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Identification
NameNateglinide
Accession NumberDB00731  (APRD00593)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionNateglinide 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. Nateglinide is an amino acid derivative that 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. Nateglinide is extensively metabolized in the liver and excreted in urine (83%) and feces (10%). The major metabolites possess less activity than the parent compound. One minor metabolite, the isoprene, has the same potency as its parent compound.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet60 mg/1OralNovartis Pharmaceuticals Corporation2000-12-04Not applicableUs
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet120 mg/1OralNovartis Pharmaceuticals Corporation2000-12-04Not applicableUs
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated60 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated180 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
StarlixTablet, film coated120 mgOralNovartis Europharm Ltd2001-04-03Not applicableEu
Starlix 120mgTablet120 mgOralNovartis Pharmaceuticals Canada Inc2002-03-052015-07-13Canada
Starlix 180mgTablet180 mgOralNovartis Pharmaceuticals Canada Inc2002-03-052009-02-19Canada
Starlix 60mgTablet60 mgOralNovartis Pharmaceuticals Canada Inc2002-03-052015-07-13Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NateglinideTablet, coated60 mg/1OralGolden State Medical Supply, Inc.2015-09-10Not applicableUs
NateglinideTablet60 mg/1OralWatson Laboratories, Inc.2011-03-30Not applicableUs
NateglinideTablet, film coated60 mg/1OralCadila Healthcare Limited2016-10-27Not applicableUs
NateglinideTablet, coated60 mg/1OralAv Kare, Inc.2016-04-06Not applicableUs
NateglinideTablet, coated120 mg/1OralPhysicians Total Care, Inc.2011-05-03Not applicableUs
NateglinideTablet, coated120 mg/1OralGolden State Medical Supply, Inc.2015-09-10Not applicableUs
NateglinideTablet, film coated120 mg/1OralCadila Healthcare Limited2016-10-27Not applicableUs
NateglinideTablet120 mg/1OralWatson Laboratories, Inc.2011-03-30Not applicableUs
NateglinideTablet, coated120 mg/1OralAv Kare, Inc.2016-04-06Not applicableUs
NateglinideTablet60 mg/1OralDr. Reddy's Laboratories Limited2009-09-09Not applicableUs
NateglinideTablet, coated60 mg/1OralAmerican Health Packaging2011-01-18Not applicableUs
NateglinideTablet, coated60 mg/1OralPar Pharmaceutical, Inc.2009-09-08Not applicableUs
NateglinideTablet, coated60 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2009-09-08Not applicableUs
NateglinideTablet, film coated60 mg/1OralZydus Pharmaceuticals (USA) Inc.2016-10-27Not applicableUs
NateglinideTablet120 mg/1OralDr. Reddy's Laboratories Limited2009-09-09Not applicableUs
NateglinideTablet, coated120 mg/1OralAmerican Health Packaging2011-01-18Not applicableUs
NateglinideTablet, coated120 mg/1OralPar Pharmaceutical, Inc.2009-09-08Not applicableUs
NateglinideTablet, coated120 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2009-09-08Not applicableUs
NateglinideTablet, film coated120 mg/1OralZydus Pharmaceuticals (USA) Inc.2016-10-27Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TrazecTablet, film coated120 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated60 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated180 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated60 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated120 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated60 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated180 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated120 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated120 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated60 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated180 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated120 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated180 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated60 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
TrazecTablet, film coated180 mgOralNovartis Europharm Ltd.2001-04-03Not applicableEu
International Brands
NameCompany
FasticNot Available
StarsisNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
SDZ-DJN 608
ThumbNot applicableDBSALT000922
Categories
UNII41X3PWK4O2
CAS number105816-04-4
WeightAverage: 317.4226
Monoisotopic: 317.199093735
Chemical FormulaC19H27NO3
InChI KeyOELFLUMRDSZNSF-YJEKIOLLSA-N
InChI
InChI=1S/C19H27NO3/c1-13(2)15-8-10-16(11-9-15)18(21)20-17(19(22)23)12-14-6-4-3-5-7-14/h3-7,13,15-17H,8-12H2,1-2H3,(H,20,21)(H,22,23)/t15?,16-,17-/m1/s1
IUPAC Name
(2R)-3-phenyl-2-{[4-(propan-2-yl)cyclohexyl]formamido}propanoic acid
SMILES
CC(C)C1CC[C@@H](CC1)C(=O)N[[email protected]](CC1=CC=CC=C1)C(O)=O
Pharmacology
IndicationFor the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
Structured Indications
PharmacodynamicsInsulin 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. Nateglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.
Mechanism of actionNateglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, nateglinide 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, nateglinide 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 nateglinide 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). Nateglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.
TargetKindPharmacological actionActionsOrganismUniProt ID
ATP-binding cassette sub-family C member 8Proteinyes
inhibitor
HumanQ09428 details
Peroxisome proliferator-activated receptor gammaProteinunknown
agonist
HumanP37231 details
Related Articles
AbsorptionRapidly absorbed following oral administration prior to a meal, absolute bioavailability is estimated to be approximately 73%. Peak plasma concentrations generally occur within 1 hour of oral administration. Onset of action is <20 minutes and the duration of action is approximately 4 hours.
Volume of distribution

10 liters in healthy subjects

Protein binding98% bound to serum proteins, primarily serum albumin and to a lesser extent α1 acid glycoprotein
Metabolism

Hepatic, via cytochrome P450 isoenzymes CYP2C9 (70%) and CYP3A4 (30%). Metabolism is via hydroxylation followed by glucuronidation. The major metabolites have less antidiabetic activity than nateglinide, but the isoprene minor metabolite has antidiabetic activity comparable to that of nateglinide.

SubstrateEnzymesProduct
Nateglinide
Nateglinide metabolite M2/M3Details
Nateglinide metabolite M2/M3
Not Available
Nateglinide metabolite M11/M12Details
Nateglinide
Nateglinide metabolite M1Details
Nateglinide metabolite M1
Not Available
Nateglinide metabolite M11/M12Details
Nateglinide
Not Available
Nateglinide metabolite M7Details
Nateglinide metabolite M7
Not Available
Nateglinide metabolite M11/M12Details
Nateglinide
Nateglinide glucuronide and isomers (M4/M5/M6)Details
Route of eliminationUrine (83%) and feces (10%)
Half life1.5 hours
ClearanceNot Available
ToxicityAn overdose may result in an exaggerated glucose-lowering effect with the development of hypoglycemic symptoms.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Nateglinide Action PathwayDrug actionSMP00453
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Nateglinide.Experimental
AbirateroneThe serum concentration of Nateglinide can be increased when it is combined with Abiraterone.Approved
AcarboseAcarbose may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Nateglinide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Nateglinide.Approved, Vet Approved
AicarAicar may increase the hypoglycemic activities of Nateglinide.Experimental
AlogliptinAlogliptin may increase the hypoglycemic activities of Nateglinide.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Nateglinide.Approved
AmiodaroneThe metabolism of Nateglinide can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Nateglinide can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArtemetherThe metabolism of Nateglinide can be decreased when combined with Artemether.Approved
ArticaineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Asenapine.Approved
AtazanavirThe metabolism of Nateglinide can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Nateglinide can be decreased when combined with Atomoxetine.Approved
BalaglitazoneBalaglitazone may increase the hypoglycemic activities of Nateglinide.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Nateglinide.Withdrawn
BetamethasoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BetaxololThe metabolism of Nateglinide can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Nateglinide can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Nateglinide can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Nateglinide can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Nateglinide can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Brexpiprazole.Approved
BuforminBuformin may increase the hypoglycemic activities of Nateglinide.Withdrawn
BumetanideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Bumetanide.Approved
BupropionThe metabolism of Nateglinide can be decreased when combined with Bupropion.Approved
BuserelinThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Buserelin.Approved
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Nateglinide.Approved
CapecitabineThe metabolism of Nateglinide can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Nateglinide can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypoglycemic activities of Nateglinide.Withdrawn
CastanospermineCastanospermine may increase the hypoglycemic activities of Nateglinide.Experimental
CelecoxibThe metabolism of Nateglinide can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Nateglinide can be increased when it is combined with Ceritinib.Approved
ChloroquineThe metabolism of Nateglinide can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorothiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpromazineThe metabolism of Nateglinide can be decreased when combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Nateglinide.Approved
ChlorthalidoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Chlorthalidone.Approved
CholecalciferolThe metabolism of Nateglinide can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CiglitazoneCiglitazone may increase the hypoglycemic activities of Nateglinide.Experimental
CimetidineThe metabolism of Nateglinide can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Nateglinide can be decreased when combined with Cinacalcet.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Nateglinide.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
CitalopramThe metabolism of Nateglinide can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Nateglinide can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Nateglinide can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Nateglinide can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Nateglinide can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Nateglinide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Nateglinide can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Nateglinide can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Nateglinide can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Nateglinide can be increased when it is combined with Conivaptan.Approved, Investigational
CorticotropinThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Cortisone acetate.Approved
CrizotinibThe metabolism of Nateglinide can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Nateglinide can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Nateglinide can be decreased when it is combined with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Nateglinide.Investigational
DarifenacinThe metabolism of Nateglinide can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Nateglinide can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Nateglinide can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Nateglinide can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Nateglinide can be decreased when combined with Delavirdine.Approved
DeoxyspergualinDeoxyspergualin may increase the hypoglycemic activities of Nateglinide.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Nateglinide.Investigational
DesipramineThe metabolism of Nateglinide can be decreased when combined with Desipramine.Approved
DesogestrelThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Nateglinide.Approved
DexamethasoneThe serum concentration of Nateglinide can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Diazoxide.Approved
DienogestThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Dienogest.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Nateglinide.Approved
DihydroergotamineThe metabolism of Nateglinide can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Nateglinide.Illicit
DiltiazemThe metabolism of Nateglinide can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Nateglinide can be decreased when combined with Diphenhydramine.Approved
DisopyramideDisopyramide may increase the hypoglycemic activities of Nateglinide.Approved
DoxycyclineThe metabolism of Nateglinide can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Nateglinide can be decreased when combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Drospirenone.Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Nateglinide.Approved
DuloxetineThe metabolism of Nateglinide can be decreased when combined with Duloxetine.Approved
EfavirenzThe serum concentration of Nateglinide can be decreased when it is combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Nateglinide can be decreased when combined with Eliglustat.Approved
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Nateglinide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Nateglinide.Approved
EnzalutamideThe serum concentration of Nateglinide can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Epinephrine.Approved, Vet Approved
ErythromycinThe metabolism of Nateglinide can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Nateglinide can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethynodiol diacetateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Nateglinide.Approved
EtravirineThe serum concentration of Nateglinide can be decreased when it is combined with Etravirine.Approved
EverolimusThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Everolimus.Approved
ExenatideExenatide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
FleroxacinFleroxacin may increase the hypoglycemic activities of Nateglinide.Approved
FloxuridineThe metabolism of Nateglinide can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Nateglinide can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Nateglinide.Withdrawn
FluorouracilThe metabolism of Nateglinide can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Nateglinide can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Nateglinide.Approved, Illicit
FluvastatinThe metabolism of Nateglinide can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Nateglinide can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Nateglinide can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Nateglinide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Nateglinide can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Nateglinide.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Nateglinide can be increased when it is combined with Fusidic Acid.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Nateglinide.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
GemfibrozilThe metabolism of Nateglinide can be decreased when combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
GlibornurideGlibornuride may increase the hypoglycemic activities of Nateglinide.Withdrawn
GliclazideNateglinide may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideGlimepiride may increase the hypoglycemic activities of Nateglinide.Approved
GlipizideNateglinide may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneGliquidone may increase the hypoglycemic activities of Nateglinide.Approved
GlyburideNateglinide may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Nateglinide.Withdrawn
GusperimusGusperimus may increase the hypoglycemic activities of Nateglinide.Investigational
HaloperidolThe metabolism of Nateglinide can be decreased when combined with Haloperidol.Approved
HistrelinThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Nateglinide.Approved
HydrochlorothiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IdelalisibThe serum concentration of Nateglinide can be increased when it is combined with Idelalisib.Approved
IloperidoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Iloperidone.Approved
ImatinibThe metabolism of Nateglinide can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Nateglinide can be decreased when combined with Imipramine.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Nateglinide.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Indapamide.Approved
IndinavirThe metabolism of Nateglinide can be decreased when combined with Indinavir.Approved
Insulin AspartNateglinide may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirNateglinide may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Nateglinide.Approved
Insulin GlulisineNateglinide may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Nateglinide.Approved
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Nateglinide.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Nateglinide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Nateglinide.Withdrawn
