Identification
- Summary
Nateglinide is a meglitinide used to treat non insulin dependent diabetes mellitus.
- Generic Name
- Nateglinide
- DrugBank Accession Number
- DB00731
- Background
Nateglinide 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.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Nateglinide (DB00731)
- Weight
- Average: 317.429
Monoisotopic: 317.199093733 - Chemical Formula
- C19H27NO3
- Synonyms
- Nateglinida
- Nateglinide
- Natéglinide
- Nateglinidum
- External IDs
- A-4166
- AY-4166
- AY4166
- DJN 608
- DJN-608
- SDZ DJN 608
- SDZ-DJN-608
Pharmacology
- Indication
For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form 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. Nateglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.
- Mechanism of action
Nateglinide 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.
Target Actions Organism AATP-binding cassette sub-family C member 8 inhibitorHumans UPeroxisome proliferator-activated receptor gamma agonistHumans - Absorption
Rapidly 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 binding
98% 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.
Hover over products below to view reaction partners
- Route of elimination
Urine (83%) and feces (10%)
- Half-life
1.5 hours
- Clearance
Not Available
- 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
An overdose may result in an exaggerated glucose-lowering effect with the development of hypoglycemic symptoms.
- Pathways
Pathway Category Nateglinide 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 softwareAbacavir Nateglinide may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Nateglinide can be increased when it is combined with Abametapir. Abatacept The metabolism of Nateglinide can be increased when combined with Abatacept. Abiraterone The metabolism of Nateglinide can be decreased when combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Nateglinide. - Food Interactions
- Take with food. Take up to 30 minutes before meals.
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
- Fastic / Starsis
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Starlix Tablet 120 mg/1 Oral Physicians Total Care, Inc. 2005-08-01 2011-06-30 US 
Starlix Tablet, film coated 180 mg Oral Novartis Europharm Limited 2016-09-08 2022-06-28 EU 
Starlix Tablet, film coated 120 mg Oral Novartis Europharm Limited 2016-09-08 2022-06-28 EU Starlix Tablet, film coated 120 mg Oral Novartis Europharm Limited 2016-09-08 2022-06-28 EU Starlix Tablet, film coated 60 mg Oral Novartis Europharm Limited 2016-09-08 2022-06-28 EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nateglinide Tablet, coated 60 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 2009-09-08 Not applicable US Nateglinide Tablet, coated 120 mg/1 Oral Golden State Medical Supply, Inc. 2009-09-09 2023-11-30 US Nateglinide Tablet, coated 60 mg/1 Oral Nivagen Pharmaceuticals, Inc. 2019-09-25 Not applicable US Nateglinide Tablet 120 mg/1 Oral American Health Packaging 2022-12-29 Not applicable US Nateglinide Tablet, coated 120 mg/1 Oral American Health Packaging 2011-01-05 2023-10-31 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image NAT-ALA 120/200 MG FILM KAPLI TABLET, 90 ADET Nateglinide (120 mg) + Lipoic acid (200 mg) Tablet, coated Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2011-12-08 Not applicable Turkey 
NAT-ALA 180/200 MG FILM KAPLI TABLET, 90 ADET Nateglinide (180 mg) + Lipoic acid (200 mg) Tablet, coated Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2011-11-21 Not applicable Turkey NATMET 120/1000 MG TEDAVI PAKETI, 90+90 ADET Nateglinide (120 mg) + Metformin hydrochloride (1000 mg) Tablet Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-06-24 Not applicable Turkey NATMET 120/500 MG TEDAVI PAKETI, 90+90 ADET Nateglinide (120 mg) + Metformin hydrochloride (500 mg) Tablet, film coated Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-06-24 Not applicable Turkey NATMET 120/850 MG TEDAVI PAKETI, 90+90 ADET Nateglinide (120 mg) + Metformin hydrochloride (850 mg) Tablet, film coated Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-08-01 Not applicable Turkey
Categories
- ATC Codes
- A10BX03 — Nateglinide
- Drug Categories
- Alimentary Tract and Metabolism
- Amino Acids
- Amino Acids, Aromatic
- Amino Acids, Cyclic
- Amino Acids, Peptides, and Proteins
- Blood Glucose Lowering Agents
- Cyclohexanes
- Cycloparaffins
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Drugs Used in Diabetes
- Glinide
- Hypoglycemia-Associated Agents
- Insulin Secretagogues
- OAT1/SLC22A6 inhibitors
- Oral Hypoglycemics
- Potassium Channel Blockers
- UGT1A9 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylalanine and derivatives. These are compounds containing phenylalanine or a derivative thereof resulting from reaction of phenylalanine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Phenylalanine and derivatives
- Alternative Parents
- N-acyl-alpha amino acids / Phenylpropanoic acids / Monocyclic monoterpenoids / Menthane monoterpenoids / Aromatic monoterpenoids / Amphetamines and derivatives / Secondary carboxylic acid amides / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds show 4 more
- Substituents
- 3-phenylpropanoic-acid / Amphetamine or derivatives / Aromatic homomonocyclic compound / Aromatic monoterpenoid / Benzenoid / Carbonyl group / Carboxamide group / Carboxylic acid / Hydrocarbon derivative / Monocarboxylic acid or derivatives show 14 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- N-acyl-D-phenylalanine (CHEBI:31897)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 41X3PWK4O2
- CAS number
- 105816-04-4
- InChI Key
- OELFLUMRDSZNSF-BRWVUGGUSA-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-{[(1r,4r)-4-(propan-2-yl)cyclohexyl]formamido}propanoic acid
- SMILES
- CC(C)[C@H]1CC[C@@H](CC1)C(=O)N[C@H](CC1=CC=CC=C1)C(O)=O
References
- Synthesis Reference
Michito Sumikawa, "Methods for producing nateglinide B-type crystals." U.S. Patent US20030229249, issued December 11, 2003.
