Identification
- Summary
Ceftibuten is a third-generation cephalosporin antibiotic commonly used in the treatment of acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsillitis.
- Brand Names
- Cedax
- Generic Name
- Ceftibuten
- DrugBank Accession Number
- DB01415
- Background
Ceftibuten is a third-generation cephalosporin antibiotic that is orally-administered. It is typically used to treat acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsilitis.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ceftibuten (DB01415)
- Weight
- Average: 410.425
Monoisotopic: 410.03547558 - Chemical Formula
- C15H14N4O6S2
- Synonyms
- (+)-(6R,7R)-7-((Z)-2-(2-amino-4-thiazolyl)-4-carboxycrotonamido)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
- Ceftibuten
- Ceftibutene
- Ceftibuteno
- Ceftibutenum
- cis-ceftibuten
- External IDs
- 7432-S
- SCH 39720
Pharmacology
- Indication
Indicated for the treatment of acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsilitis.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute bacterial exacerbation of chronic bronchitis •••••••••••• Used in combination to treat Acute bronchitis Combination Product in combination with: Clavulanic acid (DB00766) •••••••••••• •••••• Used in combination to treat Acute otitis media Combination Product in combination with: Clavulanic acid (DB00766) •••••••••••• •••••••• •••••• Used in combination to treat Acute sinusitis Combination Product in combination with: Clavulanic acid (DB00766) •••••••••••• •••••• Treatment of Bacterial infections •••••••••••• - 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
Ceftibuten is an antibiotic with bactericidal actions.
- Mechanism of action
Ceftibuten exerts its bactericidal action by binding to essential target proteins of the bacterial cell wall. This binding leads to inhibition of cell-wall synthesis.
Target Actions Organism APeptidoglycan synthase FtsI inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1A inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1B inhibitorEscherichia coli (strain K12) APenicillin-binding protein 2 inhibitorEscherichia coli (strain K12) - Absorption
Rapidly absorbed following oral administration.
- Volume of distribution
- 0.21 L/kg [adult subjects]
- 0.5 L/kg [fasting pediatric patients]
- Protein binding
Ceftibuten is 65% bound to plasma proteins. The protein binding is independent of plasma ceftibuten concentration.
- Metabolism
A study with radiolabeled ceftibuten administered to 6 healthy adult male volunteers demonstrated that cis-ceftibuten is the predominant component in both plasma and urine. About 10% of ceftibuten is converted to the trans-isomer is approximately 1/8 as antimicrobially potent as the cis-isomer.
- Route of elimination
Ceftibuten is excreted in the urine; 95% of the administered radioactivity was recovered either in urine or feces.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Overdosage of cephalosporins can cause cerebral irritation leading to convulsions.
- Pathways
- Not Available
- 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 Ceftibuten may decrease the excretion rate of Abacavir which could result in a higher serum level. Abciximab The therapeutic efficacy of Abciximab can be decreased when used in combination with Ceftibuten. Acamprosate The excretion of Acamprosate can be decreased when combined with Ceftibuten. Aceclofenac The risk or severity of nephrotoxicity can be increased when Ceftibuten is combined with Aceclofenac. Acemetacin The risk or severity of nephrotoxicity can be increased when Ceftibuten is combined with Acemetacin. - Food Interactions
- Take separate from meals. Take ceftibuten oral suspension at least one hour after eating, or two hours before eating.
- Take with or without food. Separating the administration of ceftibuten from food is not required for ceftibuten capsules because the impact of food on bioavailability is less significant.
