Cefaclor
Identification
- Summary
Cefaclor is a second generation cephalosporin used to treat a wide variety of infections in the body.
- Generic Name
- Cefaclor
- DrugBank Accession Number
- DB00833
- Background
Semisynthetic, broad-spectrum antibiotic derivative of cephalexin.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 367.807
Monoisotopic: 367.039354348 - Chemical Formula
- C15H14ClN3O4S
- Synonyms
- 3-Chloro-7-D-(2-phenylglycinamido)-3-cephem-4-carboxylic acid
- CCL
- Cefaclor
- Céfaclor
- Cefaclor anhydrous
- Cefaclorum
- Céfeaclor
- Cephaclor
- External IDs
- Compound 99638
- S 6472
Pharmacology
- Indication
For the treatment of certain infections caused by bacteria such as pneumonia and ear, lung, skin, throat, and urinary tract infections.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute exacerbation of chronic bronchitis caused by streptococcus pneumoniae •••••••••••• ••••••• •••• ••••••• •••••••• ••••••• Treatment of Acute exacerbations of chronic bronchitis caused by haemophilus influenza •••••••••••• ••••••• •••• ••••••• •••••••• ••••••• Treatment of Acute exacerbations of chronic bronchitis caused by moraxella catarrhalis •••••••••••• ••••••• •••• ••••••• •••••••• ••••••• Treatment of Bacterial infections •••••••••••• Treatment of Lower respiratory tract infection bacterial •••••••••••• •••••••• •••••••••• - 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
Cefaclor is a second generation cephalosporin antibiotic with a spectrum resembling first-generation cephalosporins. In vitro tests demonstrate that the bactericidal action of the cephalosporins results from inhibition of cell-wall synthesis. As indicated by in vitro and in vivo clinical studies, cefaclor was shown to be effective against most strains of Gram positive aerobes - Staphylococci (including coagulase-positive, coagulase-negative, and penicillinase-producing strains), Streptococcus pneumoniae, Streptococcus pyogenes (group A ß-hemolytic streptococci), as well as Gram-negative aerobes - Escherichia coli, Haemophilus influenzae (including ß-lactamase-producing ampicillin-resistant strains), Klebsiella sp, and Proteus mirabilis.
- Mechanism of action
Cefaclor, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it 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 cefaclor interferes with an autolysin inhibitor.
Target Actions Organism APenicillin-binding protein 3 inhibitorStreptococcus pneumoniae APenicillin-binding protein 1A inhibitorClostridium perfringens (strain 13 / Type A) - Absorption
Well absorbed after oral administration, independent of food intake.
- Volume of distribution
Not Available
- Protein binding
23.5%
- Metabolism
No appreciable biotransformation in liver (approximately 60% to 85% of the drug is excreted unchanged in the urine within 8 hours).
- Route of elimination
Approximately 60% to 85% of the drug is excreted unchanged in the urine within 8 hours, the greater portion being excreted within the first 2 hours.
- Half-life
0.6-0.9 hour
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Symptoms of overdose include diarrhea, nausea, stomach upset, and vomiting.
- 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 Cefaclor 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 Cefaclor. Acamprosate The excretion of Acamprosate can be decreased when combined with Cefaclor. Aceclofenac The risk or severity of nephrotoxicity can be increased when Cefaclor is combined with Aceclofenac. Acemetacin The risk or severity of nephrotoxicity can be increased when Cefaclor is combined with Acemetacin. - Food Interactions
- Take with or without food.
