Identification
- Summary
Repaglinide is a antihyperglycemic used to improve glycemic control in diabetes.
- Brand Names
- Enyglid, Gluconorm, Prandin
- Generic Name
- Repaglinide
- DrugBank Accession Number
- DB00912
- Background
Repaglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Repaglinide induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those naïve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Repaglinide is extensively metabolized in the liver and excreted in bile. Repaglinide metabolites do not possess appreciable hypoglycemic activity. Approximately 90% of a single orally administered dose is eliminated in feces and 8% in urine.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Repaglinide (DB00912)
- Weight
- Average: 452.5857
Monoisotopic: 452.26750765 - Chemical Formula
- C27H36N2O4
- Synonyms
- Repaglinida
- Repaglinide
- Repaglinidum
- External IDs
- AG-EE 388 ZW
- AG-EE 623 ZW
- AG-EE-623ZW
Pharmacology
- Indication
As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Metformin (DB00331) •••••••••••• Management of Type 2 diabetes mellitus •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Insulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. Extracellular glucose enters the cell via GLUT2 (SLC2A2) transporters. Once inside the cell, glucose is metabolized to produce ATP. High concentrations of ATP inhibit ATP-sensitive potassium channels causing membrane depolarization. When extracellular glucose concentrations are low, ATP-sensitive potassium channels open causing membrane repolarization. High glucose concentrations cause ATP-sensitive potassium channels to close resulting in membrane depolarization and opening of L-type calcium channels. The influx of calcium ions stimulates calcium-dependent exocytosis of insulin granules. Repaglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.
- Mechanism of action
Repaglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, repaglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, repaglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of repaglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Repaglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.
Target Actions Organism AATP-binding cassette sub-family C member 8 inhibitorHumans UPeroxisome proliferator-activated receptor gamma agonistHumans AHistamine H1 receptor antagonistHumans - Absorption
Rapidly and completely absorbed following oral administration. Peak plasma concentrations are observed within 1 hour (range 0.5-1.4 hours). The absolute bioavailability is approximately 56%. Maximal biological effect is observed within 3-3.5 hours and plasma insulin levels remain elevated for 4-6 hours. When a single 2 mg dose of repaglinide is given to healthy subjects, the area under the curve (AUC) is 18.0 - 18.7 (ng/mL/h)^3.
- Volume of distribution
31 L following IV administration in healthy individuals
- Protein binding
>98% (e.g. to to albumin and α1-acid glycoprotein)
- Metabolism
Repaglinide is rapidly metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2). Further oxidation produces the aromatic amine derivative (M1). Glucuronidation of the carboxylic acid group of repaglinide yields an acyl glucuronide (M7). Several other unidentified metabolites have been detected. Repaglinide metabolites to not possess appreciable hypoglycemic activity.
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- Route of elimination
90% eliminated in feces (<2% as unchanged drug), 8% in urine (0.1% as unchanged drug)
- Half-life
1 hour
- Clearance
33-38 L/hour following IV administration
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50 >1 g/kg (rat) (W. Grell)
- Pathways
Pathway Category Repaglinide Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Repaglinide can be increased when it is combined with Abametapir. Abatacept The metabolism of Repaglinide can be increased when combined with Abatacept. Abiraterone The metabolism of Repaglinide can be decreased when combined with Abiraterone. Acarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Repaglinide. Acebutolol The therapeutic efficacy of Repaglinide can be increased when used in combination with Acebutolol. - Food Interactions
- Take before a meal. Repaglinide should be taken before each meal of the day.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- GlucoNorm (Novo Nordisk) / Surepost
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Repaglinide Tablet 1 mg Oral TEVA Canada Limited 2010-10-18 Not applicable Canada 
