Identification

Name
Repaglinide
Accession Number
DB00912  (APRD00439)
Type
Small Molecule
Groups
Approved, Investigational
Description

Repaglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Repaglinide induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those naïve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Repaglinide is extensively metabolized in the liver and excreted in bile. Repaglinide metabolites do not possess appreciable hypoglycemic activity. Approximately 90% of a single orally administered dose is eliminated in feces and 8% in urine.

Structure
Thumb
Synonyms
  • AG-EE 388 ZW
  • AG-EE 623 ZW
  • Repaglinida
  • Repaglinidum
  • Surepost
External IDs
A10BX02 / AG-EE-623ZW
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act RepaglinideTablet0.5 mgOralActavis Pharma Company2010-10-18Not applicableCanada
Act RepaglinideTablet1 mgOralActavis Pharma Company2010-10-18Not applicableCanada
Act RepaglinideTablet2 mgOralActavis Pharma Company2010-10-18Not applicableCanada
Auro-repaglinideTablet1 mgOralAuro Pharma Inc2014-04-30Not applicableCanada
Auro-repaglinideTablet2 mgOralAuro Pharma Inc2014-04-30Not applicableCanada
Auro-repaglinideTablet0.5 mgOralAuro Pharma Inc2014-04-30Not applicableCanada
Gluconorm 0.5mgTablet0.5 mgOralNovo Nordisk1999-06-21Not applicableCanada
Gluconorm 1.0mgTablet1.0 mgOralNovo Nordisk1999-06-21Not applicableCanada
Gluconorm 2.0mgTablet2.0 mgOralNovo Nordisk1999-06-21Not applicableCanada
Mylan-repaglinideTablet2 mgOralMylan PharmaceuticalsNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-repaglinideTablet2.0 mgOralApotex Corporation2012-10-16Not applicableCanada
Apo-repaglinideTablet0.5 mgOralApotex Corporation2012-10-16Not applicableCanada
Apo-repaglinideTablet1.0 mgOralApotex Corporation2012-10-16Not applicableCanada
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet0.5 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet2 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
EnyglidTablet1 mgOralKrka, D.D., Novo Mesto2009-10-14Not applicableEu
International/Other Brands
GlucoNorm (Novo Nordisk) / Prandin
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
PrandiMetRepaglinide (2 mg/1) + Metformin Hydrochloride (500 mg/1)TabletOralNovo Nordisk2009-01-152017-06-02Us
PrandiMetRepaglinide (1 mg/1) + Metformin Hydrochloride (500 mg/1)TabletOralNovo Nordisk2009-01-162017-06-02Us
Repaglinide and Metformin HydrochlorideRepaglinide (2 mg/1) + Metformin Hydrochloride (500 mg/1)TabletOralLupin Pharmaceuticals2015-12-10Not applicableUs
Repaglinide and Metformin HydrochlorideRepaglinide (1 mg/1) + Metformin Hydrochloride (500 mg/1)TabletOralLupin Pharmaceuticals2015-12-10Not applicableUs
Categories
UNII
668Z8C33LU
CAS number
135062-02-1
Weight
Average: 452.5857
Monoisotopic: 452.26750765
Chemical Formula
C27H36N2O4
InChI Key
FAEKWTJYAYMJKF-QHCPKHFHSA-N
InChI
InChI=1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
IUPAC Name
2-ethoxy-4-({[(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl]carbamoyl}methyl)benzoic acid
SMILES
CCOC1=C(C=CC(CC(=O)N[[email protected]@H](CC(C)C)C2=CC=CC=C2N2CCCCC2)=C1)C(O)=O

Pharmacology

Indication

As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Structured Indications
Pharmacodynamics

Insulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. Extracellular glucose enters the cell via GLUT2 (SLC2A2) transporters. Once inside the cell, glucose is metabolized to produce ATP. High concentrations of ATP inhibit ATP-sensitive potassium channels causing membrane depolarization. When extracellular glucose concentrations are low, ATP-sensitive potassium channels open causing membrane repolarization. High glucose concentrations cause ATP-sensitive potassium channels to close resulting in membrane depolarization and opening of L-type calcium channels. The influx of calcium ions stimulates calcium-dependent exocytosis of insulin granules. Repaglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.