IrbesartanThe metabolism of Nateglinide can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Nateglinide can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Nateglinide.Approved
IsoniazidThe metabolism of Nateglinide can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Nateglinide can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Nateglinide can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Nateglinide can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Nateglinide can be decreased when combined with Ketoconazole.Approved, Investigational
LanreotideNateglinide may increase the hypoglycemic activities of Lanreotide.Approved
LeflunomideThe metabolism of Nateglinide can be decreased when combined with Leflunomide.Approved, Investigational
LeuprolideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Nateglinide.Approved
LevonorgestrelThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinagliptinLinagliptin may increase the hypoglycemic activities of Nateglinide.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Nateglinide.Approved, Nutraceutical
LiraglutideLiraglutide may increase the hypoglycemic activities of Nateglinide.Approved
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Nateglinide.Approved
LopinavirThe metabolism of Nateglinide can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Nateglinide can be decreased when combined with Lorcaserin.Approved
LosartanThe metabolism of Nateglinide can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Nateglinide can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Nateglinide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Nateglinide can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Nateglinide can be decreased when combined with Lumefantrine.Approved
LurasidoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Nateglinide.Withdrawn
MecaserminNateglinide may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Nateglinide.Approved
MestranolThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Mestranol.Approved
MetforminMetformin may increase the hypoglycemic activities of Nateglinide.Approved
MethadoneThe metabolism of Nateglinide can be decreased when combined with Methadone.Approved
MethotrimeprazineThe metabolism of Nateglinide can be decreased when combined with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Nateglinide.Investigational
MethylprednisoloneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Nateglinide.Approved
MetolazoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Metolazone.Approved
MetoprololThe metabolism of Nateglinide can be decreased when combined with Metoprolol.Approved, Investigational
MifepristoneThe serum concentration of Nateglinide can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolMiglitol may increase the hypoglycemic activities of Nateglinide.Approved
MiglustatMiglustat may increase the hypoglycemic activities of Nateglinide.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Nateglinide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Nateglinide.Approved
MirabegronThe metabolism of Nateglinide can be decreased when combined with Mirabegron.Approved
MitiglinideMitiglinide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
MitotaneThe serum concentration of Nateglinide can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Nateglinide.Approved
ModafinilThe serum concentration of Nateglinide can be decreased when it is combined with Modafinil.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NafcillinThe serum concentration of Nateglinide can be decreased when it is combined with Nafcillin.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Nateglinide.Approved
NCX 4016NCX 4016 may increase the hypoglycemic activities of Nateglinide.Investigational
NefazodoneThe metabolism of Nateglinide can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Nateglinide can be decreased when combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Nateglinide.Investigational
NetupitantThe serum concentration of Nateglinide can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Nateglinide can be increased when combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Nateglinide.Withdrawn
NicardipineThe metabolism of Nateglinide can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Nateglinide can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Nateglinide.Investigational
NorethisteroneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Nateglinide.Approved
NorgestimateThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Nateglinide.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Nateglinide.Approved
OlanzapineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Nateglinide can be decreased when combined with Olaparib.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Nateglinide.Approved
OmeprazoleThe metabolism of Nateglinide can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Nateglinide can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Nateglinide.Approved, Illicit
PalbociclibThe serum concentration of Nateglinide can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Paliperidone.Approved
PanobinostatThe serum concentration of Nateglinide can be increased when it is combined with Panobinostat.Approved, Investigational
PargylinePargyline may increase the hypoglycemic activities of Nateglinide.Approved
ParoxetineThe metabolism of Nateglinide can be decreased when combined with Paroxetine.Approved, Investigational
PasireotideNateglinide may increase the hypoglycemic activities of Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Nateglinide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Nateglinide.Approved
Peginterferon alfa-2bThe serum concentration of Nateglinide can be decreased when it is combined with Peginterferon alfa-2b.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Nateglinide.Approved
PentamidineNateglinide may increase the hypoglycemic activities of Pentamidine.Approved
PentobarbitalThe metabolism of Nateglinide can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Nateglinide.Approved
PhenforminPhenformin may increase the hypoglycemic activities of Nateglinide.Approved, Withdrawn