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 Cefaclor monohydrate 69K7K19H4L 70356-03-5 WKJGTOYAEQDNIA-IOOZKYRYSA-N - Product Images
- International/Other Brands
- Alenfral (Choseido Pharmaceutical) / Alfacet (Galenika) / Alfatil (Dexo) / Alfatil LP (Dexo) / Ceclor CD (Lilly) / Distaclor (Flynn) / Keflor (Alphapharm) / Kefral (Shionogi Seiyaku) / Panacef (Valeas) / Panoral (Eberth) / Raniclor (Ranbaxy Pharmaceuticals Inc.)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ceclor Powder, for suspension 250 mg / 5 mL Oral Pendopharm Division Of Pharmascience Inc 1980-12-31 2016-10-25 Canada Ceclor Capsule 250 mg Oral Pendopharm Division Of Pharmascience Inc 1980-12-31 2016-10-25 Canada Ceclor Powder, for suspension 125 mg / 5 mL Oral Pendopharm Division Of Pharmascience Inc 1980-12-31 2016-10-25 Canada Ceclor Powder, for suspension 375 mg / 5 mL Oral Pendopharm Division Of Pharmascience Inc 1990-12-31 2016-10-25 Canada Ceclor Capsule 500 mg Oral Pendopharm Division Of Pharmascience Inc 1980-12-31 2016-10-25 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-cefaclor Powder 375 mg / 5 mL Oral Apotex Corporation 1998-03-06 2019-01-16 Canada Apo-cefaclor Capsule 500 mg Oral Apotex Corporation 1997-01-20 2019-12-02 Canada Apo-cefaclor Powder 250 mg / 5 mL Oral Apotex Corporation 1998-03-06 2019-01-16 Canada Apo-cefaclor Capsule 250 mg Oral Apotex Corporation 1997-01-20 2019-12-02 Canada Apo-cefaclor Powder 125 mg / 5 mL Oral Apotex Corporation 1998-03-06 2019-01-16 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image SEFKLAV 1000/125 MG EFERVESAN TABLET, 20 ADET Cefaclor (500 mg) + Clavulanic acid (125 mg) Tablet, effervescent Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-12-07 Not applicable Turkey SEFKLAV 250/62.5 MG EFERVESAN TABLET, 20 ADET Cefaclor (250 mg) + Clavulanic acid (62.5 mg) Tablet, effervescent Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-12-07 Not applicable Turkey SEFKLAV 500/125 MG EFERVESAN TABLET, 20 ADET Cefaclor (500 mg) + Clavulanic acid (125 mg) Tablet, effervescent Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-12-07 Not applicable Turkey
Categories
- ATC Codes
- J01DC04 — Cefaclor
- Drug Categories
- Amides
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antiinfectives for Systemic Use
- beta-Lactams
- BSEP/ABCB11 Substrates
- Cephalosporins
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Lactams
- Nephrotoxic agents
- OAT3/SLC22A8 Inhibitors
- OAT3/SLC22A8 Substrates
- Second-Generation Cephalosporins
- Sulfur Compounds
- Thiazines
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as n-acyl-alpha amino acids and derivatives. These are compounds containing an alpha amino acid (or a derivative thereof) which bears an acyl group at its terminal nitrogen atom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- N-acyl-alpha amino acids and derivatives
- Alternative Parents
- Cephems / Aralkylamines / 1,3-thiazines / Benzene and substituted derivatives / Vinylogous halides / Tertiary carboxylic acid amides / Amino acids / Azetidines / Vinyl chlorides / Thiohemiaminal derivatives show 13 more
- Substituents
- Amine / Amino acid / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Azetidine / Benzenoid / Beta-lactam / Carbonyl group / Carboxamide group show 32 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- cephalosporin (CHEBI:3478)
- Affected organisms
- Enteric bacteria and other eubacteria
Chemical Identifiers
- UNII
- 3Z6FS3IK0K
- CAS number
- 53994-73-3
- InChI Key
- QYIYFLOTGYLRGG-GPCCPHFNSA-N
- InChI
- InChI=1S/C15H14ClN3O4S/c16-8-6-24-14-10(13(21)19(14)11(8)15(22)23)18-12(20)9(17)7-4-2-1-3-5-7/h1-5,9-10,14H,6,17H2,(H,18,20)(H,22,23)/t9-,10-,14-/m1/s1
- IUPAC Name
- (6R,7R)-7-[(2R)-2-amino-2-phenylacetamido]-3-chloro-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
- SMILES
- [H][C@]12SCC(Cl)=C(N1C(=O)[C@H]2NC(=O)[C@H](N)C1=CC=CC=C1)C(O)=O
References
- Synthesis Reference
Bing L. Wong, Yong-Qiang Shen, Yung-Pin Chen, "Enzymatic production of cefaclor from cephalexin." U.S. Patent US5939299, issued November, 1987.