Mechanism of action

Repaglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, repaglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, repaglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of repaglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Repaglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.

TargetActionsOrganism
AATP-binding cassette sub-family C member 8
inhibitor
Human
UPeroxisome proliferator-activated receptor gamma
agonist
Human
Absorption

Rapidly and completely absorbed following oral administration. Peak plasma concentrations are observed within 1 hour (range 0.5-1.4 hours). The absolute bioavailability is approximately 56%. Maximal biological effect is observed within 3-3.5 hours and plasma insulin levels remain elevated for 4-6 hours. When a single 2 mg dose of repaglinide is given to healthy subjects, the area under the curve (AUC) is 18.0 - 18.7 (ng/mL/h)^3.

Volume of distribution

31 L following IV administration in healthy individuals

Protein binding

>98% (e.g. to to albumin and α1-acid glycoprotein)

Metabolism

Repaglinide is rapidly metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2). Further oxidation produces the aromatic amine derivative (M1). Glucuronidation of the carboxylic acid group of repaglinide yields an acyl glucuronide (M7). Several other unidentified metabolites have been detected. Repaglinide metabolites to not possess appreciable hypoglycemic activity.

Route of elimination

90% eliminated in feces (<2% as unchanged drug), 8% in urine (0.1% as unchanged drug)

Half life

1 hour

Clearance

33-38 L/hour following IV administration

Toxicity

LD50 >1 g/kg (rat) (W. Grell)

