[Translation] This is a single-center, single-dose, fasting and fed, 2-formulation, 2-period, 2-sequence, open-label, randomized, crossover bioequivalence study of gliquidone tablets in healthy subjects.

主要研究目的：在健康受试者体内，分别在空腹、餐后状态下，以Glenwood GmbH Pharmazeutische Erzeugnisse持证，Boehringer Ingelheim Ellas A.E.生产的格列喹酮片（商品名：Glurenorm，规格：30 mg）为参比制剂，研究北京福元医药股份有限公司研制的格列喹酮片（受试制剂，规格：30 mg）的吸收速度和吸收程度，评价受试制剂与参比制剂是否具有生物等效性。次要研究目的：观察受试制剂和参比制剂在中国健康受试者中的安全性。

[Translation]

Main study objectives: In healthy subjects, under fasting and postprandial conditions, the absorption rate and extent of gliquidone tablets (test preparation, specification: 30 mg) developed by Beijing Fuyuan Pharmaceutical Co., Ltd. were studied using gliquidone tablets (trade name: Glurenorm, specification: 30 mg) produced by Boehringer Ingelheim Ellas A.E. licensed by Glenwood GmbH Pharmazeutische Erzeugnisse as the reference preparation, and whether the test preparation and the reference preparation are bioequivalent. Secondary study objectives: Observe the safety of the test preparation and the reference preparation in healthy Chinese subjects.

Start Date17 May 2024

Sponsor / Collaborator

Beijing Winsunny Pharmaceutical Co., Ltd.

CTR20222336 / CompletedNot Applicable

格列喹酮片随机、开放、两制剂、两周期、交叉、餐后给药健康人体生物等效性试验

[Translation] A randomized, open-label, two-dose, two-period, crossover, postprandial bioequivalence study of gliquidone tablets in healthy volunteers

主要目的：考察餐后状态下单次口服受试制剂格列喹酮片（天津药物研究院药业有限责任公司提供）与参比制剂格列喹酮片（商品名：Glurenorm®，Glenwood GmbH Pharmazeutische Erzeugnisse持证）在健康受试者体内的药代动力学特征，评价餐后状态下口服两种制剂的生物等效性。次要目的：考察受试制剂格列喹酮片和参比制剂格列喹酮片（Glurenorm®）在健康受试者中的安全性。

[Translation]

The primary objective is to investigate the pharmacokinetic characteristics of the test preparation gliquidone tablets (provided by Tianjin Pharmaceutical Research Institute Pharmaceutical Co., Ltd.) and the reference preparation gliquidone tablets (trade name: Glurenorm®, licensed by Glenwood GmbH Pharmazeutische Erzeugnisse) in healthy subjects after a single oral administration in the fed state, and to evaluate the bioequivalence of the two preparations after oral administration in the fed state. The secondary objective is to investigate the safety of the test preparation gliquidone tablets and the reference preparation gliquidone tablets (Glurenorm®) in healthy subjects.

Start Date13 Sep 2022

Sponsor / Collaborator

Tianjin Pharm Research Inst Pharm Co Ltd.

CTR20221264 / CompletedNot Applicable

格列喹酮片随机、开放、两制剂、两周期、交叉、空腹及餐后给药健康人体生物等效性试验

[Translation] A randomized, open-label, two-dose, two-period, crossover, fasting and postprandial bioequivalence study of gliquidone tablets in healthy volunteers

主要目的：考察空腹和餐后状态下单次口服受试制剂格列喹酮片（天津药物研究院药业有限责任公司提供）与参比制剂格列喹酮片（商品名：Glurenorm®，Glenwood GmbH Pharmazeutische Erzeugnisse持证）在健康受试者体内的药代动力学特征，评价空腹和餐后状态下口服两种制剂的生物等效性。次要目的：考察受试制剂格列喹酮片和参比制剂格列喹酮片（Glurenorm®）在健康受试者中的安全性。

[Translation]

Primary objective: To investigate the pharmacokinetic characteristics of the test preparation gliquidone tablets (provided by Tianjin Pharmaceutical Research Institute Pharmaceutical Co., Ltd.) and the reference preparation gliquidone tablets (trade name: Glurenorm®, licensed by Glenwood GmbH Pharmazeutische Erzeugnisse) in healthy subjects after a single oral administration in the fasting and fed state, and to evaluate the bioequivalence of the two preparations in the fasting and fed state. Secondary objective: To investigate the safety of the test preparation gliquidone tablets and the reference preparation gliquidone tablets (Glurenorm®) in healthy subjects.

Start Date20 Jun 2022

Sponsor / Collaborator

Tianjin Pharm Research Inst Pharm Co Ltd.

