Delving into the Latest Updates on Gliclazide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

1-(3-azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea, 1-(hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea, Diabeton MR

+ [19]

Target

SUR

Mechanism

SUR agonists(Sulfonylurea receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Les Laboratoires Servier SAS

Active Organization

Tianjin Huajin Pharmaceutical Co. Ltd.

Sumitomo Pharma Co., Ltd.

Inactive Organization

Guangzhou Pui's Pharmaceutical Factory Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (15 Feb 1984),

Diabetes Mellitus, Type 2

Regulation-

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Structure

Molecular FormulaC15H21N3O3S

InChIKeyBOVGTQGAOIONJV-UHFFFAOYSA-N

CAS Registry21187-98-4

Acanthosis nigricans (AN) is a skin condition characterized by hyperpigmentation and thickening, often found in individuals with insulin resistance. Despite this well-established association, the potential link between AN and hepatic fibrosis in people with type 2 diabetes (T2D) has yet to be thoroughly explored.

METHODOLOGY:

We recruited a total of 300 people with T2D, half of whom had AN (n, 150), and the other half without AN (n, 150). We evaluated body composition, biochemistry, and hepatic fat analysis (using the controlled attenuation parameter, CAP), as well as assessments of hepatic stiffness (using the kilopascal, kPa) using Fibroscan. We used multivariable regression analysis to find independent predictors of AN and their relationship to hepatic fibrosis. Furthermore, we developed a prediction equation and AUC for hepatic fibrosis.

RESULTS:

Upon comparison between AN vs. NAN group, following were significatly higher; weight, BMI, hepatic transaminases, liver span, CAP, and kPa. After adjusting for age, weight, body mass index, diabetes duration, and specific anti-hyperglycaemic drugs (gliclazide, DPP-4 inhibitors, pioglitazone, and Glucagon-like peptide-1 receptor agonists), adjusted OR for AN were, liver span, 1.78 (95% CI: 0.91-3.49, p = 0.09), CAP, 7.55 (95% CI: 0.93-61.1, p = 0.05), and kPa, 2.47 (95% CI: 1.50-4.06, p = 0.001). A ROC analysis of predictive score for hepatic fibrosis showed optimal sensitivity and specificity at a score cut-off of 25.2 (sensitivity 62%, specificity 63%), with an AUC of 0.6452 (95% CI: 0.61235-0.76420).

CONCLUSION:

Acanthosis nigricans has the potential to be used as an easy-to-identify clinical marker for risk of hepatic fat and fibrosis in Asian Indians with T2D, allowing for early detection and management strategies.

01 Jan 2024·Endocrinology, diabetes & metabolism case reports

Diabetes mellitus in Kabuki syndrome 1 on a background of post-transplant diabetes mellitus

Article

Author: Grayton, H ; Park, S M ; Chew Sue Mei, S ; Adler, A I ; Pritchard, N ; Simonicova, I

Summary:

Kabuki syndrome is a genetic disorder characterised by distinctive facial features, developmental delays, and multisystem congenital anomalies. Endocrine complications such as premature thelarche and short stature are common, whereas disorders of glycaemic control are less frequent. We describe a 23-year-old white female referred to the diabetes clinic for hyperglycaemia during haemodialysis. She was subsequently diagnosed with Kabuki syndrome based on characteristic clinical features, confirmed by detecting a heterozygous pathogenic variant in KMT2D. She was known to have had multiple congenital anomalies at birth, including complex congenital heart disease and a single dysplastic ectopic kidney, and received a cadaveric transplanted kidney at the age of 13. She had hyperglycaemia consistent with post-transplant diabetes mellitus (DM) and was started on insulin. Examination at the time revealed truncal obesity. She developed acute graft rejection and graft failure 14 months post-transplant and she was started on haemodialysis. Her blood glucose levels normalised post-graft explant, but she was hyperglycaemic again during haemodialysis at the age of 23. Given her clinical phenotype, negative diabetes antibodies and normal pancreas on ultrasound, she was assumed to have type 2 DM and achieved good glycaemic control with gliclazide.

Learning points:

Involve clinical genetics early in the investigative pathway of sick neonates born with multiple congenital anomalies to establish a diagnosis to direct medical care.Consider the possibility of Kabuki syndrome (KS) in the differential diagnoses in any neonate with normal karyotyping or microarray analysis and with multiple congenital anomalies (especially cardiac, renal, or skeletal), dysmorphic facial features, transient neonatal hypoglycaemia and failure to thrive.Consider the possibility of diabetes as an endocrine complication in KS patients who are obese or who have autoimmune disorders.