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Repaglinide Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,4-thiazolidinedione2,4-thiazolidinedione may increase the hypoglycemic activities of Repaglinide.Investigational
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Repaglinide.Experimental
AbirateroneThe serum concentration of Repaglinide can be increased when it is combined with Abiraterone.Approved
AcarboseAcarbose may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
AICA ribonucleotideAICA ribonucleotide may increase the hypoglycemic activities of Repaglinide.Experimental, Investigational
AlaproclateAlaproclate may increase the hypoglycemic activities of Repaglinide.Experimental
AllicinAllicin may increase the hypoglycemic activities of Repaglinide.Investigational
AlogliptinAlogliptin may increase the hypoglycemic activities of Repaglinide.Approved
AloxiprinAloxiprin may increase the hypoglycemic activities of Repaglinide.Experimental
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Repaglinide.Approved
AmiodaroneThe serum concentration of Repaglinide can be increased when it is combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Repaglinide can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Asenapine.Approved
AtazanavirThe serum concentration of Repaglinide can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Repaglinide can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Repaglinide is combined with Atorvastatin.Approved
BalaglitazoneBalaglitazone may increase the hypoglycemic activities of Repaglinide.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
Bempedoic acidBempedoic acid may increase the hypoglycemic activities of Repaglinide.Investigational
BendroflumethiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Repaglinide.Withdrawn
BetamethasoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BoceprevirThe serum concentration of Repaglinide can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Repaglinide can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Repaglinide can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Brexpiprazole.Approved
BrofaromineBrofaromine may increase the hypoglycemic activities of Repaglinide.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Repaglinide.Approved, Investigational
BuforminBuformin may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
BumetanideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Buserelin.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Repaglinide.Approved
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Repaglinide.Approved
CarbamazepineThe metabolism of Repaglinide can be increased when combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumCarbaspirin calcium may increase the hypoglycemic activities of Repaglinide.Experimental, Investigational
CarbomycinThe serum concentration of Repaglinide can be increased when it is combined with Carbomycin.Vet Approved
CarbutamideCarbutamide may increase the hypoglycemic activities of Repaglinide.Experimental
CaroxazoneCaroxazone may increase the hypoglycemic activities of Repaglinide.Withdrawn
CastanospermineCastanospermine may increase the hypoglycemic activities of Repaglinide.Experimental
CelecoxibThe metabolism of Repaglinide can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Repaglinide can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Repaglinide.Withdrawn
ChlorothiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Repaglinide.Approved
ChlorthalidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Chlorthalidone.Approved
CiglitazoneCiglitazone may increase the hypoglycemic activities of Repaglinide.Experimental
CinoxacinCinoxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the hypoglycemic activities of Repaglinide.Approved
ClarithromycinThe serum concentration of Repaglinide can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Repaglinide can be decreased when combined with Clemastine.Approved
ClopidogrelThe serum concentration of Repaglinide can be increased when it is combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Repaglinide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Clozapine.Approved
CobicistatThe serum concentration of Repaglinide can be increased when it is combined with Cobicistat.Approved
ConivaptanThe serum concentration of Repaglinide can be increased when it is combined with Conivaptan.Approved, Investigational
CorticotropinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Cortisone acetate.Approved
CrisaboroleThe metabolism of Repaglinide can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Repaglinide can be decreased when combined with Crizotinib.Approved
CyclopenthiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Cyclopenthiazide.Experimental
CyclosporineThe serum concentration of Repaglinide can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Repaglinide can be decreased when it is combined with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Repaglinide.Investigational
DarunavirThe serum concentration of Repaglinide can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Repaglinide can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Repaglinide can be increased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Repaglinide can be decreased when combined with Delavirdine.Approved
DeoxyspergualinDeoxyspergualin may increase the hypoglycemic activities of Repaglinide.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Repaglinide.Investigational
DesogestrelThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Repaglinide.Approved
DexamethasoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Diazoxide.Approved
DienogestThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Dienogest.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Repaglinide.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Repaglinide.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Repaglinide.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Repaglinide.Experimental
DihydroergotamineThe metabolism of Repaglinide can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Repaglinide.Illicit
DiltiazemThe metabolism of Repaglinide can be decreased when combined with Diltiazem.Approved
DisopyramideDisopyramide may increase the hypoglycemic activities of Repaglinide.Approved
DoxycyclineThe metabolism of Repaglinide can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Repaglinide can be decreased when combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Drospirenone.Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Repaglinide.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Repaglinide.Approved
EfavirenzThe metabolism of Repaglinide can be decreased when combined with Efavirenz.Approved, Investigational
EltrombopagThe serum concentration of Repaglinide can be increased when it is combined with Eltrombopag.Approved
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Repaglinide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
EnzalutamideThe serum concentration of Repaglinide can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Epinephrine.Approved, Vet Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Repaglinide.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Repaglinide.Approved
ErythromycinThe serum concentration of Repaglinide can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
EstradiolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethynodiol diacetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Repaglinide.Withdrawn
EverolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Everolimus.Approved
ExenatideExenatide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
FelodipineThe metabolism of Repaglinide can be decreased when combined with Felodipine.Approved, Investigational
FleroxacinFleroxacin may increase the hypoglycemic activities of Repaglinide.Approved
FluconazoleThe metabolism of Repaglinide can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Repaglinide.Withdrawn
