D-塔格糖(D-tagatose) - 在研适应症：普拉德-威利综合症，2型糖尿病，I型高脂蛋白血症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(3S,4S,5R)-1,3,4,5,6-pentahydroxyhexan-2-one、D-lyxo-hex-2-ulose、D-lyxo-hexulose

+ [4]

靶点-

作用方式-

作用机制

铁螯合剂

治疗领域

神经系统疾病遗传病与畸形内分泌与代谢疾病+ [1]

在研适应症

普拉德-威利综合症2型糖尿病I型高脂蛋白血症

非在研适应症-

原研机构

Niagen Bioscience, Inc.

在研机构

Biospherics.net, Inc.Niagen Bioscience, Inc.

非在研机构

Dominari Holdings, Inc.

权益机构-

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构/序列

分子式C6H12O6

InChIKeyBJHIKXHVCXFQLS-PQLUHFTBSA-N

CAS号87-81-0

关联

4

项与 D-塔格糖相关的临床试验

NCT06230900

/ CompletedN/AIIT

Assessment of Mass Balance of Orally Administered [14C] (3S,4S,5R)-1,3,4,5,6-pentahydroxy-hexan-2-one in Healthy Volunteers Using a Microtracer Approach

Worldwide almost 40% of the adult population is overweight (including >10% obese), and more than 350 million children (up to the age of 19) are overweight. Overweight and obesity are significant problems and important risk factors for several lifestyle-related diseases, such as cardiovascular disease, certain cancers, non-alcoholic fatty liver disease (NAFLD) and type 2 diabetes (T2D). Excessive consumption of glucose/sucrose is a major contributor to overweight and obesity. Alternative, low-calorie sweeteners could reduce daily energy intake and thus slow down the development of these conditions and related diseases. (3S,4S,5R)-1,3,4,5,6-pentahydroxy-hexan-2-one is a sweetener that may be suitable for use as a sugar substitute; it is only partially digested in the small intestine and as a result has a lower energy density than more traditional sweeteners such as sucrose. However, it is not yet known to what extent (3S,4S,5R)-1,3,4,5,6-pentahydroxy-hexan-2-one is used in the body and then excreted.
The aim of this study is to measure the metabolic utilization (the 'mass balance') of a single dose of 14C-labelled (3S,4S,5R)-1,3,4,5,6-pentahydroxy-hexan-2-one and AMS technology. Based on clinical data of excretion (urine and faeces) and CO2 production (expired air), the mass balance can be derived. These generated results will be used to map the metabolic pathways (3S,4S,5R)-1,3,4,5,6-pentahydroxy-hexan-2-one undergoes during the digestion process. In addition, it will provide insight into the use of AMS technology to investigate the relationship between diet and health.

开始日期2024-02-05

申办/合作机构

Wageningen University

[+2]

JPRN-UMIN000026233

/ CompletedN/AIIT

A study of the effects on oral bacteria with D-Tagatose chewing gum - A study with D-Tagatose chewing gum

开始日期2015-08-06

申办/合作机构-

NCT00961662

/ Completed临床2期

Dose Ranging Effects of Three Low-doses of Naturlose™ (Tagatose) on Glycemic Control and Safety of Naturlose™ (Tagatose) Over Six Months in Subjects With Mild Type 2 Diabetes Mellitus Under Control With Diet and Exercise.

This study is a six-month, prospective, randomized, multicenter, single- blind, controlled clinical study to evaluate the effect of three low-doses of Naturlose (Tagatose) on glycemic control and safety in subjects with Type 2 diabetes under diet control and exercise. The subjects were randomized in one of the 3 arms receiving 2.5, 5 or 7.5 gm of Tagatose.

开始日期2008-02-01

申办/合作机构

University of Kentucky

100 项与 D-塔格糖相关的临床结果

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100 项与 D-塔格糖相关的转化医学

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100 项与 D-塔格糖相关的专利（医药）

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1,872

项与 D-塔格糖相关的文献（医药）

2025-06-01·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Characterization of a tagatose 4-epimerase and optimizing its expression for efficient D-tagatose bioconversion from fructose

Article

作者: Ni, Dawei ; Chen, Jiajun ; Wei, Yuhan ; Zhao, Shenxi ; Zhang, Wenli ; Mu, Wanmeng ; Xu, Wei

D-Tagatose is a promising functional sweetener due to its safety profile and versatile physiological effects. Recently, the bioconversion of D-tagatose from cost-effective natural resources has gained increasing attention. In this study, the hypothetical protein DRJ43_04605 from Thermoprotei archaeon, abbreviated as DRJ43-T4Ease, was identified as a tagatose 4-epimerase capable of efficiently converting d-fructose into D-tagatose. DRJ43-T4Ease exhibited optimal specific activity of 0.79 U/mg at pH 7.5 and 90 °C in the presence of 1 mM Ni²⁺. The denaturation temperature (T_m) of the enzyme was determined to be 105.9 °C, with a half-life of 7.19, 6.56, and 4.84 h at 85, 90, and 95 °C, respectively. The kinetic parameters for d-fructose conversion, including K_m, k_cat, and k_cat/K_m, were calculated to be 51.86 mM, 127.22 min^-1, and 2.45 mM^-1 min^-1, respectively. Furthermore, the expression of DRJ43-T4Ease in E. coli was optimized by engineering the translation initiation sequence. The engineered strain EcDRJ43-T4Ease-M1 achieved a volume activity of 98.4 U/L through shake-flask fermentation and a conversion efficiency of 17.2 % using 100 g/L d-fructose as the substrate. This study demonstrates the potential for D-tagatose production from d-fructose via whole-cell bioconversion, providing a promising approach for the industrial-scale production of this valuable sweetener.

