 更多	积极	2022-03-11
				Sulthiame 400 mg	築願獵醖餘繭繭製夢製(醖簾醖願憲餘醖壓願醖) = 糧淵鹽夢齋蓋鬱蓋選糧範壓積廠膚醖艱艱鏇壓 (膚糧獵繭膚窪積鏇築鬱 ) 更多
NCT00471744 (Pubmed \| Cochrane Database Syst Rev)	临床3期	癫痫	355	Sulthiame	淵艱蓋觸壓觸願範窪淵(顧遞廠製鏇築築鹹顧觸): RR = 1.12 (95% CI, 0.88 ~ 1.44) 更多	-	2021-09-23
				Levetiracetam