Delving into the Latest Updates on Nateglinide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fastic, Glinate, Nageglinide

+ [38]

Target

PPARγ x SUR1

Mechanism

PPARγ antagonists(Peroxisome proliferator-activated receptor γ antagonists), SUR1 inhibitors(Sulfonylurea receptor 1 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication

Diabetes Mellitus, Noninsulin-Dependent, 2Glucose IntolerancePregnancy Complications, Cardiovascular

Originator Organization

Ajinomoto Co., Inc.

Active Organization

Ildong Pharmaceutical Co., Ltd.

EA Pharma Co., Ltd.

Jiangsu Deyuan Pharmaceutical Co., Ltd.

+ [1]

Inactive Organization

Novartis Pharmaceuticals Corp.Novartis Europharm Ltd.

Ajinomoto Health & Nutrition North America, Inc.

+ [1]

Drug Highest PhaseApproved

First Approval Date

JP (16 Jun 1999),

Diabetes Mellitus, Type 2

Regulation-

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Structure/Sequence

Molecular FormulaC19H27NO3

InChIKeyOELFLUMRDSZNSF-BRWVUGGUSA-N

CAS Registry105816-04-4

以天方药业有限公司研制的那格列奈片为受试制剂，由Novartis生产的那格列奈片（商品名：STARLIX）为参比制剂，在健康男性和女性受试者中于餐后情况下评价那格列奈片和 STARLIX®的吸收速度和程度，评价两制剂间是否具有生物等效性。

[Translation]

Nateglinide tablets developed by Tianfang Pharmaceutical Co., Ltd. were used as the test preparation, and nateglinide tablets (trade name: STARLIX) produced by Novartis were used as the reference preparation. The absorption rate and extent of nateglinide tablets and STARLIX® were evaluated in healthy male and female subjects after meals to evaluate whether the two preparations were bioequivalent.

Start Date13 May 2019

Sponsor / Collaborator

Topfond Pharmaceutical Co. Ltd.

CTR20181442

/ CompletedNot Applicable

单中心、随机开放、双周期双交叉设计评价中国健康受试者单次空腹及餐后口服那格列奈片的人体生物等效性试验

[Translation] A single-center, randomized, open-label, two-period, double-crossover design study to evaluate the bioequivalence of fasting and fed oral nateglinide tablets in healthy Chinese subjects

主要目的：以Novartis Singapore Pharmaceutical Manufacturing Pte. Ltd生产的那格列奈片(规格：120mgg，商品名：Starlix®)为参比制剂，以江苏德源药业股份有限公司生产的那格列奈片(规格：120mg)为受试制剂，来评价空腹及餐后条件下的生物等效性。次要目的：在研究过程中，通过不良事件发生率、实验室检验结果、生命体征和体格检查等的变化情况评估那格列奈片的安全性。

[Translation]

Primary objective: Using nateglinide tablets (specification: 120 mgg, trade name: Starlix®) produced by Novartis Singapore Pharmaceutical Manufacturing Pte. Ltd as the reference preparation and nateglinide tablets (specification: 120 mg) produced by Jiangsu Deyuan Pharmaceutical Co., Ltd. as the test preparation, to evaluate the bioequivalence under fasting and postprandial conditions. Secondary objective: During the study, the safety of nateglinide tablets was evaluated by changes in the incidence of adverse events, laboratory test results, vital signs and physical examinations.

Start Date20 Jun 2018

Sponsor / Collaborator

Jiangsu Deyuan Pharmaceutical Co., Ltd.

CTR20180642

/ CompletedNot Applicable

那格列奈片在健康受试者中的单剂量、随机、开放性、交叉、正式、空腹及餐后生物等效性研究

[Translation] A single-dose, randomized, open-label, crossover, formal, fasting and fed bioequivalence study of nateglinide tablets in healthy subjects

以天方药业有限公司研制的那格列奈片为受试制剂，由Novartis生产的那格列奈片（商品名：STARLIX）为参比制剂，进行空腹/餐后状态下人体生物利用度与生物等效性试验，计算受试制剂的相对生物利用度，评价两种制剂的生物等效性，并评价受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Nateglinide tablets developed by Tianfang Pharmaceutical Co., Ltd. were used as the test preparation, and nateglinide tablets (trade name: STARLIX) produced by Novartis were used as the reference preparation. Human bioavailability and bioequivalence studies were conducted under fasting/postprandial conditions to calculate the relative bioavailability of the test preparation, evaluate the bioequivalence of the two preparations, and evaluate the safety of the test preparation and the reference preparation in healthy subjects.

Start Date08 May 2018

Sponsor / Collaborator

Topfond Pharmaceutical Co. Ltd.