US5939299- General References
- Hebert AA, Sigman ES, Levy ML: Serum sickness-like reactions from cefaclor in children. J Am Acad Dermatol. 1991 Nov;25(5 Pt 1):805-8. [Article]
- Parra FM, Igea JM, Martin JA, Alonso MD, Lezaun A, Sainz T: Serum sickness-like syndrome associated with cefaclor therapy. Allergy. 1992 Aug;47(4 Pt 2):439-40. [Article]
- External Links
- Human Metabolome Database
- HMDB0014971
- KEGG Drug
- D00256
- KEGG Compound
- C06877
- PubChem Compound
- 51039
- PubChem Substance
- 46507693
- ChemSpider
- 46260
- BindingDB
- 42131
- 1450910
- ChEBI
- 3478
- ChEMBL
- CHEMBL680
- ZINC
- ZINC000003812869
- Therapeutic Targets Database
- DAP000442
- PharmGKB
- PA164749137
- PDBe Ligand
- 8XI
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cefaclor
- PDB Entries
- 7q4x
- FDA label
- Download (186 KB)
- MSDS
- Download (43.9 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Infective Endocarditis (IE) 1 0 Terminated Treatment Osteomyelitis 1 Not Available Completed Treatment Snoring / Strep Throat 1 Not Available Recruiting Prevention Antibacterial therapy / Biliary Atresia / Cholangitis 1
Pharmacoeconomics
- Manufacturers
- Eli lilly and co
- Ceph international corp
- Clonmel healthcare ltd
- Hikma pharmaceuticals
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Marsam pharmaceuticals llc
- Ranbaxy pharmaceuticals inc
- Teva pharmaceuticals usa inc
- Yung shin pharmaceutical industrial co ltd
- Acs dobfar info sa
- Ranbaxy laboratories ltd
- World gen llc
- Packagers
- Advanced Pharmaceutical Services Inc.
- Aidarex Pharmacuticals LLC
- Alvogen Inc.
- Apothecon
- A-S Medication Solutions LLC
- Bryant Ranch Prepack
- C.O. Truxton Inc.
- Carlsbad Technology Inc.
- Corepharma LLC
- DAVA Pharmaceuticals
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Eli Lilly & Co.
- H.J. Harkins Co. Inc.
- Ivax Pharmaceuticals
- Jazeera Pharmaceutical Industries
- Lake Erie Medical and Surgical Supply
- Lilly Del Caribe Inc.
- Major Pharmaceuticals
- Novopharm Ltd.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- Patheon Inc.
- PD-Rx Pharmaceuticals Inc.
- PEDiNOL
- Pharma Pac LLC
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Qualitest
- Ranbaxy Laboratories
- Rebel Distributors Corp.
- Redpharm Drug
- Southwood Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- West-Ward Pharmaceuticals
- World Gen LLC
- Yung Shin Pharmaceutical Industry Ltd.
