Cefadroxil

Identification

Summary

Cefadroxil is a cephalosporin antibiotic used in the treatment of various bacterial infections, such as urinary tract infections, skin and skin structure infections, and tonsillitis.

Generic Name
Cefadroxil
DrugBank Accession Number
DB01140
Background

Long-acting, broad-spectrum, water-soluble, cephalexin derivative.

Type
Small Molecule
Groups
Approved, Vet approved, Withdrawn
Structure
Thumb
Weight
Average: 363.388
Monoisotopic: 363.088891359
Chemical Formula
C16H17N3O5S
Synonyms
  • CDX
  • Cefadroxil
  • Cefadroxil anhydrous
  • Cefadroxilo
  • Cefadroxilum
  • Cephadroxil
  • D-Cefadroxil

Pharmacology

Indication

For the treatment of the following infections (skin, UTI, ENT) caused by; S. pneumoniae, H. influenzae, staphylococci, S. pyogenes (group A beta-hemolytic streptococci), E. coli, P. mirabilis, Klebsiella sp, coagulase-negative staphylococci and Streptococcus pyogenes

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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Cefadroxil, a first-generation cephalosporin antibiotic, is used to treat urinary tract infections, skin and skin structure infections, pharyngitis, and tonsillitis.

Mechanism of action

Like all beta-lactam antibiotics, cefadroxil binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefadroxil interferes with an autolysin inhibitor.

TargetActionsOrganism
APenicillin-binding protein 3
inhibitor
Streptococcus pneumoniae
APenicillin-binding protein 1A
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
APenicillin-binding protein 1b
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
APenicillin-binding protein 2B
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Absorption

Cefadroxil is well absorbed on oral administration; food does not interfere with its absorption.

Volume of distribution

Not Available

Protein binding

Binding rates of cefadroxil were 28.1% by U.F. method

Metabolism
Not Available
Route of elimination

Over 90% of the drug is excreted unchanged in the urine within 24 hours. Cefadroxil was detected in the placenta and breast milk.

Half-life

1.5 hours

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Nausea, vomiting, diarrhoea, allergic rashes may occur

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AbacavirCefadroxil may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Cefadroxil.
AcamprosateThe excretion of Acamprosate can be decreased when combined with Cefadroxil.
AceclofenacThe risk or severity of nephrotoxicity can be increased when Cefadroxil is combined with Aceclofenac.
AcemetacinThe risk or severity of nephrotoxicity can be increased when Cefadroxil is combined with Acemetacin.
AcenocoumarolThe risk or severity of bleeding can be increased when Cefadroxil is combined with Acenocoumarol.
AcetaminophenCefadroxil may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Cefadroxil which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidThe risk or severity of nephrotoxicity can be increased when Acetylsalicylic acid is combined with Cefadroxil.
AclidiniumCefadroxil may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Interactions
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Food Interactions
  • Take with or without food. Administration with food may be helpful in diminishing potential gastrointestinal complaints occasionally associated with oral cephalosporin therapy.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Cefadroxil hemihydrateJ9CMF6461M119922-85-9AJAMDISMDZXITN-QXBGZBSVSA-N
Cefadroxil monohydrate280111G16066592-87-8NBFNMSULHIODTC-CYJZLJNKSA-N
Cefadroxil sodiumSSZ6380I0I42284-83-3GQOVFIUWRATNJC-CYJZLJNKSA-M
Product Images
International/Other Brands
Baxan (Bristol-Myers Squibb) / Bidocef (Bristol-Myers Squibb) / Cefamox (Bristol-Myers Squibb) / Duracef (Bristol-Myers Squibb) / Oracefal (Bristol-Myers Squibb)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CefadroxilCapsule500 mg / capOralApotex CorporationNot applicableNot applicableCanada flag
CefadroxilTablet, film coated1 g/1OralORCHID HEALTHCARE (A DIVISION OF ORCHID CHEMICALS AND PHARMACEUTICALS LTD.)2008-01-23Not applicableUS flag
DuricefPowder, for suspension500 mg/5mLOralAllergan1980-09-122008-11-30US flag
DuricefCapsule500 mg/1OralAllergan1978-02-172007-04-30US flag
DuricefPowder, for suspension250 mg/5mLOralAllergan1980-09-122008-11-30US flag
DuricefTablet1 g/1OralAllergan1980-08-062006-07-31US flag
DuricefCapsule500 mgOralBristol Myers Squibb1981-12-312009-02-05Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-cefadroxilCapsule500 mgOralApotex Corporation1999-08-31Not applicableCanada flag
CefadroxilCapsule500 mg/1OralRpk Pharmaceuticals, Inc.2008-04-23Not applicableUS flag
CefadroxilPowder, for suspension125 mg/5mLOralRanbaxy Inc.2005-08-30Not applicableUS flag
CefadroxilCapsule500 mg/1OralAidarex Pharmaceuticals LLC2008-04-23Not applicableUS flag
CefadroxilPowder, for suspension250 mg/5mLOralHikma Pharmaceuticals USA Inc.2012-11-28Not applicableUS flag
CefadroxilCapsule500 mg/1OralRedPharm Drug, Inc.2019-11-01Not applicableUS flag
CefadroxilCapsule500 mg/1OralPD-Rx Pharmaceuticals, Inc.2008-04-23Not applicableUS flag
CefadroxilCapsule500 mg/1OralNucare Pharmaceuticals, Inc.2008-04-23Not applicableUS flag
CefadroxilCapsule500 mg/1OralNucare Pharmaceuticals,inc.2007-01-25Not applicableUS flag
CefadroxilTablet, film coated1 g/1OralJazeera Pharmaceutical2006-03-31Not applicableUS flag

Categories

ATC Codes
J01DB05 — Cefadroxil
Drug Categories
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 / Alpha amino acid amides / Phenylacetamides / 1-hydroxy-2-unsubstituted benzenoids / Aralkylamines / 1,3-thiazines / Tertiary carboxylic acid amides / Secondary carboxylic acid amides / Amino acids / Azetidines
show 10 more
Substituents
1-hydroxy-2-unsubstituted benzenoid / Alpha-amino acid amide / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Azetidine
show 26 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
cephalosporin (CHEBI:3479)
Affected organisms
  • Enteric bacteria and other eubacteria

Chemical Identifiers

UNII
Q525PA8JJB
CAS number
50370-12-2
InChI Key
BOEGTKLJZSQCCD-UEKVPHQBSA-N
InChI
InChI=1S/C16H17N3O5S/c1-7-6-25-15-11(14(22)19(15)12(7)16(23)24)18-13(21)10(17)8-2-4-9(20)5-3-8/h2-5,10-11,15,20H,6,17H2,1H3,(H,18,21)(H,23,24)/t10-,11-,15-/m1/s1
IUPAC Name
(6R,7R)-7-[(2R)-2-amino-2-(4-hydroxyphenyl)acetamido]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
SMILES
[H][C@]12SCC(C)=C(N1C(=O)[C@H]2NC(=O)[C@H](N)C1=CC=C(O)C=C1)C(O)=O

References

Synthesis Reference

Leonardo Marsili, "Substantially anhydrous crystalline cefadroxil and method for producing it." U.S. Patent US5329001, issued April, 1978.