100 Clinical Results associated with Nateglinide

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100 Translational Medicine associated with Nateglinide

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100 Patents (Medical) associated with Nateglinide

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544

Literatures (Medical) associated with Nateglinide

01 Aug 2024·Diabetes

Loss of ATP-Sensitive Potassium Channel Expression and Function in the Nervous System Decreases Opioid Sensitivity in a High-Fat Diet–Fed Mouse Model of Diet-Induced Obesity

Article

Author: Sadrati, Amir ; Janecek, Jody L. ; Graham, Melanie L. ; Johnson, Kayla ; Klein, Amanda H. ; Moore, Madelyn ; Fisher, Cole

During diabetes progression, β-cell dysfunction due to loss of potassium channels sensitive to ATP, known as KATP channels, occurs, contributing to hyperglycemia. The aim of this study was to investigate if KATP channel expression or activity in the nervous system was altered in a high-fat diet (HFD)–fed mouse model of diet-induced obesity. Expression of two KATP channel subunits, Kcnj11 (Kir6.2) and Abcc8 (SUR1), were decreased in the peripheral and central nervous system of mice fed HFD, which was significantly correlated with mechanical paw-withdrawal thresholds. HFD mice had decreased antinociception to systemic morphine compared with control diet (CON) mice, which was expected because KATP channels are downstream targets of opioid receptors. Mechanical hypersensitivity in HFD mice was exacerbated after systemic treatment with glyburide or nateglinide, KATP channel antagonists clinically used to control blood glucose levels. Upregulation of SUR1 and Kir6.2, through an adenovirus delivered intrathecally, increased morphine antinociception in HFD mice. These data present a potential link between KATP channel function and neuropathy during early stages of diabetes. There is a need for increased knowledge of how diabetes affects structural and molecular changes in the nervous system, including ion channels, to lead to the progression of chronic pain and sensory issues.Article Highlights

01 Apr 2024·Journal of Pharmaceutical Sciences

The Use of Carboxyfluorescein Reveals the Transport Function of MCT6/SLC16A5 Associated with CD147 as a Chloride-Sensitive Organic Anion Transporter in Mammalian Cells

Article

Author: Furuya, Takahito ; Shirasaka, Yoshiyuki ; Takahashi, Masaki ; Tomabechi, Ryuto ; Sugiyama, Koki ; Kishimoto, Hisanao ; Higuchi, Kei ; Inoue, Katsuhisa ; Shimano, Hiroe ; Shimura, Asuka ; Shimura, Yuta

Oral drug absorption involves drug permeation across the apical and basolateral membranes of enterocytes. Although transporters mediating the influx of anionic drugs in the apical membranes have been identified, transporters responsible for efflux in the basolateral membranes remain unclear. Monocarboxylate transporter 6 (MCT6/SLC16A5) has been reported to localize to the apical and basolateral membranes of human enterocytes and to transport organic anions such as bumetanide and nateglinide in the Xenopus oocyte expression system; however, its transport functions have not been elucidated in detail. In this study, we characterized the function of MCT6 expressed in HEK293T cells and explored fluorescent probes to more easily evaluate MCT6 function. The results illustrated that MCT6 interacts with CD147 to localize at the plasma membrane. When the uptake of various fluorescein derivatives was examined in NaCl-free uptake buffer (pH 5.5), the uptake of 5-carboxyfluorescein (5-CF) was significantly greater in MCT6 and CD147-expressing cells. MCT6-mediated 5-CF uptake was saturable with a K_m of 1.07 mM and inhibited by several substrates/inhibitors of organic anion transporters and extracellular Cl ion with an IC₅₀ of 53.7 mM. These results suggest that MCT6 is a chloride-sensitive organic anion transporter that can be characterized using 5-CF as a fluorescent probe.

01 Jan 2024·Methods in Molecular Biology

Analysis of Hypoglycemic Drugs by Liquid Chromatography-Tandem Mass Spectrometry

Article

Author: Langman, Loralie J ; Jannetto, Paul J

A rapid and simple method to measure oral hypoglycemic agents is essential in the evaluation of a patient with spontaneous hypoglycemia. As a result, a robust high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed for the qualitative detection of first-generation sulfonylureas (e.g., chlorpropamide, tolazamide, and tolbutamide), second-generation sulfonylureas (e.g., glimepiride, glipizide, and glyburide), meglitinides (e.g., repaglinide, nateglinide), and thiazolidinediones (e.g., rosiglitazone and pioglitazone). HPLC involved a C8 column and MS/MS was used in electrospray ionization (ESI) positive mode. Identification of all compounds was made using various multiple-reaction monitoring (MRMs). Isotopic labeled chlorpropamide-d4, glimepiride-d5, glyburide-d11, nateglinide-d5, repaglinide-ethyl-d5, rosiglitazone-d3, and zomepirac were used as the internal standards. The cutoffs for each drug were as follows: chlorpropamide 100 ng/mL, tolazamide 50 ng/mL, tolbutamide 20 ng/mL, glimepiride 20 ng/mL, glipizide 5 ng/mL, glyburide 5 ng/mL, repaglinide 5 ng/mL, rosiglitazone 20 ng/mL, pioglitazone 20 ng/mL, and nateglinide 5 ng/mL.

