Cefixime

Identification

Summary

Cefixime is a third generation cephalosporin used to treat susceptible Gram negative and Gram positive bacterial infections.

Brand Names
Suprax
Generic Name
Cefixime
DrugBank Accession Number
DB00671
Background

Cefixime, an antibiotic, is a third-generation cephalosporin like ceftriaxone and cefotaxime. Cefixime is highly stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases, may be susceptible to cefixime. The antibacterial effect of cefixime results from inhibition of mucopeptide synthesis in the bacterial cell wall.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 453.45
Monoisotopic: 453.041289239
Chemical Formula
C16H15N5O7S2
Synonyms
  • (−)-cefixim
  • Cefixim
  • Cefixima
  • Céfixime
  • Cefixime
  • Cefixime anhydrous
  • Cefiximum
External IDs
  • FK 027
  • FR 17027

Pharmacology

Indication

For use in the treatment of the following infections when caused by susceptible strains of the designated microorganisms: (1) uncomplicated urinary tract infections caused by Escherichia coli and Proteus mirabilis, (2) otitis media caused by Haemophilus influenzae (beta-lactamase positive and negative strains), Moraxella catarrhalis (most of which are beta-lactamase positive), and S. pyogenes, (3) pharyngitis and tonsillitis caused by S. pyogenes, (4) acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae and Haemophilus influenzae (beta-lactamase positive and negative strains), and (5) uncomplicated gonorrhea (cervical/urethral) caused by Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains).

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Cefixime, an antibiotic, is a third-generation cephalosporin like ceftriaxone and cefotaxime. Cefixime is highly stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases, may be susceptible to cefixime. The antibacterial effect of cefixime results from inhibition of mucopeptide synthesis in the bacterial cell wall.

Mechanism of action

Like all beta-lactam antibiotics, cefixime 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 cefixime interferes with an autolysin inhibitor.

TargetActionsOrganism
APenicillin-binding protein 2
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Absorption

About 40%-50% absorbed orally whether administered with or without food, however, time to maximal absorption is increased approximately 0.8 hours when administered with food.

Volume of distribution

Not Available

Protein binding

65% (concentration independent)

Metabolism

Hepatic. Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours.

Route of elimination

Not Available

Half-life

3-4 hours (may range up to 9 hours). In severe renal impairment (5 to 20 mL/min creatinine clearance), the half-life increased to an average of 11.5 hours.

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting.