01 Dec 2023·Heliyon

Physicochemical reports of gliclazide-carplex solid dispersions and tablets prepared with directly compressible co-processed excipients

Article

Author: Ali, Md Ashraf ; Alam, Israt Zerin ; Al-Mamun, Md Elias ; Paul, Subrata ; Rahman, Md Bytul Mokaddesur ; Asha, Kaniz Fatema

Objectives:

The main goal of this research was to develop better tablet formulations by utilizing solid dispersions (SDs) and coprocessing excipients composite to achieve a better release rate of poor water-soluble gliclazide.

Methods:

The solvent evaporation method made SDs of gliclazide with different carriers carplex 67, carplex 80, and carplex FPS 500 (weight ratio, 1:1). The drug release patterns of the SDs were all evaluated and optimized. The SDs were illustrated by using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (PXRD), and Fourier transform infrared spectroscopy (FTIR). Tablet batches FGC-1 to 8 were made using gliclazide-carplex 67 solid dispersions (GC67-SDs) and the co-processed composite of excipients, namely starch-MCC-povidone (SMP) and lactose-MCC-povidone-sodium starch glycolate (LMPS), prepared with coprocessing technology. We evaluated these batches by conducting physicochemical tests and comparing them to the existing commercial brand.

Results:

In a water medium, the release of gliclazide from SDs peaked within the first 30 min, showing a roughly 5∼6-fold increase compared to plain gliclazide. This quick dissolution rate may be due to the amorphization of the drug, which improved the specific surface area, and increased wettability caused by the hydrophilic properties of carplex particles. This has been confirmed through SEM, DSC, FTIR, and PXRD analysis. All FGC formulations had satisfactory pre-compression factor results, while the post-compression parameters indicated good mechanical strength and homogeneity across the blend. All produced tablets met the weight variation, friability, and disintegration time limit set by the compendia. Through in vitro drug release testing, it was discovered that all FGC tablet batches had consistent and nearly identical release results compared to SDs of gliclazide. However, the FGC-5 to 8 batches containing LMPS composites were determined to be the most effective formulations. In the first 30 min in a water medium, the percentage of drug generated from the FGC-8 tablets involving GC67-SDs and co-processed composite LMPS-4 is approximately 3.5 times higher than the average release of currently marketed products (MPs). After storing the selected FGC tablet batches for three months at 40 °C and 75 % RH, there were no noticeable alterations in the amount of drug and drug release profiles across the batches.

Conclusion:

Based on these findings, it appears that using the carplex silica-based SDs approach, along with gliclazide and co-processing excipients composite, could result in significant benefits compared to the current commercial brands. This approach could be effectively utilized to create solid dosage forms for drugs that have low solubility in water.

5

News (Medical) associated with Gliclazide

26 Apr 2023

·www.nsmedicaldevices.com

VySpine’s UniVy OsteoVy-Ti NanoVy-HA cervical IBF system gets FDA clearance

The implant is indicated for intervertebral body fusion to be used at one level in the cervical spine, from C3 to T1 FDA gives clearance to VySpine’s UniVy OsteoVy-Ti NanoVy-HA cervical IBF system. (Credit: The U.S. Food and Drug Administration/Wikimedia Commons) VySpine has been given the 510(k) clearance from the US Food and Drug Administration (FDA) for its UniVy OsteoVy-Ti NanoVy-HA cervical IBF system for the treatment of degenerative disc disease (DDD). According to the spine company, the implant is indicated for intervertebral body fusion to be used at one level in the cervical spine, from C3 to T1. The UniVy OsteoVy-Ti NanoVy-HA cervical IBF system features the NanoVy-HA technology of VySpine in partnership with Promimic. NanoVy-HA is a procedure in which the 3D-printed UniVy OsteoVy-Ti implant gets surface-treated using hydroxyapatite. The typical coating thickness is 50 micrometers thick, whereas NanoVy-HA’s surface treatment can be only 20 nanometers in thickness, said VySpine. The spine company stated that the NanoVy-HA technology has been designed to enhance bone integration and improve the quality of the all-around area of the implant. The NanoVy-HA coating pierces the porous structure of the UniVy OsteoVy implant. VySpine claimed that the combination of high wettability and optimal surface chemistry of NanoVy-HA with nano-roughness that is optimised, mediates bioactivity and adsorption of the specific protein to the implant. These properties regulate the behaviour of cells and impact the process of regeneration of tissues by enhancing osteoblast’s functions, which allows for the creation of more bone quicker. The UniVy OsteoVy-Ti NanoVy-HA cervical IBF system is said to have optimal dimensions and structure of the pore. It is available in a variety of footprints to suit nearly every cervical interbody technique. Furthermore, the implant is claimed to come in a variety of sizes, heights, as well as lordotic angles. Earlier this year, VySpine secured FDA’s 510(k) clearance for its LumiVy NanoVy Ti Lumbar IBF system. The implant was indicated for intervertebral body fusion for use at one level or two contiguous levels in the lumbar spine, from L2 to S1, for the treatment of degenerative disc disease with up to Grade 1 spondylolisthesis.