FluoxetineFluoxetine may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Repaglinide.Approved, Illicit
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Repaglinide.Approved
FluvoxamineThe metabolism of Repaglinide can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Repaglinide can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Repaglinide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Repaglinide can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational, Vet Approved
FurosemideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Repaglinide can be increased when it is combined with Fusidic Acid.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Repaglinide.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
GemfibrozilThe serum concentration of Repaglinide can be increased when it is combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
GlibornurideGlibornuride may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
GliclazideRepaglinide may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideGlimepiride may increase the hypoglycemic activities of Repaglinide.Approved
GlipizideRepaglinide may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneGliquidone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
GLPG-0492GLPG-0492 may increase the hypoglycemic activities of Repaglinide.Investigational
GlyburideRepaglinide may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
GuacetisalGuacetisal may increase the hypoglycemic activities of Repaglinide.Experimental
GusperimusGusperimus may increase the hypoglycemic activities of Repaglinide.Investigational
HarmalineHarmaline may increase the hypoglycemic activities of Repaglinide.Experimental
Hemoglobin crosfumarilHemoglobin crosfumaril may increase the hypoglycemic activities of Repaglinide.Experimental
HistrelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Repaglinide.Experimental
HydrochlorothiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydroflumethiazide.Approved, Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Iloperidone.Approved
ImatinibThe metabolism of Repaglinide can be decreased when combined with Imatinib.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Indapamide.Approved
IndinavirThe serum concentration of Repaglinide can be increased when it is combined with Indinavir.Approved
Insulin AspartRepaglinide may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirRepaglinide may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Repaglinide.Approved
Insulin GlulisineRepaglinide may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Repaglinide.Approved
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Repaglinide.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Repaglinide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Repaglinide.Withdrawn
IrbesartanThe metabolism of Repaglinide can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Repaglinide can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Repaglinide.Approved
IsradipineThe metabolism of Repaglinide can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Repaglinide can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Repaglinide can be increased when it is combined with Ivacaftor.Approved
JosamycinThe serum concentration of Repaglinide can be increased when it is combined with Josamycin.Approved, Investigational
KetoconazoleThe serum concentration of Repaglinide can be increased when it is combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Repaglinide can be increased when it is combined with Kitasamycin.Experimental
LanreotideRepaglinide may increase the hypoglycemic activities of Lanreotide.Approved
LapatinibThe metabolism of Repaglinide can be decreased when combined with Lapatinib.Approved, Investigational
LeuprolideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Repaglinide.Approved
LevonorgestrelThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinagliptinLinagliptin may increase the hypoglycemic activities of Repaglinide.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Repaglinide.Approved, Nutraceutical
LiraglutideLiraglutide may increase the hypoglycemic activities of Repaglinide.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Repaglinide.Approved, Investigational
LopinavirThe serum concentration of Repaglinide can be increased when it is combined with Lopinavir.Approved
LosartanThe metabolism of Repaglinide can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Repaglinide can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Repaglinide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Repaglinide can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Lurasidone.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Repaglinide.Illicit, Investigational, Withdrawn
MebanazineMebanazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
MecaserminRepaglinide may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Repaglinide.Approved
MesteroloneMesterolone may increase the hypoglycemic activities of Repaglinide.Experimental
MestranolThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Mestranol.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Repaglinide.Experimental
MetforminMetformin may increase the hypoglycemic activities of Repaglinide.Approved
MethotrimeprazineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Repaglinide.Approved
MethylprednisoloneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Repaglinide.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Repaglinide.Approved
MetolazoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Metolazone.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Repaglinide.Experimental
MifepristoneThe serum concentration of Repaglinide can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolMiglitol may increase the hypoglycemic activities of Repaglinide.Approved
MiglustatMiglustat may increase the hypoglycemic activities of Repaglinide.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Repaglinide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Repaglinide.Approved
MitiglinideMitiglinide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
MitotaneThe serum concentration of Repaglinide can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Repaglinide.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
NandroloneNandrolone may increase the hypoglycemic activities of Repaglinide.Experimental, Investigational
NateglinideNateglinide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
NefazodoneThe serum concentration of Repaglinide can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Repaglinide can be increased when it is combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Repaglinide.Investigational
NetupitantThe serum concentration of Repaglinide can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Repaglinide can be increased when combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Repaglinide.Withdrawn
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Repaglinide.Approved, Investigational
NilotinibThe metabolism of Repaglinide can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Repaglinide.Investigational
NorethisteroneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Repaglinide.Approved
NorgestimateThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Repaglinide.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
OlanzapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Repaglinide can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Repaglinide can be increased when it is combined with Oleandomycin.Vet Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Repaglinide.Approved
OsimertinibThe serum concentration of Repaglinide can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
Oxolinic acidOxolinic acid may increase the hypoglycemic activities of Repaglinide.Experimental
OxymetholoneOxymetholone may increase the hypoglycemic activities of Repaglinide.Approved, Illicit