2025-06-01·FOOD CHEMISTRY

Enhanced catalytic activity of carbonate buffer for isomerization of D-galactose into D-tagatose

Article

作者: Delidovich, Irina ; Milasing, Neeranuch ; Khuwijitjaru, Pramote ; Toussaint, Valérie ; Hametner, Christian

D-tagatose (Tag) is a rare monosaccharide with health benefits. In this work, catalytic activity of CAPS (pH 10.4), carbonate (pH 10.4), triethylamine (pH 11.2), quinuclidine (pH 11.5), and L-arginine (pH 12.5) was examined for isomerization of D-galactose (Gal) to Tag. The maximum yields of Tag were 15.0 % with CAPS, 15.2 % with carbonate, 19.3 % with triethylamine, 19.6 % with quinuclidine, and 18.1 % with L-arginine. Despite identical pH, the Tag formation rate with carbonate buffer was 3-8 times higher than with CAPS. For carbonate buffer, the reaction orders for hydroxide and carbonate anions were ∼ 1 and ∼ 0, respectively. Operando NMR studies of Gal-1-¹³C isomerization in carbonate and CAPS buffers indicate similar tautomeric distributions of the substrate in both buffers. The deuterium kinetic isotope effect demonstrated that carbonate facilitates isomerization through a proton transfer mechanism, with hydroxide anions acting as the catalytically active species whereas carbonate anions stabilize the enediolate anion and/or the transition state.

2025-05-01·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Biochemical characterization and biocatalytic application of a hyperthermostable tagatose 4-epimerase from Infirmifilum uzonense

Article

作者: Ni, Dawei ; Chen, Jiajun ; Zhu, Yingying ; Wei, Yuhan ; Zhang, Wenli ; Mu, Wanmeng ; Xu, Wei

D-Tagatose is a representative rare sugar with the physiochemical properties of low energy and high sweetness, as well as excellent physiological functions such as blood sugar regulation, enhancement of intestinal flora, and prevention of dental caries. At present, D-tagatose production involves lactose hydrolysis and D-galactose isomerization processes, resulting in high production costs that hinder its industrial advancement. Tagatose 4-epimerase (T4Ease) has the capability to directly convert d-fructose into D-tagatose through C-4 epimerization, providing a new approach for D-tagatose production. In this study, a hyperthermostable T4Ease from Infirmifilum uzonense (Inuz-TE4ase) was identified from the Foldseek clustered AlphaFold database and its biochemical properties were characterized in detail. Under the optimal reaction conditions of 90 °C and pH 8.5 (Tris-HCl) with the addition of 1 mM Ni²⁺, the maximum catalytic activity towards d-fructose was determined to be 0.680 U/mg. Inuz-TE4ase exhibited exceptional thermostability, with half-life (t_1/2) values of 19.3 h at 85 °C and 8.9 h at 90 °C, respectively. Inuz-TE4ase was strictly metal-dependent, and its stability could be enhanced by Ni²⁺ with an increase in the melting temperature (T_m) value from 101.1 °C to 105.7 °C. When 100 g/L d-fructose was used as the substrate, Inuz-TE4ase could catalyze the production of 21.67 g/L D-tagatose, indicating its significant potential for D-tagatose bioproduction.

100 项与 D-塔格糖相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	D-塔格糖	-	DB04936

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
普拉德-威利综合症	临床3期	美国	Dominari Holdings, Inc.	2020-08-06
2型糖尿病	临床3期	美国	-	2007-04-01
2型糖尿病	临床3期	印度	-	2007-04-01
I型高脂蛋白血症	临床3期	-	Niagen Bioscience, Inc.	-

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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


NCT00955747 (NEET, CTgov)	临床3期	2型糖尿病	494	Sugar Substitute Splenda (Sugar Substitute Splenda)	繭糧觸構憲構鬱選餘憲(艱築廠淵選廠繭構夢衊) = 醖鏇蓋鏇製鑰醖夢範壓憲淵鬱範襯鹽衊願構遞 (構積廠願遞衊繭鬱夢選, 0.07) 更多	-	2014-11-19
				Tagatose (Tagatose)	繭糧觸構憲構鬱選餘憲(艱築廠淵選廠繭構夢衊) = 鑰壓憲廠壓構廠夢鹹積憲淵鬱範襯鹽衊願構遞 (構積廠願遞衊繭鬱夢選, 0.07) 更多
NCT00961662 (CTgov)	临床2期	2型糖尿病	161	D-Tagatose (2.5 Active)	鬱構膚淵餘鑰獵觸窪繭 = 襯鹹糧壓積簾網鑰艱鏇襯積襯鏇鹽淵膚選餘鹹 (繭觸製觸顧艱鏇築蓋鏇, 範廠艱築齋齋築觸觸鏇 ~ 鑰鑰築襯衊膚餘糧窪壓) 更多	-	2014-11-06
				D-Tagatose (5.0 Mid Dose)	鬱構膚淵餘鑰獵觸窪繭 = 製網簾獵襯繭鑰構淵廠襯積襯鏇鹽淵膚選餘鹹 (繭觸製觸顧艱鏇築蓋鏇, 膚餘淵夢夢醖淵願衊廠 ~ 淵鏇遞淵廠簾構製鹽醖) 更多