Drug ApprovalIND

25 Apr 2023

·www.businesswire.com

VySpine Announces FDA Clearance for UniVy OsteoVy-Ti Cervical IBF with NanoVy-HA

TALLAHASSEE, Fla.--( BUSINESS WIRE )-- VySpine , a spine innovation leader using differentiated materials and designs, announced today that it has received 510(k) clearance from the FDA for its UniVy OsteoVy-Ti NanoVy-HA Cervical IBF System which is indicated for intervertebral body fusion for use at one level in the cervical spine, from C3 to T1, for the treatment of degenerative disc disease (DDD). The UniVy OsteoVy-Ti NanoVy-HA Cervical IBF System features VySpine's NanoVy-HA technology in partnership with Promimic AB. NanoVy-HA is a process in which the 3D printed UniVy OsteoVy-Ti implant is surface-treated with hydroxyapatite. Traditional coating is typically 50 micrometers, while NanoVy-HA surface treatment is a mere 20 nanometers thick. The NanoVy-HA technology is engineered to facilitate enhanced bone integration and quality to the entire surface of the UniVy OsteoVy-Ti implant. The NanoVy-HA coating penetrates the unique porous lattice structure of the UniVy OsteoVy-Ti implant. NanoVy-HA’s combination of high wettability and optimal surface chemistry, with optimized nano-roughness, mediates bioactivity and specific protein adsorption to the implant. These properties regulate cell behavior and influence tissue regeneration by increasing the osteoblast functions, building more bone faster. The UniVy OsteoVy-Ti NanoVy-HA Cervical IBF System features optimal pore size and structure. It is offered in a vast array of footprints for nearly any cervical interbody approach. Additionally, it is available in a range of sizes, heights, and lordotic angles. About VySpine VySpine was created through active internal development and the licensing of various proven technologies using innovative materials and designs. This comprehensive line of core spine products and newly developed specialty products allow us to meet the needs of both health care providers and surgeons. The company strives to outpace the competition by collaborating with key spine innovators while providing a flexible, cost-effective approach to spine care. Learn more at vyspine.com About Promimic AB Promimic AB is a growth company that develops and markets biomaterials for improved osseointegration to leading companies in the fields of dental and orthopedic implants. The main product HAnano Surface has been developed from cutting edge research at Chalmers University of Technology in Sweden. The technology is proven to improve osseointegration in over 30 scientific studies and with over 900,000 implants in clinical use. Promimic has offices in Mölndal, Sweden and Austin, Texas, USA. For more information visit www.promimic.com “VySpine,” “UniVy OsteoVy-Ti” and “NanoVy” are registered trademarks of VySpine.

Drug Approval

19 Jul 2022

·healthtechinsider.com

New CGM Device for Type 2 Diabetes

MySugarWatch has pushed the pedal on an awareness campaign for its continuous non-invasive glucose monitor called sugarBEAT. MySugarWatch is the UK licensee of Nemaura Medical, a company specializing in developing wearable diagnostic devices. The company aims to cater to the awareness needs of the people with pre-diabetes and diabetes. The campaign, featured in the DailyMail, is set to reach about 1.2 million people. MySugarWatch aims to eliminate skin-pricks test strips historically used by patients to monitor blood sugar level for Type-2 diabetes patients. Studies show that 3.6 million in the UK suffer from Type-2 Diabetes while a further 12.3 million people are at risk of developing the disorder. MySugarWatch adds to the list of continuous glucose monitoring devices. It monitors your blood sugar level every 5 minutes, providing consistent data. The data is then stored in a dedicated app, which maps the 168 glucose level readings taken during the day. This allows you to identify trends and monitor Time-in-Range right from your phone. The device does require calibration with a finger stick; a reading each morning before eating is recommended. Continuous Glucose Monitoring (CGM) was difficult to achieve so far due to difficulties in procedure including regular needle insertion. CGMs like MySugarWatch that measure interstitial fluid glucose levels do not require a needle prick and easily allows patients to make lifestyle changes based on trends in their blood sugar level. These strategic changes will greatly help patients and healthcare professionals to manage, prevent and even reverse Type-2 pre-diabetes. MySugarWatch, unfortunately, is not for Type-1 diabetes patients, or patients who receive injectable insulin or who are taking sulfonylurea medications (Glibenclamide, Gliclazide, Glimepiride, Glipizide, Tolbutamide). As a result, it’s not completely useful as an “artificial pancreas” component. The product does have CE Mark clearance, but not FDA clearance yet.