PalbociclibThe serum concentration of Repaglinide can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Paliperidone.Approved
PargylinePargyline may increase the hypoglycemic activities of Repaglinide.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
PasireotideRepaglinide may increase the hypoglycemic activities of Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Repaglinide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Repaglinide.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Repaglinide.Approved
PentamidinePentamidine may increase the hypoglycemic activities of Repaglinide.Approved
PentobarbitalThe metabolism of Repaglinide can be increased when combined with Pentobarbital.Approved, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Repaglinide.Approved, Investigational, Vet Approved, Withdrawn
PhenelzinePhenelzine may increase the hypoglycemic activities of Repaglinide.Approved
PhenforminPhenformin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational, Withdrawn
PheniprazinePheniprazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
PhenobarbitalThe metabolism of Repaglinide can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
PhenytoinThe metabolism of Repaglinide can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Repaglinide can be decreased when combined with Pioglitazone.Approved, Investigational
Pipemidic acidPipemidic acid may increase the hypoglycemic activities of Repaglinide.Experimental
PiperazineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Pipotiazine.Approved, Investigational
PirlindolePirlindole may increase the hypoglycemic activities of Repaglinide.Approved
Piromidic acidPiromidic acid may increase the hypoglycemic activities of Repaglinide.Experimental
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Repaglinide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
PolythiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Polythiazide.Approved
PosaconazoleThe serum concentration of Repaglinide can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintidePramlintide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Repaglinide.Approved
PrednisoloneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Repaglinide can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Progesterone.Approved, Vet Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Repaglinide.Investigational
QuetiapineThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Quinethazone.Approved
QuinineQuinine may increase the hypoglycemic activities of Repaglinide.Approved
RabeprazoleThe metabolism of Repaglinide can be decreased when combined with Rabeprazole.Approved, Investigational
RanolazineThe metabolism of Repaglinide can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Repaglinide.Approved
RifabutinThe metabolism of Repaglinide can be increased when combined with Rifabutin.Approved
RifampicinThe serum concentration of Repaglinide can be decreased when it is combined with Rifampicin.Approved
RifapentineThe metabolism of Repaglinide can be increased when combined with Rifapentine.Approved
RisperidoneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe serum concentration of Repaglinide can be increased when it is combined with Ritonavir.Approved, Investigational
RosiglitazoneThe metabolism of Repaglinide can be decreased when combined with Rosiglitazone.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Repaglinide.Approved
RufloxacinRufloxacin may increase the hypoglycemic activities of Repaglinide.Experimental
SafrazineSafrazine may increase the hypoglycemic activities of Repaglinide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
SaquinavirThe serum concentration of Repaglinide can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Repaglinide.Approved
SecobarbitalThe metabolism of Repaglinide can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Repaglinide.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Repaglinide.Approved
SildenafilThe metabolism of Repaglinide can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Repaglinide can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Repaglinide can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Repaglinide.Approved
SirolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Sirolimus.Approved, Investigational
SitafloxacinSitafloxacin may increase the hypoglycemic activities of Repaglinide.Experimental, Investigational
SitagliptinSitagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
SolithromycinThe serum concentration of Repaglinide can be increased when it is combined with Solithromycin.Investigational
SotagliflozinSotagliflozin may increase the hypoglycemic activities of Repaglinide.Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
St. John's WortThe serum concentration of Repaglinide can be decreased when it is combined with St. John&#39;s Wort.Investigational, Nutraceutical
StanozololStanozolol may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
StiripentolThe serum concentration of Repaglinide can be increased when it is combined with Stiripentol.Approved
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
SulfamethoxazoleRepaglinide may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleSulfisoxazole may increase the hypoglycemic activities of Repaglinide.Approved, Vet Approved
SulodexideSulodexide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
SunitinibRepaglinide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tacrolimus.Approved, Investigational
TamoxifenThe metabolism of Repaglinide can be decreased when combined with Tamoxifen.Approved
TelaprevirThe serum concentration of Repaglinide can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Repaglinide can be increased when it is combined with Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Repaglinide.Withdrawn
TemsirolimusThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Temsirolimus.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Repaglinide.Experimental
TeriflunomideThe serum concentration of Repaglinide can be increased when it is combined with Teriflunomide.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
TiclopidineThe metabolism of Repaglinide can be decreased when combined with Ticlopidine.Approved
TipranavirThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Repaglinide can be decreased when it is combined with Tocilizumab.Approved
TolazamideTolazamide may increase the hypoglycemic activities of Repaglinide.Approved
TolbutamideRepaglinide may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Repaglinide.Approved
TopiroxostatThe metabolism of Repaglinide can be decreased when combined with Topiroxostat.Approved, Investigational
TorasemideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Repaglinide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Repaglinide.Approved
TriamcinoloneThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimethoprimThe metabolism of Repaglinide can be decreased when combined with Trimethoprim.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneTroglitazone may increase the hypoglycemic activities of Repaglinide.Investigational, Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational, Withdrawn
TylosinThe serum concentration of Repaglinide can be increased when it is combined with Tylosin.Vet Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Repaglinide.Approved, Experimental
VenlafaxineThe metabolism of Repaglinide can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Repaglinide can be decreased when combined with Verapamil.Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
VogliboseVoglibose may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
VoriconazoleThe serum concentration of Repaglinide can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Vorinostat.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Repaglinide.Withdrawn
ZiprasidoneThe metabolism of Repaglinide can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take up to 30 minutes before meals.
  • When taken with a high-fat meal, AUC and Cmax decreases.