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 Ingredients
Ingredient UNII CAS InChI Key Ceftibuten dihydrate 62F4443RWP 118081-34-8 SSWTVBYDDFPFAF-DKOGRLLHSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cedax Suspension 180 mg/5mL Oral Pernix Therapeutics 2010-10-20 2017-12-31 US 
Cedax Suspension 18 mg/1mL Oral Sciele Pharma, Inc. 1995-12-20 Not applicable US Cedax Capsule 400 mg/1 Oral Shionogi USA, Inc. 1995-12-01 2011-06-30 US Cedax Suspension 90 mg/5mL Oral Pernix Therapeutics 1995-12-20 2012-08-01 US Cedax Capsule 400 mg/1 Oral Sciele Pharma, Inc. 1995-12-20 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ceftibuten Capsule 400 mg/1 Oral Macoven Pharmaceuticals 2013-10-01 2017-12-31 US Ceftibuten Suspension 180 mg/5mL Oral Macoven Pharmaceuticals 2013-10-01 2017-12-31 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BUCEF PLUS 180/62.5 MG TOZ ICEREN SASE, 20 ADET Ceftibuten dihydrate (180 mg) + Clavulanic acid (62.5 mg) Powder Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2010-12-27 Not applicable Turkey 
BUCEF PLUS 90/62.5 MG TOZ ICEREN SASE, 20 ADET Ceftibuten dihydrate (90 mg) + Clavulanic acid (62.5 mg) Powder Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2010-12-27 Not applicable Turkey WINCEF PLUS 180/62.5 MG/5 ML ORAL SUSPANSIYON HAZIRLAMAK ICIN KURU TOZ, 100 ML Ceftibuten (180 mg/5mL) + Clavulanic acid (62.5 mg/5mL) Suspension Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2012-01-12 2018-07-09 Turkey WINCEF PLUS 200/62.5 MG FILM KAPLI TABLET, 20 ADET Ceftibuten (200 mg) + Clavulanic acid (62.5 mg) Tablet, coated Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2012-02-09 2018-07-09 Turkey WINCEF PLUS 400/125 MG FILM KAPLI TABLET, 10 ADET Ceftibuten (400 mg) + Clavulanic acid (125 mg) Tablet, coated Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2012-02-09 2018-07-09 Turkey
Categories
- ATC Codes
- J01DD14 — Ceftibuten
- Drug Categories
- Amides
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antiinfectives for Systemic Use
- beta-Lactams
- Cephalosporins
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Lactams
- Nephrotoxic agents
- OAT1/SLC22A6 Substrates
- OAT3/SLC22A8 Inhibitors
- OAT3/SLC22A8 Substrates
- Sulfur Compounds
- Thiazines
- Third-Generation Cephalosporins
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cephalosporins. These are compounds containing a 1,2-thiazine fused to a 2-azetidinone to for a oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid moiety or a derivative thereof.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Lactams
- Sub Class
- Beta lactams
- Direct Parent
- Cephalosporins
- Alternative Parents
- N-acyl-alpha amino acids and derivatives / 2,4-disubstituted thiazoles / 1,3-thiazines / 2-amino-1,3-thiazoles / Dicarboxylic acids and derivatives / N-acyl amines / Tertiary carboxylic acid amides / Heteroaromatic compounds / Secondary carboxylic acid amides / Amino acids show 10 more
- Substituents
- 1,3-thiazol-2-amine / 2,4-disubstituted 1,3-thiazole / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Azetidine / Azole show 24 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- cephalosporin, dicarboxylic acid (CHEBI:3510)
- Affected organisms
- Enteric bacteria and other eubacteria
Chemical Identifiers
- UNII
- IW71N46B4Y
- CAS number
- 97519-39-6
- InChI Key
- UNJFKXSSGBWRBZ-BJCIPQKHSA-N
- InChI
- InChI=1S/C15H14N4O6S2/c16-15-17-7(5-27-15)6(1-2-9(20)21)11(22)18-10-12(23)19-8(14(24)25)3-4-26-13(10)19/h1,3,5,10,13H,2,4H2,(H2,16,17)(H,18,22)(H,20,21)(H,24,25)/b6-1-/t10-,13-/m1/s1
- IUPAC Name
- (6R,7R)-7-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
- SMILES
- [H][C@]12SCC=C(N1C(=O)[C@H]2NC(=O)C(=C/CC(O)=O)\C1=CSC(N)=N1)C(O)=O
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015485
- KEGG Drug
- D00922
- KEGG Compound
- C08117
- PubChem Compound
- 5282242
- PubChem Substance
- 46507324
- ChemSpider
- 4445419
- BindingDB
- 50370586
- 20492
- ChEBI
- 3510
- ChEMBL
- CHEMBL1605
- ZINC
- ZINC000003871967
- Therapeutic Targets Database
- DAP000456
- PharmGKB
- PA164744555
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Ceftibuten
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 3 Terminated Treatment Pyelonephritis 1 1 Completed Basic Science Healthy Subjects (HS) 2 1 Completed Basic Science Pharmacokinetics 1 1 Completed Treatment Pharmacokinetics 1 1 Not Yet Recruiting Treatment Bacterial Infections 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Schering Corp.
