GANC inhibitors(glucosidase alpha, neutral C inhibitors), MGAM inhibitors(Maltase-glucoamylase inhibitors), α-glucosidase inhibitors(Acidic alpha-glucosidase inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes MellitusDiabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Takeda Pharmaceutical Co., Ltd.

Active Organization

Tianjin Takeda Pharmaceutical Co. Ltd.

Takeda Pharmaceutical Co., Ltd.

Inactive Organization

Zhejiang Hisoar Pharmaceutical Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (01 Jul 1994),

Diabetes Mellitus, Type 2

Regulation-

Structure

Molecular FormulaC10H21NO7

InChIKeyFZNCGRZWXLXZSZ-CIQUZCHMSA-N

CAS Registry83480-29-9

Clinical Trials associated with Voglibose

CTR20243825 / Active, not recruitingNot Applicable

伏格列波糖片人体生物等效性研究

[Translation] Study on the bioequivalence of voglibose tablets in healthy volunteers

本试验旨在研究单次空腹口服北京星昊医药股份有限公司生产的伏格列波糖片（0.2 mg）的药效学特征；以天津武田药品有限公司生产的伏格列波糖片（倍欣®，0.2 mg）为参比制剂，比较口服两制剂后血糖的△CSG,max、△AUEC0-2 h，评价两制剂的人体生物等效性。

[Translation]

This study aimed to study the pharmacodynamic characteristics of a single fasting oral administration of voglibose tablets (0.2 mg) produced by Beijing Xinghao Pharmaceutical Co., Ltd.; using voglibose tablets (Bexin®, 0.2 mg) produced by Tianjin Takeda Pharmaceutical Co., Ltd. as the reference preparation, to compare the △CSG,max and △AUEC0-2 h of blood glucose after oral administration of the two preparations, and to evaluate the bioequivalence of the two preparations in humans.

Start Date02 Nov 2024

Sponsor / Collaborator

Beijing Sunho Pharmaceutical Co., Ltd.

CTR20242708 / Active, not recruitingNot Applicable

伏格列波糖片在健康受试者中的生物等效性研究

[Translation] Bioequivalence study of voglibose tablets in healthy subjects

主要目的：采用随机、开放、单剂量、两制剂、两序列、四周期、完全重复交叉给药设计比较上海现代制药股份有限公司生产的伏格列波糖片（规格：0.3mg）与Teva Takeda Yakuhin Ltd.持证的伏格列波糖片（商品名：倍欣®，规格：0.3mg）的药效动力学参数，评价受试制剂与参比制剂在空腹条件下的人体生物等效性。次要目的：观察受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Primary objective: To compare the pharmacodynamic parameters of voglibose tablets (specification: 0.3 mg) produced by Shanghai Modern Pharmaceutical Co., Ltd. and voglibose tablets (trade name: Beixin®, specification: 0.3 mg) certified by Teva Takeda Yakuhin Ltd. using a randomized, open, single-dose, two-preparation, two-sequence, four-period, completely repeated crossover design, and to evaluate the bioequivalence of the test preparation and the reference preparation under fasting conditions. Secondary objective: To observe the safety of the test preparation and the reference preparation in healthy subjects.

Start Date14 Oct 2024

Sponsor / Collaborator

Shanghai Shyndec Pharmaceutical Co., Ltd.

CTR20241548 / CompletedNot Applicable

评估受试制剂伏格列波糖片（规格：0.2 mg）与参比制剂倍欣®（规格：0.2 mg）在健康成年参与者空腹状态下的单中心、随机、开放、单剂量、四周期、两序列、完全重复交叉生物等效性研究

[Translation] A single-center, randomized, open-label, single-dose, four-period, two-sequence, fully repeated crossover bioequivalence study to evaluate the test preparation Voglibose Tablets (strength: 0.2 mg) and the reference preparation Basen® (strength: 0.2 mg) in healthy adult participants under fasting state

主要目的：研究空腹状态下单次口服受试制剂伏格列波糖片（规格：0.2 mg，浙江京新药业股份有限公司生产）与参比制剂伏格列波糖片（倍欣®，规格：0.2 mg，天津武田药品有限公司生产）在健康参与者体内的药效动力学，评价空腹状态口服两种制剂的生物等效性。次要目的：评估受试制剂伏格列波糖片（规格：0.2 mg）和参比制剂伏格列波糖片（倍欣®，规格：0.2 mg）在健康参与者中的安全性。

