Drug/Small Molecule:
repaglinide

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with repaglinide that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105235

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all repaglinide variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP No VIP available No VIP available CYP2C8 *2 N/A N/A N/A
VIP No VIP available VA CYP2C8 *3 N/A N/A N/A
VIP No VIP available No VIP available CYP2C8 *4 N/A N/A N/A
No VIP available CA VA SLCO1B1 *1A N/A N/A N/A
No VIP available CA VA SLCO1B1 *1B N/A N/A N/A
No VIP available CA VA SLCO1B1 *5 N/A N/A N/A
No VIP available CA VA SLCO1B1 *15 N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs10229583 127246903G>A, 65279746G>A
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs10494366 106-38510G>T, 13574327G>T, 162085685G>T, 51105G>T
G > T
Intronic
rs10509681 1196A>G, 35506A>G, 47603213T>C, 890A>G, 96798749T>C, 986A>G, A1196G, CYP2C8*3, CYP2C8: K399R, Lys297Arg, Lys329Arg, Lys399Arg
T > C
Missense
Lys329Arg
VIP No Clinical Annotations available No Variant Annotations available
rs1058930 16136C>G, 47622583G>C, 486C>G, 582C>G, 792C>G, 96818119G>C, C792G, CYP2C8: I264M, Ile162Met, Ile194Met, Ile264Met
G > C
Missense
Ile194Met
No VIP available CA VA
rs114202595
G > A
Missense
Arg121Trp
rs11572080 110G>A, 206G>A, 416G>A, 47631494C>T, 7225G>A, 96827030C>T, Arg139Lys, Arg37Lys, Arg69Lys, CYP2C8*3, CYP2C8: R139K, G416A, R139K, rs11572080 G>A
C > T
Missense
Arg69Lys
VIP No Clinical Annotations available No Variant Annotations available
rs11572103 16149A>T, 47622570T>A, 499A>T, 595A>T, 805A>T, 96818106T>A, A805T, CYP2C8*2, CYP2C8: I269F, Ile167Phe, Ile199Phe, Ile269Phe
T > A
Missense
Ile199Phe
No VIP available CA VA
rs13266634 118184783C>T, 227272C>T, 31458332C>T, 826C>T, 973C>T, SLC30A8:Arg325Trp, SLC30A8:R325W
C > T
Missense
Arg276Trp
No VIP available No Clinical Annotations available VA
rs1470579 185529080A>C, 18748T>G, 239+11861T>G, 92024226A>C
A > C
Intronic
No VIP available No Clinical Annotations available VA
rs16889462 118184784G>A, 118184784G>C, 118184784G>T, 227273G>A, 227273G>C, 227273G>T, 31458333G>A, 31458333G>C, 31458333G>T, 827G>A, 827G>C, 827G>T, 974G>A, 974G>C, 974G>T, Arg276Gln, Arg276Leu, Arg276Pro, Arg325Gln, Arg325Leu, Arg325Pro
G > A
G > T
G > C
Missense
Arg276Gln
Arg276Pro
Arg276Leu
No VIP available CA VA
rs1801262 133G>G, 182543455T>C, 32752873T>C, 6927G>G, Ala45=
T > C
Not Available
No VIP available CA VA
rs2237892 1414-29246C>T, 1688-29246C>T, 1795-29246C>T, 2779751C>T, 2839751C>T, 378531C>T
C > T
Intronic
No VIP available CA VA
rs2237895 1414-11803A>C, 1688-11803A>C, 1795-11803A>C, 2797194A>C, 2857194A>C, 395974A>C
A > C
Intronic
No VIP available CA VA
rs2276706 -23+160G>A, -298G>A, 119501307G>A, 25996453G>A, 6977G>A
G > A
5' Flanking
rs2306283 14089862A>G, 21329738A>G, 388A>G, 50611A>G, Asn130Asp, SLCO1B1*1B
A > G
Missense
Asn130Asp
No VIP available CA VA
rs290487 114909731C>T, 204723C>T, 65714195C>T, 705-1026C>T, 795-1026C>T, 807-1011C>T, 807-1026C>T, 876-1026C>T, 948-1026C>T, TCF7L2: intronic C>T SNP
C > T
Intronic
No VIP available CA VA
rs3814058 *1232T>C, 119537291T>C, 26032437T>C, 42961T>C
T > C
3' UTR
VIP No Clinical Annotations available No Variant Annotations available
rs4149015 -910G>A, 14043446G>A, 21283322G>A, 4195G>A, SLCO1B1:11187G>A, SLCO1B1:G-11187A
G > A
5' Flanking
rs4149056 14091673T>C, 21331549T>C, 521T>C, 52422T>C, SLCO1B1*5, Val174Ala
T > C
Missense
Val174Ala
No VIP available No Clinical Annotations available VA
rs4402960 185511687G>T, 239+29254C>A, 36141C>A, 92006833G>T
G > T
Intronic
No VIP available CA VA
rs5219 -16-179A>G, 17349572T>C, 17409572T>C, 5635A>G, 67A>G, E23K, KCNJ11: Lys23Glu, KCNJ11:67A>G, KCNJ11:E23K, Lys23Glu
T > C
Intronic
Lys23Glu
No VIP available No Clinical Annotations available VA
rs6467136 127164958A>G, 65197801A>G
A > G
Not Available
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • AG-EE 388 ZW
  • AG-EE 623 ZW
  • Repaglinida [INN-Spanish]
  • Repaglinidum [INN-Latin]
  • repaglinide
Trade Names
  • GlucoNorm
  • Prandin
Brand Mixture Names

