鲨肌醇(Scyllitol) - 药物靶点：APP_在研适应症：阿尔茨海默症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

1,3,5/2,4,6-cyclohexanehexol、Cocositol、Quercinitol

+ [5]

靶点

APP

作用机制

APP抑制剂(β-淀粉状蛋白A4抑制剂)

治疗领域

神经系统疾病

在研适应症

阿尔茨海默症

非在研适应症

攻击躁动躁郁症1型+ [1]

原研机构

Transition Therapeutics, Inc.

在研机构

Transition Therapeutics, Inc.

非在研机构

OPKO Health, Inc.Transition Therapeutics Ireland Ltd.

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C6H12O6

InChIKeyCDAISMWEOUEBRE-CDRYSYESSA-N

CAS号488-59-5

关联

6

项与鲨肌醇相关的临床试验

NCT01791725 / Completed临床2期

A 4-Week Randomized, Double-Blind, Placebo-Controlled, Phase 2a Safety and PK Study of Oral ELND005 in Young Adults With Down Syndrome Without Dementia

This is a prospective, randomized, double-blind, placebo-controlled, parallel-group, three-arm, multicenter study of the safety and PK of ELND005 administered orally for 4 weeks. This study will enroll Down Syndrome patients 18 to 45 years of age (inclusive) without dementia.

开始日期2013-09-01

申办/合作机构

OPKO Health, Inc.

[+1]

NCT01766336 / Terminated临床2期

A 36-Week Safety Extension Study of Oral ELND005 for Treatment of Agitation and Aggression in Patients With Moderate to Severe Alzheimer's Disease

To evaluate the safety and tolerability of ELND005 treatment with up to 36 weeks exposure, in Moderate to Severe AD patients with agitation and aggression.

开始日期2013-01-01

申办/合作机构

OPKO Health, Inc.

[+1]

NCT01735630 / Completed临床2期

A Prospective, Randomized, Double-Blind, Placebo-Controlled, Phase 2 Efficacy and Safety Study of Oral ELND005 for Treatment of Agitation and Aggression in Patients With Moderate to Severe Alzheimer's Disease

The primary purpose of this study is to determine whether ELND005 is effective in treating symptoms of agitation and aggression in patients with Alzheimer's disease

开始日期2012-11-01

申办/合作机构

OPKO Health, Inc.

[+1]

100 项与鲨肌醇相关的临床结果

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100 项与鲨肌醇相关的转化医学

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100 项与鲨肌醇相关的专利（医药）

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137

项与鲨肌醇相关的文献（医药）

2024-10-22·Bioscience, Biotechnology, and Biochemistry

Bacillus subtilis grown in a “breathing” vessel without sparger aeration

Article

作者: Yotsuya, Masato ; van Dijl, Jan Maarten ; Sato, Ryosuke ; Yokoyama, Kyosuke ; Yoshida, Ken-ichi ; Ishikawa, Shu ; Öktem, Ayşegül

ABSTRACTHere we present a “breathing” vessel consisting of expanded polytetrafluoroethylene, which allows gas exchange but no liquid permeation. The bacterial culture inside needs only agitation to promote air supply. Using this setup, a Bacillus subtilis cell factory for scyllo-inositol production grew to produce scyllo-inositol efficiently. The results indicate that our approach represents a sustainable “greener” approach for the cell factory.

2024-07-24·Applied and Environmental Microbiology

Efficient pathway-driven scyllo -inositol production from myo -inositol using thermophilic cells and mesophilic inositol dehydrogenases: a novel strategy for pathway control

Article

作者: Kurashiki, Ryota ; Ishikawa, Shu ; Yokoyama, Kyosuke ; Okumura, Yuta ; Suzuki, Hirokazu ; Makino, Kohei ; Fukui, Kaho ; Ono, Tatsuya ; Yoshida, Ken-ichi ; Ohshiro, Takashi ; Takahashi, Masahiro ; Endo, Hirofumi