References

Synthesis Reference

Manne Reddy, "Polymorphic forms of (S)-Repaglinide and the processes for preparation thereof." U.S. Patent US20040102477, issued May 27, 2004.

US20040102477
General References
  1. Massi-Benedetti M, Damsbo P: Pharmacology and clinical experience with repaglinide. Expert Opin Investig Drugs. 2000 Apr;9(4):885-98. [PubMed:11060717]
External Links
Human Metabolome Database
HMDB15048
KEGG Drug
D00594
KEGG Compound
C07670
PubChem Compound
65981
PubChem Substance
46508150
ChemSpider
59377
BindingDB
50153520
ChEBI
8805
ChEMBL
CHEMBL1272
Therapeutic Targets Database
DAP000133
PharmGKB
PA451234
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Repaglinide
ATC Codes
A10BD14 — Metformin and repaglinideA10BX02 — Repaglinide
AHFS Codes
  • 68:20.16 — Meglitinides
FDA label
Download (175 KB)
MSDS
Download (57.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceDrug-Drug Interaction (DDI) / Healthy Volunteers1
1CompletedBasic ScienceHealthy Volunteers / Pharmacokinetics of Caffeine / Pharmacokinetics of Repaglinide1
1CompletedTreatmentDiabetes / Healthy Volunteers1
1CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus2
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentParkinson's Disease (PD)1
1RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL) / Mantle Cell Lymphoma (MCL) / Primary Mediastinal Lymphoma1
2CompletedTreatmentType 2 Diabetes Mellitus1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / Hypercholesterolaemia / Hypertensive / Type 2 Diabetes Mellitus1
3CompletedTreatmentCystic Fibrosis (CF) / Diabetes Mellitus (DM)2
3CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus2
4CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus10
4CompletedTreatmentType 2 Diabetes Mellitus4
4RecruitingTreatmentType 2 Diabetes Mellitus2
4TerminatedTreatmentDiabetes / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingTreatmentDiabetes1
Not AvailableCompletedNot AvailableCystic Fibrosis Related Diabetes / Pancreatic Insufficiency1
Not AvailableCompletedNot AvailableDiabetes / Type 2 Diabetes Mellitus6
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus3
Not AvailableUnknown StatusNot AvailableType 2 Diabetes Mellitus1
Not AvailableWithdrawnTreatmentDiabetes1

Pharmacoeconomics

Manufacturers
  • Novo nordisk inc
  • Novo Nordisk Inc.
Packagers
Dosage forms
FormRouteStrength
TabletOral1 mg
TabletOral2 mg
TabletOral0.5 mg
TabletOral1.0 mg
TabletOral2.0 mg
TabletOral
PillOral1 mg/mg
PillOral2 mg/mg
TabletOral.5 mg/1
TabletOral1 mg/1
TabletOral2 mg/1
TabletOral5 mg
Prices
Unit descriptionCostUnit
Prandin 1 mg tablet2.48USD tablet
Prandin 0.5 mg tablet2.47USD tablet
Prandin 2 mg tablet2.33USD tablet
Gluconorm 2 mg Tablet0.34USD tablet
Gluconorm 1 mg Tablet0.32USD tablet
Gluconorm 0.5 mg Tablet0.31USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6677358No1998-06-122018-06-12Us
CA2111851No2002-02-262011-06-21Canada

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)130-131 °CNot Available
logP5.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00294 mg/mLALOGPS
logP5.05ALOGPS
logP3.95ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)3.68ChemAxon
pKa (Strongest Basic)4.82ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area78.87 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity131.83 m3·mol-1ChemAxon
Polarizability51.49 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9172
Blood Brain Barrier-0.7101
Caco-2 permeable-0.5891
P-glycoprotein substrateSubstrate0.8145
P-glycoprotein inhibitor IInhibitor0.6044
P-glycoprotein inhibitor IIInhibitor0.6868
Renal organic cation transporterNon-inhibitor0.849
CYP450 2C9 substrateNon-substrate0.8288
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.7019
CYP450 1A2 substrateNon-inhibitor0.9206
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9264
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.8136
CarcinogenicityNon-carcinogens0.8004
BiodegradationNot ready biodegradable0.919
Rat acute toxicity2.4497 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9605
hERG inhibition (predictor II)Non-inhibitor0.5272
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0udi-0000900000-c0108433e6c3f3bf1c75
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-004i-0009000000-30aa31031f07d8ae52b8
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-002r-0908000000-b76282b9697187110f0a
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0000900000-2f6de321d96a7df0cde9
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0140900000-4fef8b8042e88aa84955
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-001i-0290000000-4867f74dff429e78bb45
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-001i-0290000000-bdb018b622ca04e9d8b1
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-001i-0590000000-60f613e4ee0d364efcea
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0f89-2791700000-333192fa8176a2febaa5