PharmGKB Accession Id:
PA451234

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 beta 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.

Source: Drug Bank

Indication

For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Repaglinide activity is dependent on the presence functioning beta 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 beta cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.

Source: Drug Bank

Pharmacology

Insulin secretion by pancreatic beta 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.

Source: Drug Bank

Food Interaction

Take up to 30 minutes before meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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.

Source: Drug Bank

Protein Binding

>98% (e.g. to to albumin and alpha1-acid glycoprotein)

Source: Drug Bank

Absorption

Rapidly and completely absorbed following oral administration. Peak plasma concentrations are observed within 1 hour (range 0.5-1.4 hours). Absolutely bioavailability is approximately 56%. Maximal biological effect is observed within 3-3.5 hours and plasma insulin levels remain elevated for 4-6 hours

Source: Drug Bank

Half-Life

1 hour

Source: Drug Bank

Toxicity

LD 50 >1 g/kg (rat) (W. Grell)

Source: Drug Bank

Clearance

33-38 L/hour following IV administration

Source: Drug Bank

Route of Elimination

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

Source: Drug Bank

Volume of Distribution

31 L following IV administration in healthy individuals

Source: Drug Bank

Chemical Properties

Chemical Formula

C27H36N2O4

Source: Drug Bank

Isomeric SMILES

CCOc1cc(ccc1C(=O)O)CC(=O)N[C@@H](CC(C)C)c2ccccc2N3CCCCC3

Source: OpenEye

Canonical SMILES

CCOC1=C(C=CC(CC(=O)N[C@@H](CC(C)C)C2=CC=CC=C2N2CCCCC2)=C1)C(O)=O

Source: Drug Bank

Average Molecular Weight

452.5857

Source: Drug Bank

Monoisotopic Molecular Weight

452.26750765

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Anti-diabetic Drug Potassium Channel Inhibitors Pathway, Pharmacodynamics
    Representation of anti-diabetic drugs repaglinide, nateglinide and sulfonylurea effects on insulin secretion in pancreatic cells.
  1. Anti-diabetic Drug Repaglinide Pathway, Pharmacokinetics
    Repaglinide metabolism and transport in a liver cell.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ABCC8 (source: Drug Bank)
KCNJ1 (source: Drug Bank)
KCNJ11 (source: Drug Bank)
PPARG (source: Drug Bank)