PheniprazinePheniprazine may increase the hypoglycemic activities of Nateglinide.Withdrawn
PhenobarbitalThe metabolism of Nateglinide can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Nateglinide.Withdrawn
PhenytoinThe metabolism of Nateglinide can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazonePioglitazone may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
PiperazineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Nateglinide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Nateglinide.Withdrawn
PolythiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Polythiazide.Approved
PosaconazoleThe metabolism of Nateglinide can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintidePramlintide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
PrednisoloneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Nateglinide can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Nateglinide can be decreased when combined with Promazine.Approved, Vet Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Nateglinide.Investigational
PyrimethamineThe metabolism of Nateglinide can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuetiapineThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Quinethazone.Approved
QuinidineThe metabolism of Nateglinide can be decreased when combined with Quinidine.Approved
QuinineQuinine may increase the hypoglycemic activities of Nateglinide.Approved
RanolazineThe metabolism of Nateglinide can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Nateglinide.Approved
RepaglinideNateglinide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RifabutinThe metabolism of Nateglinide can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Nateglinide can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Nateglinide can be increased when combined with Rifapentine.Approved
RisperidoneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe metabolism of Nateglinide can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Nateglinide can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Nateglinide can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Nateglinide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Nateglinide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Nateglinide.Approved, Vet Approved
SaquinavirThe metabolism of Nateglinide can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Nateglinide.Approved
SecobarbitalThe metabolism of Nateglinide can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Nateglinide.Approved, Investigational, Vet Approved
SertralineThe metabolism of Nateglinide can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Nateglinide can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Nateglinide can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Nateglinide can be increased when it is combined with Simeprevir.Approved
SirolimusThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Sirolimus.Approved, Investigational
SitagliptinSitagliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
SorafenibThe metabolism of Nateglinide can be decreased when combined with Sorafenib.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Nateglinide.Approved
St. John's WortThe serum concentration of Nateglinide can be decreased when it is combined with St. John&#39;s Wort.Nutraceutical
StanozololStanozolol may increase the hypoglycemic activities of Nateglinide.Approved, Vet Approved
StiripentolThe serum concentration of Nateglinide can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Nateglinide can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleNateglinide may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Nateglinide can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideSulodexide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
SunitinibNateglinide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Tacrolimus.Approved, Investigational
TelaprevirThe metabolism of Nateglinide can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Nateglinide can be decreased when combined with Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Nateglinide.Withdrawn
TemsirolimusThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Temsirolimus.Approved
TerbinafineThe metabolism of Nateglinide can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
ThiazolidinedioneThiazolidinedione may increase the hypoglycemic activities of Nateglinide.Investigational
ThioridazineThe metabolism of Nateglinide can be decreased when combined with Thioridazine.Approved
TicagrelorThe metabolism of Nateglinide can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Nateglinide can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Nateglinide can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Nateglinide can be decreased when it is combined with Tocilizumab.Approved
TolazamideNateglinide may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideThe metabolism of Nateglinide can be decreased when combined with Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Nateglinide.Approved
TorasemideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Nateglinide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Nateglinide.Approved
TriamcinoloneThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimethoprimThe metabolism of Nateglinide can be decreased when combined with Trimethoprim.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneTroglitazone may increase the hypoglycemic activities of Nateglinide.Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Withdrawn
Valproic AcidThe metabolism of Nateglinide can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Nateglinide can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe metabolism of Nateglinide can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Nateglinide can be decreased when combined with Verapamil.Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
VogliboseVoglibose may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
VoriconazoleThe metabolism of Nateglinide can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Vorinostat.Approved, Investigational
ZafirlukastThe metabolism of Nateglinide can be decreased when combined with Zafirlukast.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Nateglinide.Withdrawn