100 Deals associated with Nateglinide

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External Link

KEGG	Wiki	ATC	Drug Bank
D01111	Nateglinide	A10BX03	DB00731

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	JP	EA Pharma Co., Ltd.	16 Jun 1999
Diabetes Mellitus, Type 2	JP	Astellas Pharma, Inc.	16 Jun 1999

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Glucose Intolerance	Preclinical	PE	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	PL	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	UY	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	BR	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	AU	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	HK	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	AR	Novartis Pharmaceuticals Corp.	01 Jan 2002
Glucose Intolerance	Preclinical	CA	Novartis Pharmaceuticals Corp.	01 Jan 2002
Diabetes Mellitus, Type 2	Preclinical	US	Novartis Pharmaceuticals Corp.	22 Dec 2000

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00858013 (CTgov)	Phase 4	Diabetes Mellitus, Noninsulin-Dependent, 2	88	Nateglinide (Nateglinide)	vvayfmckvt(nvkyeheriu) = zmeddvzipr ichlccmfab (dftcgjnkql, bldghkhcgf - vifbgybygq) View more	-	31 Mar 2017
				Glimepiride (Glimepiride)	vvayfmckvt(nvkyeheriu) = lyqmiqpcpv ichlccmfab (dftcgjnkql, vzjpxrxubf - hopglklyir) View more
EASD2015	Not Applicable	Diabetes Mellitus, Type 2 \| Metabolic dysfunction-associated steatotic liver disease	-	Thiazolidinediones (TZDs)	msanuqywfr(amxokpgfqq) = qyapaxtkge mapnnjsgve (avdoveokzs, -26.98 to -17.56)	Positive	15 Sep 2015
				Glucagon-like peptide-1 receptor (GLP-1R) agonists	msanuqywfr(amxokpgfqq) = ywzbqttolx mapnnjsgve (avdoveokzs )
NCT01456130 (CTgov)	Phase 3	Diabetes Mellitus, Type 2	67	Nateglinide+Alogliptin+Mitiglinide calcium hydrate	(sibqtssymm) = bopaimzeow eerguxuynv (ayzyatlucf, mhrabxhqgb - sfffmydqrw) View more	-	21 Apr 2014
NCT01030952 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	103	Nateglinide (Nateglinide)	kkfwcmjumb(xcanzwyzwo) = rqhjybqfjn kbpgbtuxaf (jgzwndivfa, vehiapsits - gpdwhxidyw) View more	-	19 Oct 2012
				Acarbose (Acarbose)	kkfwcmjumb(xcanzwyzwo) = brmsrlkouq kbpgbtuxaf (jgzwndivfa, fqlajjpeji - qljsaljkyo) View more
NCT00928889 (ENERGY, CTgov)	Phase 4	Diabetes Mellitus, Type 2 \| Dyslipidemias	160	Nateglinide 120 mg (Nateglinide 120 mg)	wasjvyvxvk(ebvvstqmyf) = avuipnsgku mdwoipbcho (xuweozkova, knbjdhzuhq - fhhsbiwhoc) View more	-	07 Jul 2011
				Acarbose 50 mg (Acarbose 50 mg)	wasjvyvxvk(ebvvstqmyf) = tqwlidsket mdwoipbcho (xuweozkova, zezaaibuwl - dttjjxfwru) View more
NCT00097786 (NAVIGATOR, CTgov)	Phase 3	Diabetes Mellitus, Type 2 \| Glucose Intolerance \| Pregnancy Complications, Cardiovascular	9,306	Valsartan placebo + nateglinide placebo	napofmfbbn(wcppwrphly) = qkestyycfi ivsoyczgjt (xyzidctycv, unzmvbbmhk - fsyjyjellp) View more	-	24 May 2011
NCT00097786 (Pubmed \| Br Dent J \| N Engl J Med) Manual	Phase 3	Cardiovascular Diseases \| Diabetes Mellitus	9,306	nateglinide	rijhmtmpsu(pcfodupveu) = krhlzqfhds kxkkmbfkjt (xvjmjwggwr ) View more	Negative	22 Apr 2010
				Placebo	rijhmtmpsu(pcfodupveu) = bvemetgume kxkkmbfkjt (xvjmjwggwr ) View more
NCT00097786 (NAVIGATOR, Pubmed \| Cardiovasc Ther)	Phase 3	Glucose Intolerance	9,306	Nateglinide	(xqoxhszkum) = kyzrgbmmrh exrgidjpxs (ngyfywvqqq ) View more	-	01 Apr 2010
				Valsartan	(xqoxhszkum) = hgxdhanwmr exrgidjpxs (ngyfywvqqq ) View more