Drug Interactions

Drug Description
repaglinide Decreased in symptoms of hypoglycemia and increase in time required for the body to compensate for hypoglycemia (source: Drug Bank)
repaglinide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide Similar mode of action-questionable association (source: Drug Bank)
repaglinide Increases the effect of repaglinide (source: Drug Bank)
repaglinide Increases the effect of repaglinide (source: Drug Bank)
repaglinide Increases repaglinide's effect (source: Drug Bank)
repaglinide Increases repaglinide's effect (source: Drug Bank)
repaglinide This macrolide increases effect of repaglinide (source: Drug Bank)
repaglinide The macrolide, erythromycin, may increase effect of repaglinide. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, esmolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide Increases the effect and toxicity of repaglinide (source: Drug Bank)
repaglinide Increases the effect and toxicity of repaglinide (source: Drug Bank)
repaglinide Similar mode of action - questionable association (source: Drug Bank)
repaglinide Similar mode of action - questionable association (source: Drug Bank)
repaglinide Similar mode of action - questionable association (source: Drug Bank)
repaglinide Similar mode of action - questionable association (source: Drug Bank)
repaglinide The beta-blocker, labetalol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
acebutolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
acebutolol The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
atenolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
atenolol The beta-blocker, atenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
betaxolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
betaxolol The beta-blocker, betaxolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
bevantolol The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
bisoprolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
bisoprolol The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
carteolol The beta-blocker, carteolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
carvedilol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
carvedilol The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
chlorpropamide Similar mode of action - questionable association (source: Drug Bank)
clarithromycin Clarithromycin increases the effect of repaglinide (source: Drug Bank)
clarithromycin Clarithromycin increases the effect of repaglinide (source: Drug Bank)
cyclosporine Cyclosporine increases the effect of repaglinide (source: Drug Bank)
cyclosporine Cyclosporine increases the effect of repaglinide (source: Drug Bank)
erythromycin The macrolide increases the effect of repaglinide (source: Drug Bank)
erythromycin The macrolide, erythromycin, may increase the effect of repaglinide. (source: Drug Bank)
esmolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
gemfibrozil Gemfibrozil increases the effect and toxicity of repaglinide (source: Drug Bank)
gemfibrozil Gemfibrozil increases the effect and toxicity of repaglinide (source: Drug Bank)
glibenclamide Similar mode of action - questionable association (source: Drug Bank)
gliclazide Similar mode of action - questionable association (source: Drug Bank)
glimepiride Similar mode of action - questionable association (source: Drug Bank)
glipizide Similar mode of action - questionable association (source: Drug Bank)
glucosamine Possible hyperglycemia (source: Drug Bank)
josamycin The macrolide, josamycin, may increase the effect of repaglinide. (source: Drug Bank)
labetalol The beta-blocker, labetolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
metoprolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
metoprolol The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
nadolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
nadolol The beta-blocker, nadolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
oxprenolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
oxprenolol The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
penbutolol The beta-blocker, penbutolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
pindolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
pindolol The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
practolol The beta-blocker, practolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
propranolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
rifampin Rifampin decreases the effect of repaglinide (source: Drug Bank)
rifampin Rifampin decreases the effect of repaglinide (source: Drug Bank)
somatropin recombinant Somatropin may antagonize the hypoglycemic effect of repaglinide. Monitor for changes in fasting and postprandial blood sugars. (source: Drug Bank)
sotalol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
sotalol The beta-blocker, sotalol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
timolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
tolbutamide Similar mode of action - questionable association (source: Drug Bank)
repaglinide Rifampin decreases the effect of repaglinide (source: Drug Bank)
repaglinide Rifampin decreases the effect of repaglinide (source: Drug Bank)
repaglinide Telithromycin may reduce clearance of Repaglinide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Repaglinide if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
repaglinide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
repaglinide The beta-blocker, timolol, may decrease symptoms of hypoglycemia. (source: Drug Bank)
repaglinide Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of repaglinide by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of repaglinide if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to repaglinide: 28