US20030229249- General References
- FDA Approved Drug Products: STARLIX (nateglinide) tablets [Link]
- External Links
- Human Metabolome Database
- HMDB14869
- KEGG Drug
- D01111
- KEGG Compound
- C12508
- PubChem Compound
- 5311309
- PubChem Substance
- 46504836
- ChemSpider
- 10482084
- BindingDB
- 50344967
- 274332
- ChEBI
- 31897
- ChEMBL
- CHEMBL783
- ZINC
- ZINC000101489663
- Therapeutic Targets Database
- DAP000918
- PharmGKB
- PA450600
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Nateglinide
- FDA label
- Download (56.5 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 Prevention Impaired Fasting Glucose (IFG) / Resistance, Insulin 1 4 Completed Treatment Diabetes Mellitus / Type 2 Diabetes Mellitus 1 4 Completed Treatment Post Transplant Diabetes Mellitus / Posttransplant Impaired Glucose Tolerance / Renal Transplant Recipient Patients 1 4 Completed Treatment Resistance, Insulin / Type 2 Diabetes Mellitus 1 4 Completed Treatment Type 2 Diabetes Mellitus 6
Pharmacoeconomics
- Manufacturers
- Dr reddys laboratories ltd
- Par pharmaceutical inc
- Teva pharmaceuticals usa
- Novartis pharmaceuticals corp
- Packagers
- Caremark LLC
- Doctor Reddys Laboratories Ltd.
- Heartland Repack Services LLC
- Mckesson Corp.
- Novartis AG
- Par Pharmaceuticals
- Physicians Total Care Inc.
- Resource Optimization and Innovation LLC
- Vangard Labs Inc.
- Dosage Forms
Form Route Strength Tablet, film coated Oral 180 mg Tablet, film coated Oral Tablet, coated Oral Tablet Oral 60 mg/1 Tablet, coated Oral 120 mg/1 Tablet, coated Oral 60 mg/1 Tablet, film coated Oral 120 mg/1 Tablet, film coated Oral 60 mg/1 Tablet Oral Tablet, film coated Oral Tablet Oral 120 mg/1 Tablet Oral 120 mg Tablet Oral 180 mg Tablet Oral 60 mg Tablet, film coated Oral 120 mg Tablet, film coated Oral 60 mg - Prices
Unit description Cost Unit Starlix 120 mg tablet 2.12USD tablet Starlix 60 mg tablet 2.01USD tablet Nateglinide 120 mg tablet 1.73USD tablet Nateglinide 60 mg tablet 1.66USD 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 USRE34878 No 1995-03-14 2009-09-08 US CA2271865 No 2003-10-14 2017-11-14 Canada 
CA2114678 No 1999-04-27 2014-02-01 Canada US6559188 No 2003-05-06 2020-09-15 US US6641841 No 2003-11-04 2017-11-14 US US6844008 No 2005-01-18 2017-11-14 US US6878749 No 2005-04-12 2020-09-15 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Practically insoluble Not Available logP 2.4 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00848 mg/mL ALOGPS logP 3.59 ALOGPS logP 4.03 Chemaxon logS -4.6 ALOGPS pKa (Strongest Acidic) 4 Chemaxon pKa (Strongest Basic) -1.1 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 66.4 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 89.46 m3·mol-1 Chemaxon Polarizability 35.55 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9156 Blood Brain Barrier + 0.7539 Caco-2 permeable - 0.7148 P-glycoprotein substrate Substrate 0.6187 P-glycoprotein inhibitor I Non-inhibitor 0.8842 P-glycoprotein inhibitor II Non-inhibitor 0.8604 Renal organic cation transporter Non-inhibitor 0.8882 CYP450 2C9 substrate Non-substrate 0.7192 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.5103 CYP450 1A2 substrate Non-inhibitor 0.9167 CYP450 2C9 inhibitor Non-inhibitor 0.8412 CYP450 2D6 inhibitor Non-inhibitor 0.9088 CYP450 2C19 inhibitor Non-inhibitor 0.8764 CYP450 3A4 inhibitor Non-inhibitor 0.8874 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8734 Ames test Non AMES toxic 0.922 Carcinogenicity Non-carcinogens 0.9354 Biodegradation Not ready biodegradable 0.7779 Rat acute toxicity 2.0362 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9881 hERG inhibition (predictor II) Non-inhibitor 0.8425
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 191.2963439 predictedDarkChem Lite v0.1.0 [M-H]- 175.08571 predictedDeepCCS 1.0 (2019) [M+H]+ 190.1752439 predictedDarkChem Lite v0.1.0 [M+H]+ 177.48126 predictedDeepCCS 1.0 (2019) [M+Na]+ 184.15628 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- 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]