- Sciele Pharma Inc.
- Shionogi Pharma Inc.
- Zyber Pharmaceuticals
- Dosage Forms
Form Route Strength Powder Oral Powder Oral Capsule Oral 200 MG Capsule Oral 400 mg/1 Capsule Oral 400 MG Capsule Oral 400.00 mg Granule, for suspension Oral 14.4 g/100g Suspension Oral 18 mg/1mL Suspension Oral 2.1600 g Suspension Oral 90 mg/5mL Tablet, effervescent Suspension Oral 180 mg/5mL Powder, for suspension Oral 3.6 g Capsule Oral 400.000 mg Suspension Oral 3.600 g Granule, for suspension Oral 200 mg Granule, for suspension Oral 36 mg/mL Granule, for suspension Oral 400 mg Suspension Oral 36 mg/ml Capsule Oral Granule, for suspension Oral Tablet, film coated 200 mg Tablet, film coated 400 mg Suspension Oral Tablet, coated Oral Capsule Oral 435.120 mg - Prices
Unit description Cost Unit Cedax 400 mg capsule 16.13USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5599557 No 1997-02-04 2014-02-04 US US4634697 No 1987-01-06 2009-10-01 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0705 mg/mL ALOGPS logP 0.31 ALOGPS logP -1.5 Chemaxon logS -3.8 ALOGPS pKa (Strongest Acidic) 2.85 Chemaxon pKa (Strongest Basic) 4.68 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 162.92 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 97.02 m3·mol-1 Chemaxon Polarizability 38.49 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 - 0.5755 Blood Brain Barrier - 0.9679 Caco-2 permeable - 0.8957 P-glycoprotein substrate Substrate 0.5424 P-glycoprotein inhibitor I Non-inhibitor 0.9274 P-glycoprotein inhibitor II Non-inhibitor 0.9586 Renal organic cation transporter Non-inhibitor 0.929 CYP450 2C9 substrate Non-substrate 0.8531 CYP450 2D6 substrate Non-substrate 0.8293 CYP450 3A4 substrate Non-substrate 0.6007 CYP450 1A2 substrate Non-inhibitor 0.8787 CYP450 2C9 inhibitor Non-inhibitor 0.8817 CYP450 2D6 inhibitor Non-inhibitor 0.9191 CYP450 2C19 inhibitor Non-inhibitor 0.8833 CYP450 3A4 inhibitor Non-inhibitor 0.9625 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9387 Ames test Non AMES toxic 0.7274 Carcinogenicity Non-carcinogens 0.8961 Biodegradation Not ready biodegradable 0.9688 Rat acute toxicity 1.6446 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9848 hERG inhibition (predictor II) Non-inhibitor 0.9305
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-00l6-4429000000-9eb742eca3a39f7f33c7 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-01q9-0902600000-c2388ee87fe4a0c57f08 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-01b9-0219000000-190493c1b5a3aa9e4571 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0j5c-0392000000-5e8978fc10ac139bd0fa Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0079-0129000000-be37f9cbf73c4ef955d4 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-001c-9618000000-8887fe2fa2644176a32c Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-05tf-0942000000-0dc6c5afe7b099d98aaa Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 191.9374743 predictedDarkChem Lite v0.1.0 [M-H]- 200.9991743 predictedDarkChem Lite v0.1.0 [M-H]- 185.77048 predictedDeepCCS 1.0 (2019) [M+H]+ 190.5948743 predictedDarkChem Lite v0.1.0 [M+H]+ 200.9544743 predictedDarkChem Lite v0.1.0 [M+H]+ 188.16603 predictedDeepCCS 1.0 (2019) [M+Na]+ 190.8420743 predictedDarkChem Lite v0.1.0 [M+Na]+ 201.3120743 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.31775 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Peptidoglycan glycosyltransferase activity
- Specific Function
- Essential cell division protein that is required for the synthesis of peptidoglycan at the division septum (PubMed:1103132, PubMed:9614966). Catalyzes the synthesis of cross-linked peptidoglycan fr...