[Translation]

Primary objective: To study the pharmacodynamics of a single oral dose of the test preparation voglibose tablets (specification: 0.2 mg, produced by Zhejiang Jingxin Pharmaceutical Co., Ltd.) and the reference preparation voglibose tablets (Bexin®, specification: 0.2 mg, produced by Tianjin Takeda Pharmaceutical Co., Ltd.) in healthy participants under fasting conditions, and to evaluate the bioequivalence of the two preparations when taken orally under fasting conditions. Secondary objective: To evaluate the safety of the test preparation voglibose tablets (specification: 0.2 mg) and the reference preparation voglibose tablets (Bexin®, specification: 0.2 mg) in healthy participants.

Start Date29 May 2024

Sponsor / Collaborator

Zhejiang Jingxin Pharmaceutical Co., Ltd.

100 Clinical Results associated with Voglibose

100 Translational Medicine associated with Voglibose

100 Patents (Medical) associated with Voglibose

366

Literatures (Medical) associated with Voglibose

01 Nov 2024·Archives of physiology and biochemistry

Exploring plant-based alpha-glucosidase inhibitors: promising contenders for combatting type-2 diabetes

Review

Author: Mishra, Abha ; Kumari, Sonali ; Saini, Ravi ; Bhatnagar, Aditi

OBJECTIVE:

This systematic review aimed to provide comprehensive details on the α-G inhibitory potential of various bioactive compounds derived from natural sources.

METHODS:

A comprehensive literature search was conducted using various databases and search engines, including Science Direct, Google Scholar, SciFinder, Web of Science, and PubMed until May, 2023.

RESULTS AND CONCLUSIONS:

The enzyme alpha-glucosidase (α-G) is found in the brush border epithelium of the small intestine and consists of duplicated glycoside hydrolase (GH31) domain. It involves the conversion of disaccharides and oligosaccharides into monosaccharides by acting on alpha (1 → 4) and (1 → 6) linked glucose residue. Once absorbed, glucose enters the bloodstream and elevates postprandial glucose, which is associated with the development of type 2 Diabetes (T2D). Epidemic obesity, cardiovascular disease, and nephropathy are linked to T2D. Traditional medicinal plants with α-G inhibitory potential are commonly used to treat T2D due to the adverse effects of currently used α-G inhibitors miglitol, acarbose, and voglibose. Various bioactive compounds derived from natural sources, including lupenone, Wilforlide A, Baicalein, Betulinic acid, Ursolic acid, Oleanolic acid, Katononic acid, Carnosol, Hypericin, Astilbin, lupeol, betulonic acid, Fagomine, Lactucaxanthin, Erythritol, GP90-1B, Procyanidins, Galangin, and vomifoliol retain α-G inhibitory potential for regulating hyperglycaemia.

01 Nov 2024·Journal of Diabetes Investigation

Theragnostic utility of continuous glucose monitoring in post‐gastrectomy hypoglycemia

Article

Author: Son, Heejun ; Lee, Bon Hyang ; Cho, Young Min

Abstract:

Diagnosing post‐gastrectomy hypoglycemia is challenging, often relying on medical history with documented low plasma glucose levels. Here, we present three cases of patients who presented a high probability of post‐gastrectomy hypoglycemia diagnosed and managed successfully using “theragnostic” continuous glucose monitoring and alpha‐glucosidase inhibitors. In the first week, patients maintained their current lifestyle without medical intervention; in the second week, voglibose 0.2 mg before meals was prescribed. Continuous glucose monitoring data from the first week confirmed the diagnosis with multiple hypoglycemic events after postprandial peaks, whereas data from the second week showed reduced hypoglycemic events and lower glycemic variability, demonstrating voglibose's therapeutic effect. This report highlights the effective management of post‐gastrectomy hypoglycemia using voglibose and theragnostic continuous glucose monitoring, showing its potential benefits and safety for similar cases.