- 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. [Article]
- Norman P, Rabasseda X: Nateglinide: A structurally novel, short-acting, hypoglycemic agent. Drugs Today (Barc). 2001 Jun;37(6):411-426. [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]
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
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Kirchheiner J, Meineke I, Muller G, Bauer S, Rohde W, Meisel C, Roots I, Brockmoller J: Influence of CYP2C9 and CYP2D6 polymorphisms on the pharmacokinetics of nateglinide in genotyped healthy volunteers. Clin Pharmacokinet. 2004;43(4):267-78. doi: 10.2165/00003088-200443040-00005. [Article]
- Takanohashi T, Kubo S, Nakayama A, Mihara R, Hayashi M: Inhibition of human liver microsomal CYP by nateglinide. J Pharm Pharmacol. 2010 May;62(5):592-7. doi: 10.1211/jpp.62.05.0005. [Article]
- Pakkir Maideen NM, Manavalan G, Balasubramanian K: Drug interactions of meglitinide antidiabetics involving CYP enzymes and OATP1B1 transporter. Ther Adv Endocrinol Metab. 2018 Apr 6;9(8):259-268. doi: 10.1177/2042018818767220. eCollection 2018. [Article]
- Nateglinide FD label [File]
- 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
- 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]
- Takanohashi T, Kubo S, Nakayama A, Mihara R, Hayashi M: Inhibition of human liver microsomal CYP by nateglinide. J Pharm Pharmacol. 2010 May;62(5):592-7. doi: 10.1211/jpp.62.05.0005. [Article]
- Pakkir Maideen NM, Manavalan G, Balasubramanian K: Drug interactions of meglitinide antidiabetics involving CYP enzymes and OATP1B1 transporter. Ther Adv Endocrinol Metab. 2018 Apr 6;9(8):259-268. doi: 10.1177/2042018818767220. eCollection 2018. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- 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 un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- 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 un...
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- 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 gas...
- Gene Name
- PTGS1
- Uniprot ID
- P23219
- Uniprot Name
- Prostaglandin G/H synthase 1
- Molecular Weight
- 68685.82 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]
- Kind
- Protein
- Organism
- Humans
- 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 trans...
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1-9
- Molecular Weight
- 59940.495 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]
- Kind
- Protein
- Organism
- Humans
- 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...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Kirchheiner J, Meineke I, Muller G, Bauer S, Rohde W, Meisel C, Roots I, Brockmoller J: Influence of CYP2C9 and CYP2D6 polymorphisms on the pharmacokinetics of nateglinide in genotyped healthy volunteers. Clin Pharmacokinet. 2004;43(4):267-78. doi: 10.2165/00003088-200443040-00005. [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
- Kind
- Protein
- Organism
- Humans
- 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...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- 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
- Uniprot Name
- Multidrug resistance-associated protein 4
- Molecular Weight
- 149525.33 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 leucin...
- Gene Name
- SLC16A1
- Uniprot ID
- P53985
- Uniprot Name
- Monocarboxylate transporter 1
- Molecular Weight
- 53943.685 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Uniprot Name
- Solute carrier family 15 member 1
- Molecular Weight
- 78805.265 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Uniprot Name
- Solute carrier family 15 member 2
- Molecular Weight
- 81782.77 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at December 02, 2023 06:54