- Gene Name
- ftsI
- Uniprot ID
- P0AD68
- Uniprot Name
- Peptidoglycan synthase FtsI
- Molecular Weight
- 63876.925 Da
References
- Wise R, Andrews JM, Ashby JP, Thornber D: Ceftibuten--in-vitro activity against respiratory pathogens, beta-lactamase stability and mechanism of action. J Antimicrob Chemother. 1990 Aug;26(2):209-13. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation. Synthesis of cross-linked peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcA
- Uniprot ID
- P02918
- Uniprot Name
- Penicillin-binding protein 1A
- Molecular Weight
- 93635.545 Da
References
- Wise R, Andrews JM, Ashby JP, Thornber D: Ceftibuten--in-vitro activity against respiratory pathogens, beta-lactamase stability and mechanism of action. J Antimicrob Chemother. 1990 Aug;26(2):209-13. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation. Synthesis of cross-linked peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcB
- Uniprot ID
- P02919
- Uniprot Name
- Penicillin-binding protein 1B
- Molecular Weight
- 94291.875 Da
References
- Wise R, Andrews JM, Ashby JP, Thornber D: Ceftibuten--in-vitro activity against respiratory pathogens, beta-lactamase stability and mechanism of action. J Antimicrob Chemother. 1990 Aug;26(2):209-13. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. It synthesizes cross-linked peptidoglycan from lipid intermediates.
- Gene Name
- mrdA
- Uniprot ID
- P0AD65
- Uniprot Name
- Penicillin-binding protein 2
- Molecular Weight
- 70856.1 Da
References
- Wise R, Andrews JM, Ashby JP, Thornber D: Ceftibuten--in-vitro activity against respiratory pathogens, beta-lactamase stability and mechanism of action. J Antimicrob Chemother. 1990 Aug;26(2):209-13. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Ganapathy ME, Prasad PD, Mackenzie B, Ganapathy V, Leibach FH: Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Biochim Biophys Acta. 1997 Mar 13;1324(2):296-308. [Article]
- Luckner P, Brandsch M: Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. Eur J Pharm Biopharm. 2005 Jan;59(1):17-24. [Article]
- Saito H, Okuda M, Terada T, Sasaki S, Inui K: Cloning and characterization of a rat H+/peptide cotransporter mediating absorption of beta-lactam antibiotics in the intestine and kidney. J Pharmacol Exp Ther. 1995 Dec;275(3):1631-7. [Article]
- Terada T, Saito H, Mukai M, Inui K: Characterization of stably transfected kidney epithelial cell line expressing rat H+/peptide cotransporter PEPT1: localization of PEPT1 and transport of beta-lactam antibiotics. J Pharmacol Exp Ther. 1997 Jun;281(3):1415-21. [Article]
- Terada T, Saito H, Mukai M, Inui K: Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells. Am J Physiol. 1997 Nov;273(5 Pt 2):F706-11. [Article]
- Tsuji A: Transporter-mediated Drug Interactions. Drug Metab Pharmacokinet. 2002;17(4):253-74. [Article]
- Menon RM, Barr WH: Transporters involved in apical and basolateral uptake of ceftibuten into Caco-2 cells. Biopharm Drug Dispos. 2002 Nov;23(8):317-26. [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
- Ganapathy ME, Prasad PD, Mackenzie B, Ganapathy V, Leibach FH: Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Biochim Biophys Acta. 1997 Mar 13;1324(2):296-308. [Article]
- Terada T, Saito H, Mukai M, Inui K: Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells. Am J Physiol. 1997 Nov;273(5 Pt 2):F706-11. [Article]
- Luckner P, Brandsch M: Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. Eur J Pharm Biopharm. 2005 Jan;59(1):17-24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Substrate profile was investigated in in vitro studies using HEK293 cells.
- 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
- VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Substrate and inhibitor profile was investigated in vitro using human OAT3 expressed on HEK293 cells.
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]
Drug created at July 23, 2007 13:06 / Updated at February 02, 2024 22:51