01 Sep 2024·CURRENT DRUG TARGETS

Recent Advances in the Development of Alpha-Glucosidase and Alpha-Amylase Inhibitors in Type 2 Diabetes Management: Insights from In silico to In vitro Studies

Article

Author: Khan, Fariya ; Kumar, Ajay ; Akhtar, Salman ; Khan, Mohsin Vahid

Diabetes is a metabolic disorder caused by high glucose levels, leading to serious threats such as diabetic neuropathy and cardiovascular diseases. One of the most reliable measures for controlling postprandial hyperglycemia is to reduce the glucose level by inhibiting enzymes in the digestive system, such as Alpha-Glucosidase and Alpha-Amylase. Here, we have investigated the use of inhibitors to inhibit carbohydrate metabolism in order to restrict glucose levels in diabetic patients. Acarbose, Voglibose, and Miglitol are three inhibitors approved by the FDA that efficiently inhibit these two enzymes and thereby minimising hyperglycemia but are also significantly helpful in reducing the risk of cardiovascular effects. We also provide insight into the other known inhibitors currently available in the market. The adverse effects associated with other inhibitors emphasise the demand for the latest in silico screening and in vitro validation in the development of potent inhibitors with greater efficacy and safety for the treatment of Type 2 diabetes. The recent findings suggest that Alpha-Glucosidase and Alpha-Amylase play a major role in carbohydrate metabolism and triggering the increase in glucose levels. This review provides the latest scientific literature findings related to these two enzymes as well as the role of primary and secondary inhibitors as potential candidates. Moreover, this review elaborates the framework on the mechanism of action, different plant sources of extraction of these enzymes, as well as kinetic assay of inhibitors and their interaction that can be used in future prospects to develop potential leads to combat Type 2 diabetes.

News (Medical) associated with Voglibose

23 Dec 2020

·www.geneonline.com

China’s Hasten Biopharmaceutic Acquires Five Non-Core Assets from Japan’s Takeda

Continuing its divestiture strategy since January 2019, Takeda has planned on releasing non-core assets to focus on creating innovative therapies and developments on Gastroenterology (GI), Rare Diseases, Plasma-Derived Therapies, Oncology, and Neuroscience, the 5 chosen areas that are essential to its long-term growth strategy. After the divestiture with Celltrion in early December, Takeda struck up another deal with Hasten Biopharmaceutic, a company funded by Feidong County of Hefei City, China and established by Ray Capital Management Limited. Takeda is letting go of five prescription drugs, including cardiovascular and metabolism products that are mainly sold in China in exchange for around 322 million. The portfolio of select drugs generated 109.5 million net sales in 2019, mostly contributed by cardiovascular drug Ebrantil, one of the products sold to Hasten. As per the contract, the employees who are dedicated to the commercial support of these products will also be transferred to Hasten. As for the manufacturing and supply agreement, Takeda will continue to manufacture and supply the divested products to Hasten. The agreement is estimated to close by June 30, 2021, and until then, Takeda will have the full right of these products. For future use of proceeds, Takeda will firstly reduce its debt and then facilitate the R&D and expand its manufacturing capacity of these five core business areas. “This announcement marks continued progress on our commitment to simplify our global portfolio and remain focused on investing in our growth drivers, and research and development pipeline,” said Costa Saroukos, Chief Financial Officer, Takeda. “We remain committed to expansion in China with more than 15 planned approvals over the next five years. By continuing to execute and deliver on Takeda’s financial commitments, including paying down debt and focusing on our highly innovative portfolio, we can sustain our long-term growth and continue to deliver life-transforming treatments for patients worldwide.” For the past two years, Takeda has exceeded its $10 billion non-core asset divestiture target. Here are some of the divestiture agreements in 2020. March 2: Sold 30 prescription pharmaceuticals and over-the-counter (OTC) products in Near East, Middle East, and African countries within its Growth and Emerging Markets Business Unit (GEM BU) to Acino for 200 million March 2: Sold 18 select OTC and prescription pharmaceutical assets in Brazil, Mexico, Argentina, Colombia, Ecuador, Panama, and Peru to Hypera Pharma for 825 million March 4: Sold 20 OTC and prescription pharmaceutical products exclusively in Russia, Georgia, and several countries from within the Commonwealth of Independent States to STADA Arzneimittel AG for 660 million. April 24: Sold 110 select OTC and prescription pharmaceutical assets in Europe to Orifarm for 670 million September 8: Sold non-core prescription pharmaceutical products sold predominantly in Europe and Canada to Cheplapharm for 562 million. December 1: Sold 18 pharmaceutical products and OTC products in the Asia Pacific to Celltrion for 278 million.