100 Deals associated with Gliclazide

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External Link

KEGG	Wiki	ATC	Drug Bank
D01599	Gliclazide	A10BB09	DB01120

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	JP	Sumitomo Pharma Co., Ltd.	15 Feb 1984

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


EASD2022	Not Applicable	-	-	Gliclazide 1 µM	ebibhwspnv(oytiuqefmb) = jqfydbfepq sejgctfoae (ntfagzqser, 3) View more	Positive	22 Sep 2022
				Rilpivirine 10 µM	qekujuvkgr(cwqhhrjzse) = bsbrjujffu mtylgrzwqr (wwvrlztaoh, 0.32) View more
NCT04198948 (CTgov)	Phase 1	Diabetes Mellitus, Type 2	15	Omeprazole+Gliclazide (Gliclazide + Omeprazole)	doioxzpnbp(skwoamervl) = akiaswsojj efbbvoqhsc (lrjkexufww, knnpqogpjl - zduftrgzvz) View more	-	15 Jul 2021
				Placebo+Gliclazide (Gliclazide + Placebo)	doioxzpnbp(skwoamervl) = knnbywocau efbbvoqhsc (lrjkexufww, ofdkaqfjgr - mjjksmusdo) View more
ADA2020	Not Applicable	Diabetes Mellitus, Type 2 Second line	2,346	Gliclazide MR	acockydgau(owwoqlzepy): HR = 1.28 (95% CI, 1.1 - 1.49) View more	Positive	01 Jun 2020
				Sitagliptin
ChiCTR-IPR-14005716 (EASD2018)	Phase 4	Diabetes Mellitus, Type 2	648	Saxagliptin plus Acarbose	wrmzhghjzn(tfpwzpaoeg) = Hypoglycemic events, almost all are mild, were reported during treatment period in acrabose (0.38%), gliclazide MR (1.42%), and metformin (0.68%) wxuexcazvk (epopgqjevn )	Positive	03 Oct 2018
				Saxagliptin plus Gliclazide MR
NCT01709305 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	5,570	Sitagliptin+Glimepiride+Metformin (Phase 2: Metformin + Sitagliptin + Glimepiride)	mejrjmzrnc(msdvwjfaoa) = ktqrnksltd tywzlptbjk (knbjqcvctf, jxvtanauhh - vxqxvlsftx) View more	-	11 May 2016
				Repaglinide+Sitagliptin+Metformin (Phase 2: Metformin + Sitagliptin + Repaglinide)	mejrjmzrnc(msdvwjfaoa) = fqytyehdau tywzlptbjk (knbjqcvctf, herzhmgtmi - zrufjigtod) View more
Pubmed \| Diabetes Metab Res Rev	Not Applicable	-	-	Insulin glargine plus gliclazide modified release combination therapy	jdkhbwibvd(gidfmqnzub) = gpkwgdntjd rxcvocymmq (mnjpkhqppl )	Positive	01 Oct 2015
				Twice-daily premixed insulin monotherapy	jdkhbwibvd(gidfmqnzub) = dbpttazwhp rxcvocymmq (mnjpkhqppl )
ISRCTN00943368 (EASD2015)	Not Applicable	Second line	7,170	Gliclazide MR 60 mg QD as first-line prescription	jhxtkdbvft(dhlezbssbu) = yqbtbdewny ydjswlxmdg (avvykneswv, 1.36) View more	Positive	15 Sep 2015
				Gliclazide MR 60 mg QD as add-on prescription	jhxtkdbvft(dhlezbssbu) = ezbiwomxau ydjswlxmdg (avvykneswv, 1.28)
NCT01022762 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	440	repaglinide (Repaglinide)	ungtcawfii(iouedhylff) = ptwmhnkqic iowwtycycf (dardnrimgi, hxuzjiihld - lkkttvgcrj) View more	-	29 Dec 2011
				gliclazide (Gliclazide)	ungtcawfii(iouedhylff) = hevgjwkuws iowwtycycf (dardnrimgi, mzsbxyctem - pqnwnoutri) View more
NCT00102388 (Pubmed \| Horm Metab Res)	Phase 3	Diabetes Mellitus, Type 2	546	Vildagliptin 50 mg bid	uwqakqadvg(zuseqoctje) = yfydncvkin onrgdrqlpg (vqoxjtqtjw ) View more	-	01 Dec 2009
				Gliclazide up to 320 mg/day	uwqakqadvg(zuseqoctje) = nhtktatpne onrgdrqlpg (vqoxjtqtjw ) View more
Int J Experimental Diab Res 2000 (ARVO2005)	Not Applicable	Diabetic Retinopathy	-	0.2% gliclazide-treated group	xikrqcpfis(qjkydnndvz) = zzdkitjygh jrvxwvjrec (bizvtnxntg )	Positive	01 May 2005
				0.0125% glibenclamide-treated group	xikrqcpfis(qjkydnndvz) = rctolkpfgs jrvxwvjrec (bizvtnxntg )