US5329001
General References
Not Available
Human Metabolome Database
HMDB0015271
KEGG Drug
D00257
KEGG Compound
C06878
PubChem Compound
47965
PubChem Substance
46509128
ChemSpider
43630
BindingDB
50350467
RxNav
1545975
ChEBI
3479
ChEMBL
CHEMBL1644
ZINC
ZINC000003830391
Therapeutic Targets Database
DAP000446
PharmGKB
PA448835
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cefadroxil
FDA label
Download (334 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedOtherUrinary Tract Infection1
4CompletedTreatmentAnti-Infective Agents / Bacterial Infections / Breast Implantation1
3Enrolling by InvitationTreatmentJoint Infections1
2CompletedTreatmentPulmonary Tuberculosis (TB)1
1CompletedNot AvailableHealthy Subjects (HS)3
1CompletedBasic ScienceHealthy Subjects (HS)1
1CompletedBasic ScienceOsteomyelitis / Pyomyositis / Septic Arthritis1
Not AvailableCompletedTreatmentMastitis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Aidarex Pharmacuticals LLC
  • Apothecon
  • A-S Medication Solutions LLC
  • Aurobindo Pharma Ltd.
  • Barr Pharmaceuticals
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Greenstone LLC
  • H.J. Harkins Co. Inc.
  • Hikma Pharmaceuticals
  • Innoviant Pharmacy Inc.
  • Institut Biochemique SA
  • Jazeera Pharmaceutical Industries
  • Lupin Pharmaceuticals Inc.
  • Major Pharmaceuticals
  • Murfreesboro Pharmaceutical Nursing Supply
  • Northstar Rx LLC
  • Nucare Pharmaceuticals Inc.
  • Orchid Healthcare
  • Palmetto Pharmaceuticals Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prescript Pharmaceuticals
  • Prescription Dispensing Service Inc.
  • Putney Inc.
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Sandoz
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Warner Chilcott Co. Inc.
  • West-Ward Pharmaceuticals
Dosage Forms
FormRouteStrength
Powder, for suspensionOral10.5 g
Tablet, film coatedOral
Powder, for suspensionOral
CapsuleOral
Granule, for suspensionOral
CapsuleOral500 mg/1
CapsuleOral500 mg / cap
Powder, for suspensionOral125 mg/5mL
Powder, for suspensionOral250 mg/5mL
Powder, for suspensionOral500 mg/5mL
TabletOral1000 mg/1
Tablet, film coatedOral1 g/1
TabletOral1000 MG
Tablet, coatedOral
Tablet, film coatedOral1000 MG
Tablet, coatedOral1 g
Powder, for suspensionOral5 g
Powder, for suspensionOral10 g
Injection, powder, for suspensionParenteral2.5 g
Suspension
TabletOral
Tablet, for suspension
Powder, for suspensionOral2.5 g
TabletOral1 g/1
TabletOral1 G
PowderParenteral500 MG/5ML
Syrup
Solution / drops; suspension / drops
Capsule, coatedOral500 mg
CapsuleOral500 MG
CapsuleOral250 mg
PowderParenteral250 mg/5ml
Prices
Unit descriptionCostUnit
Duricef 1 gm tablet7.35USD tablet
Cefadroxil 1 gm tablet7.14USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)197 °Clshirnaru.T.and Kodarna.Y.: US. Patent 3864340; February 4,1975; assigned to Toyama Chemical Co. Ltd. (Japan) Crast, L.B. Jr. and Gottstein, W.J.; U S . Patent 3,985,741; October 12,1976; assigned to Bristol-Mvers Co.
water solubility1110 mg/LNot Available
logP-0.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.399 mg/mLALOGPS
logP0.51ALOGPS
logP-2.4ChemAxon
logS-3ALOGPS
pKa (Strongest Acidic)3.45ChemAxon
pKa (Strongest Basic)7.43ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area132.96 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity90.95 m3·mol-1ChemAxon
Polarizability35.86 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.692
Blood Brain Barrier-0.9966
Caco-2 permeable-0.8634
P-glycoprotein substrateSubstrate0.7944
P-glycoprotein inhibitor INon-inhibitor0.9106
P-glycoprotein inhibitor IINon-inhibitor0.99
Renal organic cation transporterNon-inhibitor0.9398
CYP450 2C9 substrateNon-substrate0.8156
CYP450 2D6 substrateNon-substrate0.8285
CYP450 3A4 substrateNon-substrate0.5
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8421
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.873
Ames testNon AMES toxic0.6606
CarcinogenicityNon-carcinogens0.881
BiodegradationNot ready biodegradable0.9564
Rat acute toxicity1.5290 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9939
hERG inhibition (predictor II)Non-inhibitor0.8295
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets2
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Kind
Protein
Organism
Streptococcus pneumoniae
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type d-ala-d-ala carboxypeptidase activity
Specific Function
Not Available
Gene Name
pbp3
Uniprot ID
Q75Y35
Uniprot Name
Penicillin-binding protein 3
Molecular Weight
45209.84 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [Article]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Penicillin binding
Specific Function
Cell wall formation.
Gene Name
pbpA
Uniprot ID
Q8DR59
Uniprot Name
Penicillin-binding protein 1A