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Piperidines
Sub Class
Phenylpiperidines
Direct Parent
Phenylpiperidines
Alternative Parents
Phenylacetamides / Benzoic acids / Aniline and substituted anilines / Benzoyl derivatives / Dialkylarylamines / Phenol ethers / Phenoxy compounds / Alkyl aryl ethers / Amino acids / Secondary carboxylic acid amides
show 7 more
Substituents
Phenylpiperidine / Phenylacetamide / Benzoic acid or derivatives / Benzoic acid / Phenoxy compound / Benzoyl / Phenol ether / Tertiary aliphatic/aromatic amine / Dialkylarylamine / Aniline or substituted anilines
show 23 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
piperidines (CHEBI:8805)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Sulfonylurea receptor activity
Specific Function
Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
Gene Name
ABCC8
Uniprot ID
Q09428
Uniprot Name
ATP-binding cassette sub-family C member 8
Molecular Weight
176990.36 Da
References
  1. Hu S, Wang S, Fanelli B, Bell PA, Dunning BE, Geisse S, Schmitz R, Boettcher BR: Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: A comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther. 2000 May;293(2):444-52. [PubMed:10773014]
  2. Sunaga Y, Gonoi T, Shibasaki T, Ichikawa K, Kusama H, Yano H, Seino S: 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. Eur J Pharmacol. 2001 Nov 9;431(1):119-25. [PubMed:11716850]
  3. Hansen AM, Christensen IT, Hansen JB, Carr RD, Ashcroft FM, Wahl P: Differential interactions of nateglinide and repaglinide on the human beta-cell sulphonylurea receptor 1. Diabetes. 2002 Sep;51(9):2789-95. [PubMed:12196472]
  4. Wangler B, Schneider S, Thews O, Schirrmacher E, Comagic S, Feilen P, Schwanstecher C, Schwanstecher M, Shiue CY, Alavi A, Hohnemann S, Piel M, Rosch F, Schirrmacher R: Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbam oyl]-methyl)-benzoic acid ([18F]repaglinide): a promising radioligand for quantification of pancreatic beta-cell mass with positron emission tomography (PET). Nucl Med Biol. 2004 Jul;31(5):639-47. [PubMed:15219283]
  5. Wangler B, Beck C, Shiue CY, Schneider S, Schwanstecher C, Schwanstecher M, Feilen PJ, Alavi A, Rosch F, Schirrmacher R: Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-be nzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5205-9. [PubMed:15380228]
  6. Dornhorst A: Insulinotropic meglitinide analogues. Lancet. 2001 Nov 17;358(9294):1709-16. [PubMed:11728565]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE...
Gene Name
PPARG
Uniprot ID
P37231
Uniprot Name
Peroxisome proliferator-activated receptor gamma
Molecular Weight
57619.58 Da
References
  1. Scarsi M, Podvinec M, Roth A, Hug H, Kersten S, Albrecht H, Schwede T, Meyer UA, Rucker C: Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach. Mol Pharmacol. 2007 Feb;71(2):398-406. Epub 2006 Nov 2. [PubMed:17082235]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14. [PubMed:12919179]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14. [PubMed:12919179]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. He J, Qiu Z, Li N, Yu Y, Lu Y, Han D, Li T, Zhao D, Sun W, Fang F, Zheng J, Fan H, Chen X: Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. Eur J Clin Pharmacol. 2011 Jul;67(7):701-7. doi: 10.1007/s00228-011-0994-7. Epub 2011 Feb 17. [PubMed:21327909]

Drug created on June 13, 2005 07:24 / Updated on November 13, 2017 21:49