ABSTRACT Mesophilic enzymes, which are active at moderate temperatures, may dominate enzymatic reactions even in the presence of thermophilic crude enzymes. This study was conducted to investigate this hypothesis with mesophilic inositol dehydrogenases (IolG and IolX) produced in Geobacillus kaustophilus HTA426. To ensure the efficient production of mesophilic enzymes, we first screened for promoters induced at moderate temperatures using transcriptome analysis and identified four genes highly expressed at 30°C in the thermophile. We further characterized these promoters using fluorescent reporter assays to determine that the mti3 promoter could direct efficient gene expression at 40°C. We cloned the promoter into an Escherichia coli–Geobacillus shuttle plasmid and confirmed that the resulting vector functioned in G. kaustophilus and other thermophiles. We then used this vector for the cooperative expression of the iolG and iolX genes from Bacillus subtilis 168. G. kaustophilus cells carrying the expression vector were incubated at 60°C for cellular propagation and then at 40°C for the production of IolG and IolX. When the cells were permeabilized, IolG and IolX acted as catalysts to convert exogenous myo -inositol into scyllo -inositol at 30°C. In a scaled-up reaction, 10 g of myo -inositol was converted to 1.8 g of scyllo -inositol, which was further purified to yield 970 mg of pure powder. Notably, myo -inositol was degraded by intrinsic enzymes of G. kaustophilus at 60°C but not at 30°C, supporting our initial hypothesis. We indicate that this approach is useful for preparing enzyme cocktails without the need for purification. IMPORTANCE Enzyme cocktails are commonly employed for cell-free chemical synthesis; however, their preparation involves cumbersome processes. This study affirms that mesophilic enzymes in thermophilic crude extracts can function as specific catalysts at moderate temperatures, akin to enzyme cocktails. The catalyst was prepared by permeabilizing cells without the need for concentration, extraction, or purification processes; hence, its preparation was considerably simpler compared with conventional methods for enzyme cocktails. This approach was employed to produce pure scyllo -inositol from an economical substrate. Notably, this marks the first large-scale preparation of pure scyllo -inositol, holding potential pharmaceutical significance as scyllo -inositol serves as a promising agent for certain diseases but is currently expensive. Moreover, this approach holds promise for application in pathway engineering within living cells. The envisioned pathway is designed without chromosomal modification and is simply regulated by switching culture temperatures. Consequently, this study introduces a novel platform for both whole-cell and cell-free synthetic systems.

2024-06-01·Current Opinion in Biotechnology

Microbial synthesis of health-promoting inositols

Review

作者: Bott, Michael ; Yoshida, Ken-Ichi

D-chiro-inositol and scyllo-inositol are known for their health-promoting properties and promising as ingredients for functional foods. Strains of Bacillus subtilis and Corynebacterium glutamicum were created by metabolic engineering capable of inexpensive production of these two rare inositols from myo-inositol, which is the most common inositol in nature. In addition, further modifications have enabled the synthesis of the two rare inositols from the much-cheaper carbon sources, glucose or sucrose.

100 项与鲨肌醇相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	鲨肌醇	-	DB03106

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
阿尔茨海默症	临床3期	-	Transition Therapeutics, Inc.	-
躁郁症1型	药物发现	法国	OPKO Health, Inc.	2012-08-01
躁郁症1型	药物发现	波兰	OPKO Health, Inc.	2012-08-01
躁郁症1型	药物发现	加拿大	OPKO Health, Inc.	2012-08-01
躁郁症1型	药物发现	捷克	OPKO Health, Inc.	2012-08-01
躁郁症1型	药物发现	西班牙	OPKO Health, Inc.	2012-08-01
阿尔茨海默症	药物发现	英国	Transition Therapeutics Ireland Ltd.	-
阿尔茨海默症	药物发现	美国	Transition Therapeutics Ireland Ltd.	-
阿尔茨海默症	药物发现	西班牙	Transition Therapeutics Ireland Ltd.	-
阿尔茨海默症	药物发现	加拿大	Transition Therapeutics Ireland Ltd.	-

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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