Act Repaglinide Tablet 0.5 mg Oral TEVA Canada Limited 2010-10-18 Not applicable Canada Act Repaglinide Tablet 2 mg Oral TEVA Canada Limited 2010-10-18 Not applicable Canada Enyglid Tablet 0.5 mg Oral Krka, D.D., Novo Mesto 2016-09-08 Not applicable EU 
Enyglid Tablet 0.5 mg Oral Krka, D.D., Novo Mesto 2016-09-08 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-repaglinide Tablet 1.0 mg Oral Apotex Corporation 2012-10-16 Not applicable Canada Apo-repaglinide Tablet 0.5 mg Oral Apotex Corporation 2012-10-16 Not applicable Canada Apo-repaglinide Tablet 2.0 mg Oral Apotex Corporation 2012-10-16 Not applicable Canada Auro-repaglinide Tablet 1 mg Oral Auro Pharma Inc 2014-04-30 Not applicable Canada Auro-repaglinide Tablet 0.5 mg Oral Auro Pharma Inc 2014-04-30 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image PAREGLIN 1 MG/500 MG FILM KAPLI TABLET, 90 ADET Repaglinide (1 mg) + Metformin hydrochloride (500 mg) Tablet, film coated Oral İLKO İLAÇ SAN.VE TİC. A.Ş. 2015-09-14 Not applicable Turkey 
PAREGLIN 2 MG/500 MG FILM KAPLI TABLET, 90 ADET Repaglinide (2 mg) + Metformin hydrochloride (500 mg) Tablet, film coated Oral İLKO İLAÇ SAN.VE TİC. A.Ş. 2015-09-14 Not applicable Turkey Prandimet Repaglinide (1 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Novo Nordisk 2009-01-16 2017-05-31 US 
Prandimet Repaglinide (2 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Novo Nordisk 2009-01-15 2017-05-31 US Repaglinide and Metformin Hydrochloride Repaglinide (2 mg/1) + Metformin hydrochloride (500 mg/1) Tablet Oral Lupin Pharmaceuticals, Inc. 2015-12-10 2017-10-31 US
Categories
- ATC Codes
- A10BD14 — Metformin and repaglinide
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Acids, Acyclic
- Alimentary Tract and Metabolism
- Blood Glucose Lowering Agents
- BSEP/ABCB11 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs Used in Diabetes
- Glinide
- Hypoglycemia-Associated Agents
- Insulin Secretagogues
- Meglitinides
- OATP1B1/SLCO1B1 Substrates
- Oral Hypoglycemics
- Potassium Channel Blockers
- Stereoisomerism
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Piperidines
- Sub Class
- Phenylpiperidines
- Direct Parent
- Phenylpiperidines
- Alternative Parents
- Phenylacetamides / Benzoic acids / Aniline and substituted anilines / Benzoyl derivatives / Dialkylarylamines / Phenol ethers / Phenoxy compounds / Alkyl aryl ethers / Amino acids / Secondary carboxylic acid amides show 7 more
- Substituents
- Alkyl aryl ether / Amine / Amino acid / Amino acid or derivatives / Aniline or substituted anilines / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Benzoic acid / Benzoic acid or derivatives show 23 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- piperidines (CHEBI:8805)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 668Z8C33LU
- CAS number
- 135062-02-1
- InChI Key
- FAEKWTJYAYMJKF-QHCPKHFHSA-N
- InChI
- InChI=1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
- IUPAC Name
- 2-ethoxy-4-({[(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl]carbamoyl}methyl)benzoic acid
- SMILES
- CCOC1=C(C=CC(CC(=O)N[C@@H](CC(C)C)C2=CC=CC=C2N2CCCCC2)=C1)C(O)=O
References
- Synthesis Reference
Manne Reddy, "Polymorphic forms of (S)-Repaglinide and the processes for preparation thereof." U.S. Patent US20040102477, issued May 27, 2004.
US20040102477- General References
- External Links
- Human Metabolome Database
- HMDB0015048
- KEGG Drug
- D00594
- KEGG Compound
- C07670
- PubChem Compound
- 65981
- PubChem Substance
- 46508150
- ChemSpider
- 59377
- BindingDB
- 50153520
- 73044
- ChEBI
- 8805
- ChEMBL
- CHEMBL1272
- ZINC
- ZINC000003798537
- Therapeutic Targets Database
- DAP000133
- PharmGKB
- PA451234
- PDBe Ligand
- BJX
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Repaglinide
- PDB Entries
- 6jb1 / 6jb3 / 6pz9 / 7tys / 7tyt / 7u1q / 7u1s / 7y1j / 7y1k / 7y1l … show 2 more
- FDA label
- Download (175 KB)
- MSDS
- Download (57.3 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Diabetes Mellitus 1 4 Completed Treatment Diabetes / Type 2 Diabetes Mellitus 10 4 Completed Treatment Type 2 Diabetes Mellitus 6 4 Terminated Treatment Diabetes / Type 2 Diabetes Mellitus 1 4 Unknown Status Treatment Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Novo nordisk inc
- Novo Nordisk Inc.
- Packagers
- Boehringer Ingelheim Ltd.
- Cardinal Health
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Novo Nordisk Inc.