ZiprasidoneThe metabolism of Nateglinide can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take upto 30 minutes before meals.
References
Synthesis Reference

Michito Sumikawa, “Methods for producing nateglinide B-type crystals.” U.S. Patent US20030229249, issued December 11, 2003.

US20030229249
General ReferencesNot Available
External Links
ATC CodesA10BX03
AHFS Codes
  • 68:20.16
PDB EntriesNot Available
FDA labelDownload (56.5 KB)
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier+0.7539
Caco-2 permeable-0.7148
P-glycoprotein substrateSubstrate0.6187
P-glycoprotein inhibitor INon-inhibitor0.8842
P-glycoprotein inhibitor IINon-inhibitor0.8604
Renal organic cation transporterNon-inhibitor0.8882
CYP450 2C9 substrateNon-substrate0.7192
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5103
CYP450 1A2 substrateNon-inhibitor0.9167
CYP450 2C9 inhibitorNon-inhibitor0.8412
CYP450 2D6 inhibitorNon-inhibitor0.9088
CYP450 2C19 inhibitorNon-inhibitor0.8764
CYP450 3A4 inhibitorNon-inhibitor0.8874
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8734
Ames testNon AMES toxic0.922
CarcinogenicityNon-carcinogens0.9354
BiodegradationNot ready biodegradable0.7779
Rat acute toxicity2.0362 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9881
hERG inhibition (predictor II)Non-inhibitor0.8425
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Dr reddys laboratories ltd
  • Par pharmaceutical inc
  • Teva pharmaceuticals usa
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Tablet, coatedOral120 mg/1
Tablet, coatedOral60 mg/1
Tablet, film coatedOral120 mg/1
Tablet, film coatedOral60 mg/1
TabletOral120 mg/1
TabletOral60 mg/1
Tablet, film coatedOral120 mg
Tablet, film coatedOral180 mg
Tablet, film coatedOral60 mg
TabletOral120 mg
TabletOral180 mg
TabletOral60 mg
Prices
Unit descriptionCostUnit
Starlix 120 mg tablet2.12USD tablet
Starlix 60 mg tablet2.01USD tablet
Nateglinide 120 mg tablet1.73USD tablet
Nateglinide 60 mg tablet1.66USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2114678 No1999-04-272014-02-01Canada
CA2271865 No2003-10-142017-11-14Canada
US6559188 No2000-09-152020-09-15Us
US6641841 No1997-11-142017-11-14Us
US6844008 No1997-11-142017-11-14Us
US6878749 No2000-09-152020-09-15Us
USRE34878 No1992-09-082009-09-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityPractically insolubleNot Available
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00848 mg/mLALOGPS
logP3.59ALOGPS
logP4.03ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)4ChemAxon
pKa (Strongest Basic)-0.38ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area66.4 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity89.46 m3·mol-1ChemAxon
Polarizability35.57 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-acyl-aliphatic-alpha amino acids. These are alpha amino acids carrying a N-acylated aliphatic chain.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentN-acyl-aliphatic-alpha amino acids
Alternative Parents
Substituents
  • N-acyl-aliphatic-alpha amino acid
  • 3-phenylpropanoic-acid
  • Menthane monoterpenoid
  • Monoterpenoid
  • Monocyclic monoterpenoid
  • Aromatic monoterpenoid
  • Amphetamine or derivatives
  • Amino fatty acid
  • Fatty acyl
  • Benzenoid
  • Monocyclic benzene moiety
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

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
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. Chachin M, Yamada M, Fujita A, Matsuoka T, Matsushita K, Kurachi Y: Nateglinide, a D-phenylalanine derivative lacking either a sulfonylurea or benzamido moiety, specifically inhibits pancreatic beta-cell-type K(ATP) channels. J Pharmacol Exp Ther. 2003 Mar;304(3):1025-32. [PubMed:12604678 ]
  5. Norman P, Rabasseda X: Nateglinide: A structurally novel, short-acting, hypoglycemic agent. Drugs Today (Barc). 2001 Jun;37(6):411-426. [PubMed:12764427 ]
  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) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation...
Gene Name:
PPARG
Uniprot ID:
P37231
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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 ]

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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Uchida Y, Kamiie J, Ohtsuki S, Terasaki T: Multichannel liquid chromatography-tandem mass spectrometry cocktail method for comprehensive substrate characterization of multidrug resistance-associated protein 4 transporter. Pharm Res. 2007 Dec;24(12):2281-96. Epub 2007 Oct 16. [PubMed:17939016 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Symporter activity
Specific Function:
Proton-coupled monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate. Depending on the tissue and on cicumstances, mediates the import or export of lactic acid and ketone bod...
Gene Name:
SLC16A1
Uniprot ID:
P53985
Molecular Weight:
53943.685 Da
References
  1. Okamura A, Emoto A, Koyabu N, Ohtani H, Sawada Y: Transport and uptake of nateglinide in Caco-2 cells and its inhibitory effect on human monocarboxylate transporter MCT1. Br J Pharmacol. 2002 Oct;137(3):391-9. [PubMed:12237260 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name:
SLC15A1
Uniprot ID:
P46059
Molecular Weight:
78805.265 Da
References
  1. Terada T, Sawada K, Saito H, Hashimoto Y, Inui K: Inhibitory effect of novel oral hypoglycemic agent nateglinide (AY4166) on peptide transporters PEPT1 and PEPT2. Eur J Pharmacol. 2000 Mar 24;392(1-2):11-7. [PubMed:10748266 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Peptide:proton symporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
Gene Name:
SLC15A2
Uniprot ID:
Q16348
Molecular Weight:
81782.77 Da
References
  1. Terada T, Sawada K, Saito H, Hashimoto Y, Inui K: Inhibitory effect of novel oral hypoglycemic agent nateglinide (AY4166) on peptide transporters PEPT1 and PEPT2. Eur J Pharmacol. 2000 Mar 24;392(1-2):11-7. [PubMed:10748266 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Uwai Y, Saito H, Hashimoto Y, Inui K: Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1. Eur J Pharmacol. 2000 Jun 16;398(2):193-7. [PubMed:10854830 ]
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 02:38