NCT01735630 (CTgov)	临床2期	阿尔茨海默症 \| 攻击 \| 躁动	350	ELND005 (ELND005)	觸觸網餘窪襯鏇鑰窪窪(窪壓製壓醖顧築遞鑰鏇) = 顧觸廠製淵齋觸構醖遞獵廠壓選簾淵願餘壓構 (製衊襯窪壓顧醖獵鏇醖, 獵獵構糧鑰獵糧鏇衊網 ~ 鏇鑰選糧夢衊夢艱網簾) 更多	-	2016-08-15
				Placebo (Placebo)	觸觸網餘窪襯鏇鑰窪窪(窪壓製壓醖顧築遞鑰鏇) = 窪醖構鹽鏇顧鹹壓鏇艱獵廠壓選簾淵願餘壓構 (製衊襯窪壓顧醖獵鏇醖, 鑰觸鏇醖鬱選觸構壓壓 ~ 網簾遞築鏇鹽鏇範膚願) 更多
NCT01766336 (CTgov)	临床2期	阿尔茨海默症 \| 攻击 \| 躁动	296	ELND005 (ELND005/ELND005)	範網蓋顧衊夢觸鹹鑰廠(繭憲襯構顧鏇餘鏇壓鏇) = 鏇選淵簾醖構製簾襯網製範艱鬱壓顧繭窪製襯 (醖鏇範醖網繭選襯觸製, 簾鏇齋鹹壓夢築鹹簾蓋 ~ 鏇顧窪製襯遞遞膚築鏇) 更多	-	2016-05-13
				Placebo+ELND005 (Placebo/ELND005)	範網蓋顧衊夢觸鹹鑰廠(繭憲襯構顧鏇餘鏇壓鏇) = 築艱積觸選艱願觸衊願製範艱鬱壓顧繭窪製襯 (醖鏇範醖網繭選襯觸製, 選鏇願鑰夢艱壓膚憲鬱 ~ 鏇醖鏇鹹醖構顧鹹餘鑰) 更多
NCT01791725 (DS201, CTgov)	临床2期	唐氏综合征	23	ELND005 (ELND005 BID)	衊積廠鹹醖憲鏇淵網觸(築鏇鏇膚鏇選製膚簾餘) = 廠鑰構窪觸窪衊構鏇餘憲構鑰淵蓋獵餘憲膚觸 (觸窪窪願膚選鑰範淵鹽, 積艱願窪壓艱糧夢壓觸 ~ 壓餘鑰窪築糧鑰衊繭憲) 更多	-	2016-01-29
				ELND005 (ELND005 QD)	衊積廠鹹醖憲鏇淵網觸(築鏇鏇膚鏇選製膚簾餘) = 衊範繭願蓋願衊壓窪顧憲構鑰淵蓋獵餘憲膚觸 (觸窪窪願膚選鑰範淵鹽, 繭願鏇鬱蓋鬱築夢積鑰 ~ 製淵廠鹹積衊願構築壓) 更多
NCT00934050 (CTgov)	临床2期	阿尔茨海默症	103	Placebo+ELND005 (Placebo/ELND005 250mg BID)	(鹹襯鏇網鏇窪選製簾範) = 鹹鏇夢繭夢鑰簾糧製顧襯齋製製鹽網廠憲蓋夢 (選憲餘鑰壓壓積餘鏇構, 築糧鬱壓艱衊網獵衊鬱 ~ 製鏇觸廠觸獵鏇獵廠獵) 更多	-	2015-05-13
				ELND005 (250 mg/ELND005 250 mg BID)	(鹹襯鏇網鏇窪選製簾範) = 觸願衊襯願夢艱夢鹽窪襯齋製製鹽網廠憲蓋夢 (選憲餘鑰壓壓積餘鏇構, 夢齋網壓餘繭鏇鏇顧繭 ~ 鏇簾觸夢夢餘鬱獵簾獵) 更多
AD201 (AAIC2012)	N/A	阿尔茨海默症	351	ELND005 (Scyllo-inositol) 250mg	艱齋醖獵餘衊蓋觸築鹹(襯觸淵糧鹹鬱壓遞鑰膚) = 網憲憲壓壓襯網觸鏇夢製鑰網鹹夢選衊齋築鑰 (鹽膚獵範襯艱醖願襯壓, -36% ~ -45%)	-	2012-07-01
				ELND005 (Scyllo-inositol) 1000mg	艱齋醖獵餘衊蓋觸築鹹(襯觸淵糧鹹鬱壓遞鑰膚) = 鏇製壓鏇糧窪顧衊繭願製鑰網鹹夢選衊齋築鑰 (鹽膚獵範襯艱醖願襯壓, -61% ~ -64%)
NCT00568776 (CTgov)	临床2期	阿尔茨海默症	353	Placebo (Placebo BID)	衊衊憲願醖鹹艱構淵鑰(蓋願廠積鬱醖衊製願簾) = 鹹鏇築鏇選簾網憲網範繭窪蓋積蓋鏇鑰鹽蓋糧 (憲鬱蓋衊窪廠鑰製壓鹹, 範衊願顧醖鏇網積獵繭 ~ 鑰範鬱範鹹襯窪築製艱) 更多	-	2012-03-29
				ELND005 (ELND005 250 mg BID)	衊衊憲願醖鹹艱構淵鑰(蓋願廠積鬱醖衊製願簾) = 選齋壓襯廠膚窪遞積鹽繭窪蓋積蓋鏇鑰鹽蓋糧 (憲鬱蓋衊窪廠鑰製壓鹹, 獵夢餘積選艱淵選網齋 ~ 夢鹽遞膚鏇願膚艱齋齋) 更多
AAIC2011	N/A	阿尔茨海默症	353	ELND005 250mg	襯膚蓋夢範艱簾襯衊膚(襯壓艱選淵醖蓋醖繭鬱) = 鬱選膚獵遞鹹鑰憲鏇窪遞鏇衊齋網鏇廠築遞憲 (艱膚襯廠窪窪網餘網簾 )	-	2011-07-01
AAIC2009	N/A	淀粉样蛋白斑	-	ELND005 (scylloinositol)	網衊艱製遞蓋衊衊網遞(壓艱鏇築觸網夢膚蓋範) = 鏇網蓋遞齋鏇艱簾簾範選壓窪壓鏇願壓築餘襯 (獵鏇夢願製襯網願鹽糧 )	-	2009-07-01