- Recipharm AB
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral 0.5 mg Tablet Oral 1 mg Tablet Oral 2 mg Tablet Oral 1.0 mg Tablet Oral 2.0 mg Capsule, coated Oral 0.5 mg Tablet Oral 1 mg/tablet Tablet Oral 2 mg/tablet Tablet, film coated Oral Tablet Oral Tablet Oral 0.5 mg/1 Tablet Oral 1 mg/1 Tablet Oral 2 mg/1 Tablet, effervescent Tablet Oral 4 mg Tablet Oral 0.50 mg Tablet, effervescent Oral - Prices
Unit description Cost Unit Prandin 1 mg tablet 2.48USD tablet Prandin 0.5 mg tablet 2.47USD tablet Prandin 2 mg tablet 2.33USD tablet Gluconorm 2 mg Tablet 0.34USD tablet Gluconorm 1 mg Tablet 0.32USD tablet Gluconorm 0.5 mg Tablet 0.31USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6677358 No 2004-01-13 2018-06-12 US CA2111851 No 2002-02-26 2011-06-21 Canada
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 130-131 °C Not Available logP 5.9 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00294 mg/mL ALOGPS logP 5.05 ALOGPS logP 3.95 Chemaxon logS -5.2 ALOGPS pKa (Strongest Acidic) 3.68 Chemaxon pKa (Strongest Basic) 4.82 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 78.87 Å2 Chemaxon Rotatable Bond Count 10 Chemaxon Refractivity 131.83 m3·mol-1 Chemaxon Polarizability 51.49 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9172 Blood Brain Barrier - 0.7101 Caco-2 permeable - 0.5891 P-glycoprotein substrate Substrate 0.8145 P-glycoprotein inhibitor I Inhibitor 0.6044 P-glycoprotein inhibitor II Inhibitor 0.6868 Renal organic cation transporter Non-inhibitor 0.849 CYP450 2C9 substrate Non-substrate 0.8288 CYP450 2D6 substrate Non-substrate 0.9117 CYP450 3A4 substrate Substrate 0.7019 CYP450 1A2 substrate Non-inhibitor 0.9206 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.9264 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8682 Ames test Non AMES toxic 0.8136 Carcinogenicity Non-carcinogens 0.8004 Biodegradation Not ready biodegradable 0.919 Rat acute toxicity 2.4497 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9605 hERG inhibition (predictor II) Non-inhibitor 0.5272
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 233.2199722 predictedDarkChem Lite v0.1.0 [M-H]- 234.0079722 predictedDarkChem Lite v0.1.0 [M-H]- 207.23181 predictedDeepCCS 1.0 (2019) [M+H]+ 232.1213722 predictedDarkChem Lite v0.1.0 [M+H]+ 232.2016722 predictedDarkChem Lite v0.1.0 [M+H]+ 209.62738 predictedDeepCCS 1.0 (2019) [M+Na]+ 232.6062722 predictedDarkChem Lite v0.1.0 [M+Na]+ 232.5770722 predictedDarkChem Lite v0.1.0 [M+Na]+ 215.53992 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Sulfonylurea receptor activity
- Specific Function
- Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
- Gene Name
- ABCC8
- Uniprot ID
- Q09428
- Uniprot Name
- ATP-binding cassette sub-family C member 8
- Molecular Weight
- 176990.36 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Wangler B, Schneider S, Thews O, Schirrmacher E, Comagic S, Feilen P, Schwanstecher C, Schwanstecher M, Shiue CY, Alavi A, Hohnemann S, Piel M, Rosch F, Schirrmacher R: Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbam oyl]-methyl)-benzoic acid ([18F]repaglinide): a promising radioligand for quantification of pancreatic beta-cell mass with positron emission tomography (PET). Nucl Med Biol. 2004 Jul;31(5):639-47. [Article]
- Wangler B, Beck C, Shiue CY, Schneider S, Schwanstecher C, Schwanstecher M, Feilen PJ, Alavi A, Rosch F, Schirrmacher R: Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-be nzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5205-9. [Article]
- Dornhorst A: Insulinotropic meglitinide analogues. Lancet. 2001 Nov 17;358(9294):1709-16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE...
- Gene Name
- PPARG
- Uniprot ID
- P37231
- Uniprot Name
- Peroxisome proliferator-activated receptor gamma
- Molecular Weight
- 57619.58 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Horak F, Unkauf M, Beckers C, Mittermaier EM: Efficacy and tolerability of intranasally applied dimetindene maleate solution versus placebo in the treatment of seasonal allergic rhinitis. Arzneimittelforschung. 2000 Dec;50(12):1099-105. doi: 10.1055/s-0031-1300341. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- 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. [Article]
- Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- 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 react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT: CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol. 2003 Sep;56(3):305-14. [Article]
- Kajosaari LI, Laitila J, Neuvonen PJ, Backman JT: Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin. Basic Clin Pharmacol Toxicol. 2005 Oct;97(4):249-56. doi: 10.1111/j.1742-7843.2005.pto_157.x. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- He J, Qiu Z, Li N, Yu Y, Lu Y, Han D, Li T, Zhao D, Sun W, Fang F, Zheng J, Fan H, Chen X: Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. Eur J Clin Pharmacol. 2011 Jul;67(7):701-7. doi: 10.1007/s00228-011-0994-7. Epub 2011 Feb 17. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55