MITIGLINIDE

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C19H25NO3
Molecular Weight	315.4067
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)[C@H](CC(=O)N1C[C@H]2CCCC[C@H]2C1)CC3=CC=CC=C3

InChI

InChIKey=WPGGHFDDFPHPOB-BBWFWOEESA-N

InChI=1S/C19H25NO3/c21-18(20-12-15-8-4-5-9-16(15)13-20)11-17(19(22)23)10-14-6-2-1-3-7-14/h1-3,6-7,15-17H,4-5,8-13H2,(H,22,23)/t15-,16+,17-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C19H25NO3
Molecular Weight	315.4067
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.pharmacodia.com/yaodu/html/v1/chemicals/a1d33d0dfec820b41b54430b50e96b5c.html#onlineretailersBasic

Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Kir6.2/SUR1 3 Target ID: CHEMBL3038487 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11264248	Inhibitor 8504		4.0 nM [IC50]
Sulfonylurea receptor 2, Kir6.2 11 Target ID: CHEMBL2095198 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11264248	Inhibitor 8504		3.0 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: https://www.pharmacodia.com/yaodu/html/v1/chemicals/a1d33d0dfec820b41b54430b50e96b5c.html#onlineretailersBasic	Primary		Approved 8583	Glufast Approved Use Unknown Launch Date 2004

C_max

Value	Dose	Co-administered	Analyte	Population
683.2 μg/L CLINICAL TRIAL https://link.springer.com/article/10.1007/s40261-012-0012-6	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: Metformin	Metformin	MITIGLINIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
704 μg/L CLINICAL TRIAL https://link.springer.com/article/10.1007/s40261-012-0012-6	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: Metformin	Metformin	MITIGLINIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
915.1 μg × h/L CLINICAL TRIAL https://link.springer.com/article/10.1007/s40261-012-0012-6	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: Metformin	Metformin	MITIGLINIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1025.5 μg × h/L CLINICAL TRIAL https://link.springer.com/article/10.1007/s40261-012-0012-6	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: Metformin	Metformin	MITIGLINIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.19 h CLINICAL TRIAL https://link.springer.com/article/10.1007/s40261-012-0012-6	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: Metformin	Metformin	MITIGLINIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.67 h CLINICAL TRIAL https://link.springer.com/article/10.1007/s40261-012-0012-6	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: Metformin	Metformin	MITIGLINIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

PubMed

Title	Date	PubMed
Effects of S 21403 on hormone secretion from isolated rat pancreas at different glucose concentrations.	2002 Dec 5	12450580
[Mitiglinide (KAD-1229)].	2002 Sep	12387051
[Nateglinide and mitiglinide].	2003 Jul	12877090
[Pharmacological and clinical profile of mitiglinide calcium hydrate (Glufast), a new insulinotropic agent with rapid onset].	2004 Oct	15467258
[Effects of mitiglinide in treatment of impaired glucose tolerance].	2005 Feb	15779420
[Glinide(s), sulfonylurea(s)].	2006 Nov	17087304
Long-term effect of combination therapy with mitiglinide and once daily insulin glargine in patients who were successfully switched from intensive insulin therapy in short-term study.	2007 Feb	17185877
High-performance liquid chromatography-electrospray ionization mass spectrometry determination of mitiglinide in human plasma and its pharmacokinetics.	2007 Feb	17173338
Nateglinide and mitiglinide, but not sulfonylureas, induce insulin secretion through a mechanism mediated by calcium release from endoplasmic reticulum.	2007 Jul	17409272
Carboxyl-glucuronidation of mitiglinide by human UDP-glucuronosyltransferases.	2007 Jun 1	17359941
Mitiglinide, a novel oral hypoglycemic agent, preserves the cardioprotective effect of ischemic preconditioning in isolated perfused rat hearts.	2007 May	17592198
Miglitol increases the adiponectin level and decreases urinary albumin excretion in patients with type 2 diabetes mellitus.	2007 Nov	17950094
Quantitative determination of mitiglinide in human plasma by ultra-performance liquid chromatography/electrospray ionization tandem mass spectrometry.	2008 Jun 1	18486570
Ca(2+) channels on the move.	2009 Dec 29	19928968
Multicentre, double-blind, randomized study of mitiglinide compared with nateglinide in type 2 diabetes mellitus patients in China.	2009 May-Jun	19589264
Effect of mitiglinide on Streptozotocin-induced experimental type 2 diabetic rats: a urinary metabonomics study based on ultra-performance liquid chromatography-tandem mass spectrometry.	2009 Nov 1	19748326
Efficacy and safety of mitiglinide in diabetic patients on maintenance hemodialysis.	2010	20467165
Combination therapy with mitiglinide and voglibose improves glycemic control in type 2 diabetic patients on hemodialysis.	2010 Feb	20025554

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose is 10 mg three times daily just before each meal (within 5 minutes).

Route of Administration: Oral

In Vitro Use Guide

3T3-L1 cells were challenged during the first 4 days of differentiation with Mitiglinide at 1, 10 and 100 mkM. Seven days after the induction of 3T3-L1 cells, oil red O staining was used to detect triglyceride accumulation in 3T3-L1 cells.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:26:03 GMT 2025` Edited by `admin` on `Mon Mar 31 18:26:03 GMT 2025`
Record UNII	D86I0XLB13
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MITIGLINIDE

Official Name

English

MITIGLINIDE [MI]

Preferred Name

English

(-)-(2S,3A,7A-CIS)-A-BENZYLHEXAHYDRO-.GAMMA.-OXO-2-ISOINDOLINEBUTYRIC ACID

Common Name

English

mitiglinide [INN]

Common Name

English

Mitiglinide [WHO-DD]

Common Name

English

MITIGLINIDE [MART.]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C98079