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of PAX4 genetic variants with oral antidiabetic drugs efficacy in Chinese type 2 diabetes patients. The pharmacogenomics journal. 2014. Chen M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
PXR polymorphisms and their impact on pharmacokinetics/pharmacodynamics of repaglinide in healthy Chinese volunteers. European journal of clinical pharmacology. 2013. Du Qing-qing, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 8. Pharmacogenetics and genomics. 2013. Aquilante Christina L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide, and ibuprofen enantiomers in vitro. Biopharmaceutics & drug disposition. 2013. Yu Lushan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
NeuroD1 A45T and PAX4 R121W polymorphisms are associated with plasma glucose level of repaglinide monotherapy in Chinese patients with type 2 diabetes. British journal of clinical pharmacology. 2012. Gong Zhi-Cheng, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
KCNQ1 gene polymorphisms are associated with the therapeutic efficacy of repaglinide in Chinese type 2 diabetic patients. Clinical and experimental pharmacology & physiology. 2012. Dai Xing-Ping, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. European journal of clinical pharmacology. 2011. He Jiake, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide. Drug metabolism and disposition: the biological fate of chemicals. 2011. Tomalik-Scharte Dorota, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of KCNQ1 Polymorphisms on the Therapeutic Efficacy of Oral Antidiabetic Drugs in Chinese Patients With Type 2 Diabetes. Clinical pharmacology and therapeutics. 2011. Yu W, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association analysis of SLC30A8 rs13266634 and rs16889462 polymorphisms with type 2 diabetes mellitus and repaglinide response in Chinese patients. European journal of clinical pharmacology. 2010. Huang Qiong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
IGF2BP2 variations influence repaglinide response and risk of type 2 diabetes in Chinese population. Acta pharmacologica Sinica. 2010. Huang Qiong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A variation in NOS1AP gene is associated with repaglinide efficacy on insulin resistance in type 2 diabetes of Chinese. Acta pharmacologica Sinica. 2010. Qin Wen, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomics of membrane transporters: past, present and future. Pharmacogenomics. 2010. Yee Sook Wah, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
KCNJ11 Lys23Glu and TCF7L2 rs290487(C/T) polymorphisms affect therapeutic efficacy of repaglinide in Chinese patients with type 2 diabetes. Clinical pharmacology and therapeutics. 2010. Yu M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB very important pharmacogene: SLCO1B1. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cytochrome P450 2C8 pharmacogenetics: a review of clinical studies. Pharmacogenomics. 2009. Daily Elizabeth B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Impact of OATP transporters on pharmacokinetics. British journal of pharmacology. 2009. Kalliokoski A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effects of the SLCO1B1*1B haplotype on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. Pharmacogenetics and genomics. 2008. Kalliokoski Annikka, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The effect of gemfibrozil on repaglinide pharmacokinetics persists for at least 12 h after the dose: evidence for mechanism-based inhibition of CYP2C8 in vivo. Clinical pharmacology and therapeutics. 2008. Tornio A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Characterization of novel CYP2C8 haplotypes and their contribution to paclitaxel and repaglinide metabolism. The pharmacogenomics journal. 2008. Rodríguez-Antona C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Interaction of oral antidiabetic drugs with hepatic uptake transporters: focus on organic anion transporting polypeptides and organic cation transporter 1. Diabetes. 2008. Bachmakov Iouri, et al. PubMed
Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. Journal of clinical pharmacology. 2008. Kalliokoski Annikka, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of glucose-lowering drug treatment: a systematic review. Molecular diagnosis & therapy. 2007. Bozkurt Ozlem, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Telithromycin, but not montelukast, increases the plasma concentrations and effects of the cytochrome P450 3A4 and 2C8 substrate repaglinide. Clinical pharmacology and therapeutics. 2006. Kajosaari Lauri I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The impact of CYP2C8 polymorphism and grapefruit juice on the pharmacokinetics of repaglinide. British journal of clinical pharmacology. 2006. Bidstrup Tanja Busk, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Clinical pharmacology and therapeutics. 2005. Niemi Mikko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cytochrome P450 2C8: substrates, inhibitors, pharmacogenetics, and clinical relevance. Clinical pharmacology and therapeutics. 2005. Totah Rheem A, et al. PubMed
Polymorphism in CYP2C8 is associated with reduced plasma concentrations of repaglinide. Clinical pharmacology and therapeutics. 2003. Niemi Mikko, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00912
KEGG Compound:
C07670
KEGG Drug:
D00594
PubChem Compound:
65981
PubChem Substance:
208038
46508150
Drugs Product Database (DPD):
2239925
BindingDB:
50153520
ChemSpider:
59377
Therapeutic Targets Database:
DAP000133

Clinical Trials

These are trials that mention repaglinide and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.