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
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Cefixime.
AcenocoumarolThe risk or severity of bleeding can be increased when Cefixime is combined with Acenocoumarol.
AlteplaseThe therapeutic efficacy of Alteplase can be decreased when used in combination with Cefixime.
AncrodThe therapeutic efficacy of Ancrod can be decreased when used in combination with Cefixime.
AnistreplaseThe therapeutic efficacy of Anistreplase can be decreased when used in combination with Cefixime.
Antithrombin AlfaThe therapeutic efficacy of Antithrombin Alfa can be decreased when used in combination with Cefixime.
Antithrombin III humanThe therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Cefixime.
ApixabanThe therapeutic efficacy of Apixaban can be decreased when used in combination with Cefixime.
ArdeparinThe therapeutic efficacy of Ardeparin can be decreased when used in combination with Cefixime.
ArgatrobanThe therapeutic efficacy of Argatroban can be decreased when used in combination with Cefixime.
Interactions
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Food Interactions
  • Take with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Cefixime trihydrate97I1C92E55125110-14-7IPYWNMVPZOAFOQ-NABDTECSSA-N
Product Images
International/Other Brands
Cefixoral (Menarini) / Cefspan (GlaxoSmithKline) / Cephoral (Merck) / Fixam (Solas) / Fixspor (Invision) / Hifen (Hetero) / InfectoOpticef (Infectopharm) / Kuracef (Sanofi-Aventis) / Letix (Adley) / Ofex (Delta) / Omnatax-O (Abbott) / Oracef (Micro Labs) / Oroken (Sanofi Aventis) / Sancefix (Sandoz) / Secef (Novartis) / Supran (Teva) / Suprax 125 (Lupin) / Tricef (Merck) / Unixime (Firma) / Uro-Cephoral (Merck)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
SupraxPowder, for suspension500 mg/5mLOralLupin Pharmaceuticals, Inc.2013-03-15Not applicableUS flag
SupraxCapsule400 mg/1OralLUPIN LIMITED2013-03-152018-12-03US flag
SupraxTablet400 mgOralOdan Laboratories Ltd1990-12-31Not applicableCanada flag
SupraxCapsule400 mg/1OralPD-Rx Pharmaceuticals, Inc.2013-03-15Not applicableUS flag
SupraxPowder, for suspension500 mg/5mLOralLUPIN LIMITED2013-03-152018-12-03US flag
SupraxCapsule400 mg/1OralLupin Pharmaceuticals, Inc.2013-03-15Not applicableUS flag
SupraxCapsule400 mg/1OralREMEDYREPACK INC.2019-04-092020-06-02US flag
SupraxPowder, for suspension100 mg / 5 mLOralOdan Laboratories Ltd1990-12-31Not applicableCanada flag
SupraxPowder, for solution100 mg / 5 mLOralAventis Pharma Ltd.1990-12-312005-12-07Canada flag
SupraxCapsule400 mg/1OralDenton Pharma, Inc. Dba Northwind Pharmaceuticals2018-02-09Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Auro-cefiximePowder, for suspension100 mg / 5 mLOralAuro Pharma Inc2018-01-08Not applicableCanada flag
Auro-cefiximeTablet400 mgOralAuro Pharma Inc2014-10-24Not applicableCanada flag
CefiximeCapsule400 mg/1OralLupin Pharmaceuticals, Inc.2020-10-14Not applicableUS flag
CefiximePowder, for suspension200 mg/5mLOralBelcher Pharmaceuticals,LLC2017-03-15Not applicableUS flag
CefiximePowder, for suspension200 mg/5mLOralLupin Pharmaceuticals, Inc.2015-04-24Not applicableUS flag
CefiximePowder, for suspension200 mg/5mLOralNorthstar RxLLC2018-05-11Not applicableUS flag
CefiximePowder, for suspension200 mg/5mLOralDr. Reddy’s Laboratories, Inc2017-08-03Not applicableUS flag
CefiximeCapsule400 mg/1OralAscend Laboratories, LLC2018-10-12Not applicableUS flag
CefiximePowder, for suspension200 mg/5mLOralAurobindo Pharma Limited2015-04-14Not applicableUS flag
CefiximePowder, for suspension100 mg/5mLOralBelcher Pharmaceuticals,LLC2017-03-15Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
INNOCEF PLUS 100/62.5 MG SASE, 20 ADETCefixime trihydrate (111.9 mg) + Clavulanate potassium (62.5 mg)PowderOralVİTALİS İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
INNOCEF PLUS 200/125 MG SAŞE, 20 ADETCefixime trihydrate (223.8 mg) + Clavulanate potassium (125 mg)PowderOralVİTALİS İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
INNOCEF PLUS 200/62.5 MG SASE, 20 ADETCefixime trihydrate (223.8 mg) + Clavulanate potassium (62.5 mg)PowderOralVİTALİS İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
INNOCEF PLUS 400/125 MG SAŞE, 10 ADETCefixime trihydrate (447.63 mg) + Clavulanate potassium (125 mg)PowderOralVİTALİS İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
INNOCEF PLUS 400/125 MG SAŞE, 20 ADETCefixime trihydrate (447.63 mg) + Clavulanate potassium (125 mg)PowderOralVİTALİS İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
MOLCEF 200 MG/62.5/5 ML ORAL SÜSPANSİYON HAZIRLAMAK İÇİN KURU TOZ, 100 MLCefixime (200 mg/5ml) + Clavulanic acid (62.5 mg/5ml)SuspensionOralNEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
MOLCEF PLUS 100/62.5 MG FILM KAPLI TABLET, 20 ADETCefixime (100 mg) + Clavulanic acid (62.5 mg)Tablet, coatedOralNEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
MOLCEF PLUS 100/62.5/5 ML ORAL SUSPANSIYON HAZIRLAMAK ICIN KURU TOZ, 100 MLCefixime (100 mg/5ml) + Clavulanic acid (62.5 mg/5ml)SuspensionOralNEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
MOLCEF PLUS 200/125 MG FILM KAPLI TABLET, 20 ADETCefixime (200 mg) + Clavulanic acid (125 mg)Tablet, coatedOralNEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
MOLCEF PLUS 400/125 MG FILM KAPLI TABLET, 10 ADETCefixime (400 mg) + Clavulanic acid (125 mg)Tablet, coatedOralNEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag

Categories

ATC Codes
J01DD08 — Cefixime
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 / 2,4-disubstituted thiazoles / 1,3-thiazines / 2-amino-1,3-thiazoles / Dicarboxylic acids and derivatives / Tertiary carboxylic acid amides / Heteroaromatic compounds / Secondary carboxylic acid amides / Amino acids / Azetidines
show 9 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 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
cephalosporin (CHEBI:472657)
Affected organisms
  • Enteric bacteria and other eubacteria

Chemical Identifiers

UNII
XZ7BG04GJX
CAS number
79350-37-1
InChI Key
OKBVVJOGVLARMR-QSWIMTSFSA-N
InChI
InChI=1S/C16H15N5O7S2/c1-2-6-4-29-14-10(13(25)21(14)11(6)15(26)27)19-12(24)9(20-28-3-8(22)23)7-5-30-16(17)18-7/h2,5,10,14H,1,3-4H2,(H2,17,18)(H,19,24)(H,22,23)(H,26,27)/b20-9-/t10-,14-/m1/s1
IUPAC Name
(6R,7R)-7-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(carboxymethoxy)imino]acetamido]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
SMILES
[H][C@]12SCC(C=C)=C(N1C(=O)[C@H]2NC(=O)C(=N/OCC(O)=O)\C1=CSC(N)=N1)C(O)=O

References

Synthesis Reference

Pandurang Deshpande, "Process for the preparation of cefixime." U.S. Patent US20040082560, issued April 29, 2004.

US20040082560
General References
  1. McMillan A, Young H: The treatment of pharyngeal gonorrhoea with a single oral dose of cefixime. Int J STD AIDS. 2007 Apr;18(4):253-4. [Article]
  2. Adam D, Hostalek U, Troster K: 5-day cefixime therapy for bacterial pharyngitis and/or tonsillitis: comparison with 10-day penicillin V therapy. Cefixime Study Group. Infection. 1995;23 Suppl 2:S83-6. [Article]
Human Metabolome Database
HMDB0014809
KEGG Drug
D00258
KEGG Compound
C06881
PubChem Compound
5362065
PubChem Substance
46508684
ChemSpider
4514923
BindingDB
84007
RxNav
25033
ChEBI
472657
ChEMBL
CHEMBL1541
ZINC
ZINC000004468778
Therapeutic Targets Database
DAP000439
PharmGKB
PA164768821
PDBe Ligand
C04
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Cefixime
PDB Entries
4kou
FDA label
Download (3.07 MB)
MSDS
Download (43.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedHealth Services ResearchAntibiotic Resistant Infection / Uncomplicated Urinary Tract Infections1
4Not Yet RecruitingTreatmentSalmonella Typhi Infection1
4Unknown StatusTreatmentSalmonella Typhi Infection1
3Active Not RecruitingPreventionChronic Kidney Disease (CKD) / Renal Hypodysplasia, Nonsyndromic, 1 / Vesicoureteral Reflux (VUR)1
3Not Yet RecruitingTreatmentHepatic abscess1
3RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections / Syphilis1
3TerminatedTreatmentBacterial Vaginitis / Cervicitis1
2CompletedTreatmentUrinary Tract Infection1
2RecruitingTreatmentEarly Syphilis / Syphilis1
2, 3CompletedTreatmentAcute Exacerbation of Chronic Obstructive Pulmonary Disease1

