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

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	MOL RATIO 1 MOL RATIO (average)

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

Description

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	Inhibitor 8,504		4.0 nM [IC50]
Sulfonylurea receptor 2, Kir6.2 11	Inhibitor 8,504		3.0 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262	Primary		Approved 8,583	Glufast

C_max

Value	Dose	Co-administered	Analyte	Population
683.2 μg/L	10 mg single, oral	Metformin	MITIGLINIDE plasma	Homo sapiens
704 μg/L	10 mg single, oral	Metformin	MITIGLINIDE plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
915.1 μg × h/L	10 mg single, oral	Metformin	MITIGLINIDE plasma	Homo sapiens
1025.5 μg × h/L	10 mg single, oral	Metformin	MITIGLINIDE plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.19 h	10 mg single, oral	Metformin	MITIGLINIDE plasma	Homo sapiens
2.67 h	10 mg single, oral	Metformin	MITIGLINIDE plasma	Homo sapiens

PubMed

Show entries

Title	Date	PubMed
Insulinotropic meglitinide analogues.	2001 Nov 17	11728565
Absence of exacerbation of myocardial stunning in anesthetized dogs treated with KAD-1229, a novel hypoglycemic agent.	2001 Nov 23	11730726
The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide.	2001 Nov 9	11716850
Therapeutic efficacy of mitiglinide combined with once daily insulin glargine after switching from multiple daily insulin regimen of aspart insulin and glargine in patients with type 2 diabetes mellitus.	2006 Feb	16543674
Imaging docking and fusion of insulin granules induced by antidiabetes agents: sulfonylurea and glinide drugs preferentially mediate the fusion of newcomer, but not previously docked, insulin granules.	2006 Oct	17003348

Showing 1 to 5 of 14 entries

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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.