Acquisition

12 May 2005

·www.pharmatimes.com

First profits decline at Takeda in decade

Japan’s Takeda Pharmaceutical has posted a disappointing set of results for the year to March 2005, which show a fall of 2.7% to 277.4 billion yen ($2.6 billion), the first earnings decline the company has posted for 11 years. The firm’s sales increased 3.4% to 1.12 trillion yen, helped by strong domestic revenues of drugs such as the anti-hypertensive Blopress (candesartan), which had sales in Japan of 103.5 billion yen, up 11.6%. Domestic turnover of the diabetes agent Basen (voglibose), was up 8.1% to 61.5 billion yen, while Japanese sales of another treatment in the diabetes portfolio, Actos (pioglitazone), rose 33.6% to 15.5 billion yen. Lupron (leuprorelin), a treatment for prostate cancer, and the osteoporosis drug Benet (risedronate) both made useful contributions to domestic sales. However, it was abroad that Takeda came somewhat unstuck with a weaker contribution to profits from TAP Pharmaceutical, its US joint venture with Abbott Laboratories, down to 45.4 billion yen from 72.7 billion yen last year. The decline was due to falling sales of the gastrointestinal drug Prevacid (lansoprazole), but Takeda believes that the drop will be stemmed this year. Nevertheless, total overseas drug sales were up 3.5% to 462.9 billion yen and Takeda is also enthusiastic about its pipeline, having submitted an earlier-than-scheduled New Drug Application to the US Food and Drug Administration for its insomnia drug TAK-375 (ramelteon) last September[[24/09/04c]]. It also has high hopes for future drug candidates to come from Syrrx, the US biotechnology firm Takeda acquired for about $270 million earlier this year [[08/02/05d]]. Given these factors, and an upturn in TAP’s fortunes, for the year to March 2006, Takeda expects net income to rise to 295 billion yen.

100 Deals associated with Voglibose

External Link

KEGG	Wiki	ATC	Drug Bank
D01665	Voglibose	A10BF03	DB04878

R&D Status

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Diabetes Mellitus	CN	Tianjin Takeda Pharmaceutical Co. Ltd.	01 Jan 2001
Diabetes Mellitus, Type 2	JP	Takeda Pharmaceutical Co., Ltd.	01 Jul 1994

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02049814 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	494	Metformin+Voglibose (Metformin + Voglibose 0.2 mg)	ymbvfvocvk(dsilyxmkoz) = emsbegloop lkfmghrwap (qounvpgsqz, owcdvitqcu - xekejwdxhp) View more	-	04 Feb 2019
				Metformin+Acarbose (Metformin + Acarbose 50 mg)	ymbvfvocvk(dsilyxmkoz) = tkhdurjbeq lkfmghrwap (qounvpgsqz, pamzllklin - ypmoczkvyt) View more
NCT02287402 (CTgov)	Phase 4	Glucose Intolerance	197	AO-128	rwiedpomll(epujkjlrmg) = pspblhusji atkzirhnkh (owgpuumlmb, owasnoxenx - quxopjsoig) View more	-	09 Apr 2015
Pubmed \| Int J Clin Pharmacol Ther	Not Applicable	-	22	Metformin	zzxrzazyay(wevhxmgjie): geometric mean ratio = 0.99 (90% CI, 0.92 - 1.06), P-Value = > 0.05 View more	-	01 Nov 2014
				Metformin + Voglibose
NCT00837577 (0431-104, Pubmed \| J Diabetes Investig)	Phase 3	Diabetes Mellitus, Type 2	133	Sitagliptin 50 mg/day	(utwvpfygsi) = bqcyxejqjm fzevpbrsfm (ntdkjenzbf ) View more	-	27 Nov 2013
NCT00411554 (Pubmed \| Diabetes Obes Metab)	Phase 3	Diabetes Mellitus, Type 2	319	Sitagliptin 50 mg once daily	(ahzodbyqfk) = dxsejixjti iqqvhslqoq (fcpjkirtqu, -0.8 to -0.6) View more	Positive	01 Jul 2010
				Voglibose 0.2 mg thrice daily	(ahzodbyqfk) = cznmglrkdc iqqvhslqoq (fcpjkirtqu, -0.4 to -0.2) View more

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