Pharmacoeconomics

Manufacturers
  • Lederle laboratories div american cyanamid co
  • Lupin pharmaceuticals inc
  • Lupin ltd
Packagers
  • A-S Medication Solutions LLC
  • Dept Health Central Pharmacy
  • Dispensing Solutions
  • Lupin Pharmaceuticals Inc.
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Redpharm Drug
  • Remedy Repack
Dosage Forms
FormRouteStrength
Tablet, coatedOral
Capsule, coatedOral400 mg
PowderParenteral100 MG/5ML
Tablet, film coatedOral200 MG
Granule, for suspensionOral
TabletOral200 mg
SyrupOral2 g
TabletOral400 mg
Powder, for suspensionOral
Powder, for suspensionOral100 mg/5mL
Powder, for suspensionOral200 mg/5mL
Powder, for suspensionOral1 g
SuspensionOral
CapsuleOral
Powder, for suspensionOral2 g
GranuleOral100 mg
SyrupOral100 MG/5ML
Solution / drops; suspension / drops
Tablet, orally disintegratingOral
GranuleOral
Tablet, film coatedOral
GranuleOral100 MG/5ML
PowderOral
PowderOral
SuspensionOral
Tablet, coatedOral
CapsuleOral100 MG
CapsuleOral200 MG
Tablet, effervescent
SyrupOral
Powder, for suspensionOral
Granule, for suspensionOral100 MG/5ML
SuspensionOral100 MG/5ML
Tablet, coatedOral400 MG
Tablet, for suspensionOral400 MG
CapsuleOral400 mg/1
Granule, for suspensionOral2 g/100ml
Powder, for solutionOral100 mg / 5 mL
Powder, for suspensionOral100 mg / 5 mL
Powder, for suspensionOral500 mg/5mL
TabletOral400 mg/1
Tablet, chewableOral100 mg/1
Tablet, chewableOral200 mg/1
Tablet, coatedOral200 MG
TabletOral200 mg / tab
Tablet, film coatedOral400 mg
Capsule, coatedOral52.5 mg
Powder, for solutionOral
TabletOral
Prices
Unit descriptionCostUnit
Suprax 400 mg Tablet3.86USD tablet
Suprax 100 mg/5ml Suspension2.8USD ml
Suprax 20 mg/ml Suspension0.45USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9233112No2016-01-122028-12-14US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)218-225 °CNot Available
water solubility55.11 mg/LNot Available
logP-0.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.104 mg/mLALOGPS
logP0.25ALOGPS
logP-1.2ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)3.45ChemAxon
pKa (Strongest Basic)2.92ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area184.51 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity104.91 m3·mol-1ChemAxon
Polarizability41.62 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.7776
Blood Brain Barrier-0.9704
Caco-2 permeable-0.7432
P-glycoprotein substrateSubstrate0.6934
P-glycoprotein inhibitor INon-inhibitor0.8863
P-glycoprotein inhibitor IINon-inhibitor0.8724
Renal organic cation transporterNon-inhibitor0.8301
CYP450 2C9 substrateNon-substrate0.9002
CYP450 2D6 substrateNon-substrate0.8161
CYP450 3A4 substrateNon-substrate0.5
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9029
Ames testNon AMES toxic0.7495
CarcinogenicityNon-carcinogens0.8549
BiodegradationNot ready biodegradable0.9911
Rat acute toxicity1.6878 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9897
hERG inhibition (predictor II)Non-inhibitor0.895
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-3920000000-3269e737530417831893

Targets

Drugtargets2
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Learn more
Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Penicillin binding
Specific Function
Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. Its synthesize cross-linked peptidoglycan from the lipid intermediates (By similarity).
Gene Name
mrdA
Uniprot ID
P44469
Uniprot Name
Penicillin-binding protein 2
Molecular Weight
73812.47 Da
References
  1. Takahata S, Senju N, Osaki Y, Yoshida T, Ida T: Amino acid substitutions in mosaic penicillin-binding protein 2 associated with reduced susceptibility to cefixime in clinical isolates of Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2006 Nov;50(11):3638-45. Epub 2006 Aug 28. [Article]
  2. Zhao S, Duncan M, Tomberg J, Davies C, Unemo M, Nicholas RA: Genetics of chromosomally mediated intermediate resistance to ceftriaxone and cefixime in Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2009 Sep;53(9):3744-51. doi: 10.1128/AAC.00304-09. Epub 2009 Jun 15. [Article]

Transporters

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
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. 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]
  2. 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]
  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. 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]
  5. 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]
  6. Tsuji A: Transporter-mediated Drug Interactions. Drug Metab Pharmacokinet. 2002;17(4):253-74. [Article]
  7. 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]
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, 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]
  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]
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Drug created on June 13, 2005 13:24 / Updated on September 28, 2021 07:54