100 Clinical Results associated with Gliquidone

100 Translational Medicine associated with Gliquidone

100 Patents (Medical) associated with Gliquidone

169

Literatures (Medical) associated with Gliquidone

01 Mar 2024·Molecular Pharmacology

Inhibition of Cardiac Kv4.3/KChIP2 Channels by Sulfonylurea Drug Gliquidone

Article

Author: Hu, Fang ; Li, Qinqin ; Liu, Yani ; Yang, Chenxia ; Wang, KeWei

The Kv4.3 channel features fast N-type inactivation and also undergoes a slow C-type inactivation. The gain-of-function mutations of Kv4.3 channels cause an inherited disease called Brugada syndrome (BrS), characterized by a shortened duration of cardiac action potential repolarization and ventricular arrhythmia. The sulfonylurea drug gliquidone, an ATP-dependent K⁺ channel antagonist, is widely used for the treatment of type 2 diabetes. Here, we report a novel role of gliquidone in inhibiting Kv4.3 and Kv4.3/KChIP2 channels that encode the cardiac transient outward K⁺ currents responsible for the initial phase of action potential repolarization. Gliquidone results in concentration-dependent inhibition of both Kv4.3 and Kv4.3/KChIP2 fast or steady-state inactivation currents with an IC₅₀ of approximately 8 μM. Gliquidone also accelerates Kv4.3 channel inactivation and shifts the steady-state activation to a more depolarizing direction. Site-directed mutagenesis and molecular docking reveal that the residues S301 in the S4 and Y312A and L321A in the S4-S5 linker are critical for gliquidone-mediated inhibition of Kv4.3 currents, as mutating those residues to alanine significantly reduces the potency for gliquidone-mediated inhibition. Furthermore, gliquidone also inhibits a gain-of-function Kv4.3 V392I mutant identified in BrS patients in voltage- and concentration-dependent manner. Taken together, our findings demonstrate that gliquidone inhibits Kv4.3 channels by acting on the residues in the S4 and the S4-S5 linker. Therefore, gliquidone may hold repurposing potential for the therapy of Brugada syndrome. SIGNIFICANCE STATEMENT: We describe a novel role of gliquidone in inhibiting cardiac Kv4.3 currents and the channel gain-of-function mutation identified from patients with Brugada syndrome, suggesting its repurposing potential for therapy for the heart disease.

01 Feb 2024·Biotechnology and Applied Biochemistry

Purification and characterization of thioredoxin reductase enzyme from commercial Spirulina platensis tablets by affinity chromatography and investigation of the effects of some chemicals and drugs on enzyme activity

Article

Author: Yanardag, Refiye ; Dagsuyu, Eda

AbstractThioredoxin reductase (TrxR, enzyme code [E.C.] 1.6.4.5) is a widely distributed flavoenzyme that catalyzes nicotinamide adenine dinucleotide phosphate (NADPH)‐dependent reduction of thioredoxin and many other physiologically important substrates. Spirulina platensis is a blue–green algae that is often used as a dietary supplement. S. platensis is rich in protein, lipid, polysaccharide, pigment, carotenoid, enzyme, vitamins and many other chemicals and exhibits a variety of pharmacological functions. In the present study, a simple and efficient method to purify TrxR from S. platensis tablets is reported. The extractions were carried out using two different methods: heat denaturation and 2′,5′‐adenosine diphosphate Sepharose 4B affinity chromatography. The enzyme was purified by 415.04‐fold over the crude extract, with a 19% yield, and specific activity of 0.7640 U/mg protein. Optimum pH, temperature and ionic strength of the enzyme activity, as well as the Michaelis constant (Km) and maximum velocity of enzyme (Vmax) values for NADPH and 5,5′‐dithiobis(2‐nitrobenzoic acid) were determined. Tested metal ions, vitamins, and drugs showed inhibition effects, except Se4+ ion, cefazolin sodium, teicoplanin, and tobramycin that increased the enzyme activity in vitro. Ag+, Cu2+, Mg2+, Ni2+, Pb2+, Zn2+, Al3+, Cr3+, Fe3+, and V4+ ions; vitamin B3, vitamin B6, vitamin C, and vitamin U and aciclovir, azithromycin, benzyladenine, ceftriaxone sodium, clarithromycin, diclofenac, gibberellic acid, glurenorm, indole‐3‐butyric acid, ketorolac, metformin, mupirocin, mupirocin calcium, paracetamol, and tenofovir had inhibitory effects on TrxR. Ag+ exhibited stronger inhibition than 1‐chloro‐2,4‐dinitrobenzene (a positive control).

01 Sep 2023·Genomics & informatics

M Protein from Dengue virus oligomerizes to pentameric channel protein: in silico analysis study.

Article

Author: Sekar, Kanagaraj ; Ganjiwale, Anjali ; Zeba, Ayesha

The Dengue virus M protein is a 75 amino acid polypeptide with two helical transmembranes (TM). The TM domain oligomerizes to form an ion channel, facilitating viral release from the host cells. The M protein has a critical role in the virus entry and life cycle, making it a potent drug target. The oligomerization of the monomeric protein was studied using ab initio modeling and molecular dynamics (MD) simulation in an implicit membrane environment. The representative structures obtained showed pentamer as the most stable oligomeric state, resembling an ion channel. Glutamic acid, threonine, serine, tryptophan, alanine, isoleucine form the pore-lining residues of the pentameric channel, conferring an overall negative charge to the channel with approximate length of 51.9 Å. Residue interaction analysis (RIN) for M protein shows that Ala94, Leu95, Ser112, Glu124, and Phe155 are the central hub residues representing the physicochemical interactions between domains. The virtual screening with 165 different ion channel inhibitors from the ion channel library shows monovalent ion channel blockers, namely lumacaftor, glipizide, gliquidone, glisoxepide, and azelnidipine to be the inhibitors with high docking scores. Understanding the three-dimensional structure of M protein will help design therapeutics and vaccines for Dengue infection.

100 Deals associated with Gliquidone

External Link

KEGG	Wiki	ATC	Drug Bank
D02430	Gliquidone	A10BB08	DB01251

R&D Status

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	CN	Beijing Wanhui Double-Crane Pharmaceutical Co. Ltd.	01 Jan 1994

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis