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
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 |
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 |
---|---|---|---|
Target ID: CHEMBL3038487 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11264248 |
4.0 nM [IC50] | ||
Target ID: CHEMBL2095198 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11264248 |
3.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Glufast Approved UseUnknown Launch Date2004 |
Cmax
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 |
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 |
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 |
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 |
MITIGLINIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
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 |
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 |
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 |
|
[Mitiglinide (KAD-1229)]. | 2002 Sep |
|
[Nateglinide and mitiglinide]. | 2003 Jul |
|
[Pharmacological and clinical profile of mitiglinide calcium hydrate (Glufast), a new insulinotropic agent with rapid onset]. | 2004 Oct |
|
[Effects of mitiglinide in treatment of impaired glucose tolerance]. | 2005 Feb |
|
[Glinide(s), sulfonylurea(s)]. | 2006 Nov |
|
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 |
|
High-performance liquid chromatography-electrospray ionization mass spectrometry determination of mitiglinide in human plasma and its pharmacokinetics. | 2007 Feb |
|
Nateglinide and mitiglinide, but not sulfonylureas, induce insulin secretion through a mechanism mediated by calcium release from endoplasmic reticulum. | 2007 Jul |
|
Carboxyl-glucuronidation of mitiglinide by human UDP-glucuronosyltransferases. | 2007 Jun 1 |
|
Mitiglinide, a novel oral hypoglycemic agent, preserves the cardioprotective effect of ischemic preconditioning in isolated perfused rat hearts. | 2007 May |
|
Miglitol increases the adiponectin level and decreases urinary albumin excretion in patients with type 2 diabetes mellitus. | 2007 Nov |
|
Quantitative determination of mitiglinide in human plasma by ultra-performance liquid chromatography/electrospray ionization tandem mass spectrometry. | 2008 Jun 1 |
|
Ca(2+) channels on the move. | 2009 Dec 29 |
|
Multicentre, double-blind, randomized study of mitiglinide compared with nateglinide in type 2 diabetes mellitus patients in China. | 2009 May-Jun |
|
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 |
|
Efficacy and safety of mitiglinide in diabetic patients on maintenance hemodialysis. | 2010 |
|
Combination therapy with mitiglinide and voglibose improves glycemic control in type 2 diabetic patients on hemodialysis. | 2010 Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.pharmacodia.com/yaodu/html/v1/chemicals/a1d33d0dfec820b41b54430b50e96b5c.html#onlineretailersBasic
Curator's Comment: https://clinicaltrials.gov/ct2/show/NCT02143765
The recommended dose is 10 mg three times daily just before each meal (within 5 minutes).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18191001
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
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admin
on
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Mon Mar 31 18:26:03 GMT 2025
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Record UNII |
D86I0XLB13
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Record Status |
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C98079
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C087255
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MITIGLINIDE
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |