Identification

Name
Cloxacillin
Accession Number
DB01147
Description

A semi-synthetic antibiotic that is a chlorinated derivative of oxacillin.

Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Thumb
Weight
Average: 435.881
Monoisotopic: 435.065569098
Chemical Formula
C19H18ClN3O5S
Synonyms
  • (2S,5R,6R)-6-({[3-(2-chlorophenyl)-5-methylisoxazol-4-yl]carbonyl}amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
  • (3-(o-chlorophenyl)-5-methyl-4-isoxazolyl)penicillin
  • 6-(3-(o-chlorophenyl)-5-methyl-4-isoxazolecarboxamido)penicillanic acid
  • Cloxacilina
  • Cloxacillin
  • Cloxacilline
  • Cloxacillinum

Pharmacology

Indication

Used to treat infections caused by penicillinase-producing staphylococci, including pneumococci, group A beta-hemolytic streptococci, and penicillin G-sensitive and penicillin G-resistant staphylococci.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Cloxacillin is a semisynthetic antibiotic in the same class as penicillin. Cloxacillin is for use against staphylococci that produce beta-lactamase.

Mechanism of action

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, cloxacillin inhibits 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 cloxacillin interferes with an autolysin inhibitor.

TargetActionsOrganism
APenicillin-binding protein 1A
inhibitor
Clostridium perfringens (strain 13 / Type A)
UBeta-lactamase
inducer
Escherichia coli (strain K12)
APenicillin-binding protein 2a
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
APenicillin-binding protein 2B
inhibitor
Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
APenicillin-binding protein 3
inhibitor
Pseudomonas aeruginosa
UD-alanyl-D-alanine carboxypeptidase DacA
inhibitor
Escherichia coli O6:H1 (strain CFT073 / ATCC 700928 / UPEC)
Absorption

Well absorbed from the gastrointestinal tract.

Volume of distribution
Not Available
Protein binding

95%

Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Oral LD50 in rat and mouse is 5000 mg/kg. Intravenous LD50 in rat is 1660 mg/kg. Symptoms of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, and swelling of face, lips, tongue, or throat.

Affected organisms
  • Enteric bacteria and other eubacteria
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
AcemetacinAcemetacin may decrease the excretion rate of Cloxacillin which could result in a higher serum level.
AcenocoumarolCloxacillin may increase the anticoagulant activities of Acenocoumarol.
AcyclovirThe excretion of Acyclovir can be decreased when combined with Cloxacillin.
Adefovir dipivoxilThe excretion of Adefovir dipivoxil can be decreased when combined with Cloxacillin.
AlprostadilThe excretion of Alprostadil can be decreased when combined with Cloxacillin.
AmikacinThe serum concentration of Amikacin can be decreased when it is combined with Cloxacillin.
Aminohippuric acidThe excretion of Aminohippuric acid can be decreased when combined with Cloxacillin.
AtracuriumThe therapeutic efficacy of Atracurium can be increased when used in combination with Cloxacillin.
Atracurium besylateThe therapeutic efficacy of Atracurium besylate can be increased when used in combination with Cloxacillin.
CapreomycinThe serum concentration of Capreomycin can be decreased when it is combined with Cloxacillin.
Additional Data Available
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    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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  • Action
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Food Interactions
  • Take on an empty stomach.

Products

Purchasing individual compounds or compound libraries for your research?
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Product Ingredients
IngredientUNIICASInChI Key
Cloxacillin benzathineAC79L7PV2G23736-58-5COCFKSXGORCFOW-VZHMHXRYSA-N
Cloxacillin sodiumMWQ645MKMF642-78-4SCLZRKVZRBKZCR-SLINCCQESA-M
Cloxacillin sodium hydrate65LCB00B4Y7081-44-9KCUWTKOTPIUBRI-VICXVTCVSA-M
International/Other Brands
Aclox (Southshourne) / Apo-Cloxi (Apotex) / Auropen Inj. (Cirin) / Cloxacil (Saiph) / Cloxam (MacroPhar) / Orbenin (GlaxoSmithKline) / Vaclox (Atlantic) / Vamcloxil (Vamsler)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CloxacillinCapsuleOralPro Doc Limitee1994-12-312013-07-15Canada flag
Cloxacillin for InjectionPowder, for solutionIntravenousSterimax Inc2011-07-28Not applicableCanada flag
Cloxacillin for InjectionPowder, for solutionIntravenousSterimax Inc2011-07-28Not applicableCanada flag
Cloxacillin for InjectionPowder, for solutionIntravenousSterimax Inc2013-04-03Not applicableCanada flag
Cloxacillin for InjectionPowder, for solutionIntramuscular; IntravenousSterimax Inc2011-09-14Not applicableCanada flag
Cloxacillin Sodium for InjectionPowder, for solutionIntramuscular; IntravenousTEVA Canada Limited1992-12-312017-12-01Canada flag
Cloxacillin Sodium for InjectionPowder, for solutionIntravenousTEVA Canada Limited1992-12-312017-12-01Canada flag
Cloxacillin Sodium for InjectionPowder, for solutionIntramuscular; IntravenousTEVA Canada Limited1992-12-312017-12-01Canada flag
Cloxacillin Sodium Sterile Inj 250mg/vialLiquidIntramuscular; IntravenousNovopharm Limited1992-12-312005-08-10Canada flag
Cloxacillin-250 CapCapsuleOralPro Doc Limitee1994-12-312009-07-23Canada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo Cloxi Cap 250mgCapsuleOralApotex Corporation1984-12-31Not applicableCanada flag
Apo Cloxi Cap 500mgCapsuleOralApotex Corporation1984-12-31Not applicableCanada flag
Apo Cloxi for Oral Soln 125mg/5mlPowder, for solutionOralApotex Corporation1985-12-312019-12-03Canada flag
Nu-cloxi Capsules 250mgCapsuleOralNu Pharm Inc1990-12-312012-09-04Canada flag
Nu-cloxi Capsules 500mgCapsuleOralNu Pharm Inc1990-12-312012-09-04Canada flag
Nu-cloxi Solution 125mg/5mlPowder, for solutionOralNu Pharm Inc1990-12-312012-09-04Canada flag
Riva-cloxacillin 250 Mg CapsulesCapsuleOralLaboratoire Riva Inc1999-11-192003-07-28Canada flag
Riva-cloxacillin 500 Mg CapsulesCapsuleOralLaboratoire Riva Inc1999-11-192003-07-28Canada flag
Taro-cloxacillin Cap 250mgCapsuleOralTaro Pharmaceuticals, Inc.1993-12-312000-08-31Canada flag
Taro-cloxacillin Cap 500mgCapsuleOralTaro Pharmaceuticals, Inc.1993-12-312000-08-31Canada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
J01CR50 — Combinations of penicillinsJ01CF02 — Cloxacillin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dipeptides. These are organic compounds containing a sequence of exactly two alpha-amino acids joined by a peptide bond.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Dipeptides
Alternative Parents
Penicillins / N-acyl-alpha amino acids and derivatives / Chlorobenzenes / Aryl chlorides / Thiazolidines / Tertiary carboxylic acid amides / Heteroaromatic compounds / Isoxazoles / Secondary carboxylic acid amides / Azetidines
show 12 more
Substituents
Alpha-amino acid or derivatives / Alpha-dipeptide / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Azetidine / Azole / Benzenoid / Beta-lactam
show 30 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
penicillin (CHEBI:49566)

Chemical Identifiers

UNII
O6X5QGC2VB
CAS number
61-72-3
InChI Key
LQOLIRLGBULYKD-JKIFEVAISA-N
InChI
InChI=1S/C19H18ClN3O5S/c1-8-11(12(22-28-8)9-6-4-5-7-10(9)20)15(24)21-13-16(25)23-14(18(26)27)19(2,3)29-17(13)23/h4-7,13-14,17H,1-3H3,(H,21,24)(H,26,27)/t13-,14+,17-/m1/s1
IUPAC Name
(2S,5R,6R)-6-[3-(2-chlorophenyl)-5-methyl-1,2-oxazole-4-amido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
SMILES
[H][[email protected]]12SC(C)(C)[[email protected]@H](N1C(=O)[[email protected]]2NC(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl)C(O)=O

References

Synthesis Reference

Doyle, F.P. and Nayler, J.H.C.; British Patent 905,778; September 12, 1962; assigned to Beecham Research Laboratories, Ltd. Doyle, F.P. and Nayler, J.H.C.; US. Patent 2,996,501; August 15, 1961.

General References
Not Available
Human Metabolome Database
HMDB0015278
KEGG Compound
C06923
PubChem Compound
6098
PubChem Substance
46507109
ChemSpider
5873
BindingDB
50022788
RxNav
2625
ChEBI
49566
ChEMBL
CHEMBL891
ZINC
ZINC000003875417
Therapeutic Targets Database
DAP001161
PharmGKB
PA449059
PDBe Ligand
CXN
Drugs.com
Drugs.com Drug Page
Wikipedia
Cloxacillin
AHFS Codes
  • 08:12.16.12 — Penicillinase-resistant Penicillins
  • 08:12.16 — Penicillins
MSDS
Download (38 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentSkin Diseases, Infectious1
4RecruitingTreatmentAbscesses / CNS Infection / Coagulase Negative Staphylococcal Infection / Diabetic Foot Infection / Infection caused by staphylococci / Osteomyelitis / Septic Arthritis / Vertebral Osteomyelitis1
4TerminatedTreatmentImpaired kidney function / S. Aureus Bacteremia / Skin and Subcutaneous Tissue Bacterial Infections1
4Unknown StatusTreatmentInfection caused by staphylococci / Prosthesis-Related Infections1
3CompletedTreatmentInfection1
3CompletedTreatmentStaphylococcus Aureus Infections1
3TerminatedTreatmentBacteremia1
3TerminatedTreatmentMethicillin-Resistant Staphylococcus Aureus (MRSA)1
3TerminatedTreatmentStaphylococcus1
2CompletedTreatmentBacteremia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Apothecon
  • Dispensing Solutions
  • H.J. Harkins Co. Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
Capsule250 mg
CapsuleOral250 mg
Powder; syrupOral250 mg/5mL
Powder, for suspensionOral25 mg/mL
Powder, for solutionIntramuscular; Intravenous
Powder, for solutionIntravenous
LiquidIntramuscular; Intravenous
Powder; syrupOral125 mg/5mL
Tablet, coatedOral500 mg
Injection, powder, for solution250 mg
Injection, powder, for solution1 g
Powder, for suspensionOral125 mg
Injection, powder, for solution500 mg
CapsuleOral500 MG
Injection, powder, for solution
Injection250 mg
Injection500 mg
CapsuleOral
Powder, for solutionOral
Granule, for suspensionOral25 mg/mL
Granule, for solutionOral
Prices
Unit descriptionCostUnit
Cloxacillin Sodium 2 g/vial7.69USD vial
Cloxacillin Sodium 1 g/vial5.89USD vial
Cloxacillin Sodium 500 mg/vial4.79USD vial
Apo-Cloxi 500 mg Capsule0.38USD capsule
Novo-Cloxin 500 mg Capsule0.38USD capsule
Nu-Cloxi 500 mg Capsule0.38USD capsule
Apo-Cloxi 250 mg Capsule0.19USD capsule
Novo-Cloxin 250 mg Capsule0.19USD capsule
Nu-Cloxi 250 mg Capsule0.19USD capsule
Apo-Cloxi 25 mg/ml Liquid0.05USD ml
Novo-Cloxin 25 mg/ml Liquid0.05USD ml
Nu-Cloxi 25 mg/ml Liquid0.05USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility13.9 mg/LNot Available
logP2.48SANGSTER (1994)
pKa2.78SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0532 mg/mLALOGPS
logP2.61ALOGPS
logP2.3ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)3.75ChemAxon
pKa (Strongest Basic)-0.41ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area112.74 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity106.64 m3·mol-1ChemAxon
Polarizability41.64 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.8368
Blood Brain Barrier-0.9903
Caco-2 permeable-0.8957
P-glycoprotein substrateNon-substrate0.6204
P-glycoprotein inhibitor INon-inhibitor0.8951
P-glycoprotein inhibitor IINon-inhibitor0.9204
Renal organic cation transporterNon-inhibitor0.9629
CYP450 2C9 substrateNon-substrate0.8262
CYP450 2D6 substrateNon-substrate0.905
CYP450 3A4 substrateSubstrate0.5977
CYP450 1A2 substrateInhibitor0.8592
CYP450 2C9 inhibitorNon-inhibitor0.891
CYP450 2D6 inhibitorNon-inhibitor0.918
CYP450 2C19 inhibitorNon-inhibitor0.8832
CYP450 3A4 inhibitorNon-inhibitor0.819
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9186
Ames testNon AMES toxic0.6979
CarcinogenicityCarcinogens 0.5672
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9946 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9996
hERG inhibition (predictor II)Non-inhibitor0.8486
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a5a-0560910000-05dcf2cead0bc1f49482
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01q9-1900000000-a2a9637ec3640b22d439

Targets

Kind
Protein
Organism
Clostridium perfringens (strain 13 / Type A)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transferase activity, transferring glycosyl groups
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
pbpA
Uniprot ID
Q8XJ01
Uniprot Name
Penicillin-binding protein 1A
Molecular Weight
75176.35 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Kleppe G, Yu W, Strominger JL: Penicillin-binding proteins in Bacillus subtilis mutants. Antimicrob Agents Chemother. 1982 Jun;21(6):979-83. [PubMed:6810758]
Kind
Protein
Organism
Escherichia coli (strain K12)
Pharmacological action
Unknown
Actions
Inducer
General Function
Beta-lactamase activity
Specific Function
This protein is a serine beta-lactamase with a substrate specificity for cephalosporins.
Gene Name
ampC
Uniprot ID
P00811
Uniprot Name
Beta-lactamase
Molecular Weight
41555.3 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Mirelis B, Rivera A, Miro E, Mesa RJ, Navarro F, Coll P: A simple phenotypic method for differentiation between acquired and chromosomal AmpC beta-lactamases in Escherichia coli. Enferm Infecc Microbiol Clin. 2006 Jun-Jul;24(6):370-2. [PubMed:16792938]
  4. Ruppe E, Bidet P, Verdet C, Arlet G, Bingen E: First detection of the Ambler class C 1 AmpC beta-lactamase in Citrobacter freundii by a new, simple double-disk synergy test. J Clin Microbiol. 2006 Nov;44(11):4204-7. Epub 2006 Sep 13. [PubMed:16971653]
  5. Guan XZ, Liu YN, Luo YP, She DY, Zhou G, Chen LA, Xu YP: [A new member of CMY type cephalosporinase prevailing in Escherichia coli]. Zhonghua Yi Xue Za Zhi. 2004 Nov 17;84(22):1872-5. [PubMed:15631796]
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
pbp2a
Uniprot ID
Q8DNB6
Uniprot Name
Penicillin-binding protein 2a
Molecular Weight
80797.94 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. [PubMed:7447421]
Kind
Protein
Organism
Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Penicillin binding
Specific Function
Not Available
Gene Name
penA
Uniprot ID
P0A3M5
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. [PubMed:7447421]
Kind
Protein
Organism
Pseudomonas aeruginosa
Pharmacological action
Yes
Actions
Inhibitor
General Function
Peptidoglycan glycosyltransferase activity
Specific Function
Not Available
Gene Name
pbpB
Uniprot ID
Q51504
Uniprot Name
Cell division protein
Molecular Weight
62855.78 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. [PubMed:7447421]
Kind
Protein
Organism
Escherichia coli O6:H1 (strain CFT073 / ATCC 700928 / UPEC)
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Removes C-terminal D-alanyl residues from sugar-peptide cell wall precursors.
Specific Function
Serine-type d-ala-d-ala carboxypeptidase activity
Gene Name
dacA
Uniprot ID
P0AEB3
Uniprot Name
D-alanyl-D-alanine carboxypeptidase DacA
Molecular Weight
44443.62 Da
References
  1. Nicola G, Tomberg J, Pratt RF, Nicholas RA, Davies C: Crystal structures of covalent complexes of beta-lactam antibiotics with Escherichia coli penicillin-binding protein 5: toward an understanding of antibiotic specificity. Biochemistry. 2010 Sep 21;49(37):8094-104. doi: 10.1021/bi100879m. [PubMed:20726582]

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
References
  1. Bratlid D, Bergan T: Displacement of albumin-bound antimicrobial agents by bilirubin. Pharmacology. 1976;14(5):464-72. [PubMed:1031216]
  2. Friedman LA, Lewis PJ: The effect of semisynthetic penicillins on the binding of bilirubin by neonatal serum. Br J Clin Pharmacol. 1980 Jan;9(1):61-5. [PubMed:7356894]
  3. Okore VC: Effect of ascorbic acid on the binding of cloxacillin sodium to bovine serum albumin. Arzneimittelforschung. 1994 May;44(5):671-3. [PubMed:8024646]

Transporters

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
  1. 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. [PubMed:15567297]
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. 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. [PubMed:15567297]
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. 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. [PubMed:10411577]

Drug created on June 13, 2005 07:24 / Updated on November 30, 2020 13:38

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