Molecular Weight
79700.9 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [Article]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transferase activity, transferring acyl groups
Specific Function
Not Available
Gene Name
pbp1b
Uniprot ID
Q7CRA4
Uniprot Name
Penicillin-binding protein 1b
Molecular Weight
89479.92 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [Article]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Penicillin binding
Gene Name
penA
Uniprot ID
P0A3M6
Uniprot Name
Penicillin-binding protein 2B
Molecular Weight
73872.305 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [Article]
  2. Ocheltree SM, Shen H, Hu Y, Xiang J, Keep RF, Smith DE: Mechanisms of cefadroxil uptake in the choroid plexus: studies in wild-type and PEPT2 knockout mice. J Pharmacol Exp Ther. 2004 Feb;308(2):462-7. Epub 2003 Nov 4. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
  1. Ganapathy ME, Brandsch M, Prasad PD, Ganapathy V, Leibach FH: Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2. J Biol Chem. 1995 Oct 27;270(43):25672-7. [Article]
  2. Wenzel U, Gebert I, Weintraut H, Weber WM, Clauss W, Daniel H: Transport characteristics of differently charged cephalosporin antibiotics in oocytes expressing the cloned intestinal peptide transporter PepT1 and in human intestinal Caco-2 cells. J Pharmacol Exp Ther. 1996 May;277(2):831-9. [Article]
  3. Balimane PV, Tamai I, Guo A, Nakanishi T, Kitada H, Leibach FH, Tsuji A, Sinko PJ: Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir. Biochem Biophys Res Commun. 1998 Sep 18;250(2):246-51. [Article]
  4. Guo A, Hu P, Balimane PV, Leibach FH, Sinko PJ: Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line. J Pharmacol Exp Ther. 1999 Apr;289(1):448-54. [Article]
  5. 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]
  6. 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]
  7. Tsuji A: Transporter-mediated Drug Interactions. Drug Metab Pharmacokinet. 2002;17(4):253-74. [Article]
  8. Tamai I, Nakanishi T, Hayashi K, Terao T, Sai Y, Shiraga T, Miyamoto K, Takeda E, Higashida H, Tsuji A: The predominant contribution of oligopeptide transporter PepT1 to intestinal absorption of beta-lactam antibiotics in the rat small intestine. J Pharm Pharmacol. 1997 Aug;49(8):796-801. [Article]
  9. Sala-Rabanal M, Loo DD, Hirayama BA, Turk E, Wright EM: Molecular interactions between dipeptides, drugs and the human intestinal H+ -oligopeptide cotransporter hPEPT1. J Physiol. 2006 Jul 1;574(Pt 1):149-66. Epub 2006 Apr 20. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
Molecular Weight
62751.08 Da
References
  1. Ganapathy ME, Huang W, Rajan DP, Carter AL, Sugawara M, Iseki K, Leibach FH, Ganapathy V: beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter. J Biol Chem. 2000 Jan 21;275(3):1699-707. [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
  1. Takeda M, Babu E, Narikawa S, Endou H: Interaction of human organic anion transporters with various cephalosporin antibiotics. Eur J Pharmacol. 2002 Mar 8;438(3):137-42. [Article]
  2. Jung KY, Takeda M, Shimoda M, Narikawa S, Tojo A, Kim DK, Chairoungdua A, Choi BK, Kusuhara H, Sugiyama Y, Sekine T, Endou H: Involvement of rat organic anion transporter 3 (rOAT3) in cephaloridine-induced nephrotoxicity: in comparison with rOAT1. Life Sci. 2002 Mar 8;70(16):1861-74. [Article]
  3. Jariyawat S, Sekine T, Takeda M, Apiwattanakul N, Kanai Y, Sophasan S, Endou H: The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1. J Pharmacol Exp Ther. 1999 Aug;290(2):672-7. [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
  1. Ganapathy ME, Brandsch M, Prasad PD, Ganapathy V, Leibach FH: Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2. J Biol Chem. 1995 Oct 27;270(43):25672-7. [Article]
  2. 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]
  3. 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]
  4. Ocheltree SM, Shen H, Hu Y, Xiang J, Keep RF, Smith DE: Mechanisms of cefadroxil uptake in the choroid plexus: studies in wild-type and PEPT2 knockout mice. J Pharmacol Exp Ther. 2004 Feb;308(2):462-7. Epub 2003 Nov 4. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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
  1. Takeda M, Babu E, Narikawa S, Endou H: Interaction of human organic anion transporters with various cephalosporin antibiotics. Eur J Pharmacol. 2002 Mar 8;438(3):137-42. [Article]
  2. Jung KY, Takeda M, Shimoda M, Narikawa S, Tojo A, Kim DK, Chairoungdua A, Choi BK, Kusuhara H, Sugiyama Y, Sekine T, Endou H: Involvement of rat organic anion transporter 3 (rOAT3) in cephaloridine-induced nephrotoxicity: in comparison with rOAT1. Life Sci. 2002 Mar 8;70(16):1861-74. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 22, 2021 23:18