- Dosage Forms
Form Route Strength Suspension Oral Capsule Oral 500 Tablet, extended release Oral Suspension Oral 7.500 g Tablet, effervescent 1000 mg Tablet, film coated Oral 250 mg/1 Tablet, effervescent 250 mg Tablet, film coated Oral 500 mg/1 Tablet, effervescent 500 mg Powder, for solution Oral Tablet, film coated Oral Tablet, film coated Oral 750 mg Granule, for suspension Oral 375 mg/5ml Tablet, film coated Oral 375 mg Capsule Oral 250 mg/1 Capsule Oral 500 mg/1 For suspension Oral 125 mg/5mL For suspension Oral 250 mg/5mL For suspension Oral 375 mg/5mL Solution / drops Oral Suspension Oral 125 mg / 5 mL Suspension Oral 125 mg/5mL Suspension Oral 187 mg/5mL Suspension Oral 250 mg / 5 mL Suspension Oral 250 mg/5mL Suspension Oral 375 mg / 5 mL Suspension Oral 375 mg/5mL Tablet, film coated, extended release Oral 375 mg/1 Tablet, film coated, extended release Oral 500 mg/1 Tablet, film coated Oral 500 MG Powder Parenteral 250 mg/5mL Granule Oral 125 MG/5ML Granule Oral 125 MG Granule Oral 250 MG Capsule, coated Oral 500 mg Powder, for suspension Oral 3 g Powder, for suspension Oral 125 mg / 5 mL Powder, for suspension Oral 187 mg / 5 mL Powder, for suspension Oral 250 mg / 5 mL Powder, for suspension Oral 375 mg / 5 mL Powder Oral 125 mg / 5 mL Powder Oral 250 mg / 5 mL Powder Oral 375 mg / 5 mL Granule, for suspension Oral 250 MG/5ML Powder, for solution Oral 250 mg/5ml Tablet, effervescent Powder, for suspension Oral Granule, for suspension Oral Tablet Oral 500 MG Tablet, extended release Oral 375 MG Tablet, extended release Oral 750 MG Powder, for suspension Oral 187 mg/5ml Tablet, delayed release Oral 375 mg Suspension Oral 25 mg / mL Suspension Oral 50 mg / mL Suspension Oral 75 mg / mL Suspension Oral 5.000 g Capsule Oral 250.000 mg Suspension Oral 1.875 g Syrup Granule Oral 500 mg Capsule Oral 500 mg Tablet Oral 750 MG Capsule Oral Granule, for suspension Oral 375 mg Suspension / drops Oral 50 mg/mL Tablet Oral 250 mg Tablet, delayed release Oral 500 mg Tablet, delayed release Oral 750 mg Tablet, soluble Oral 500 mg Capsule Oral 10 g Capsule Oral 5 g Granule Oral 2.5 g Tablet Oral Powder, for solution Oral 25 mg / mL Powder, for solution Oral 50 mg / mL Powder, for solution Oral 75 mg / mL Tablet, effervescent Oral Granule, for suspension Oral 125 mg/5ml Suspension Oral 3.75 g Granule, for suspension Oral 187 mg/5ml Tablet, delayed release Oral Powder 125 mg/5ml Powder 250 mg/5ml Granule Oral 250 mg/5ml Capsule Oral 250 mg Powder, for suspension Oral 125 mg/5ml Powder, for suspension Oral 250 mg/5ml - Prices
Unit description Cost Unit Ceclor 15 500 mg capsule Bottle 70.0USD bottle Ceclor 375 mg/5ml Suspension 100ml Bottle 59.99USD bottle Ceclor 250 mg/5ml Suspension 150ml Bottle 58.98USD bottle Cefaclor 250 mg/5ml Suspension 150ml Bottle 53.87USD bottle Cefaclor 375 mg/5ml Suspension 100ml Bottle 53.87USD bottle Ceclor 15 250 mg capsule Bottle 38.0USD bottle Ceclor 125 mg/5ml Suspension 150ml Bottle 34.99USD bottle Ceclor 187 mg/5ml Suspension 100ml Bottle 34.99USD bottle Ceclor 250 mg/5ml Suspension 75ml Bottle 31.99USD bottle Cefaclor 125 mg/5ml Suspension 150ml Bottle 29.41USD bottle Cefaclor 250 mg/5ml Suspension 75ml Bottle 29.37USD bottle Cefaclor 187 mg/5ml Suspension 100ml Bottle 29.26USD bottle Cefaclor 375 mg/5ml Suspension 50ml Bottle 27.44USD bottle Cefaclor 187 mg/5ml Suspension 50ml Bottle 14.92USD bottle Cefaclor 125 mg/5ml Suspension 75ml Bottle 14.7USD bottle Ceclor 500 mg pulvule 5.69USD each Cefaclor 500 mg capsule 4.05USD capsule Cefaclor CR 500 mg 12 Hour tablet 3.79USD tablet Ceclor 250 mg pulvule 3.28USD each Raniclor 375 mg chewable tablet 2.98USD tablet Cefaclor 250 mg capsule 2.07USD capsule Raniclor 250 mg chewable tablet 1.99USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 327 °C Not Available water solubility 1E+004 mg/L YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 0.4 Not Available - Predicted Properties
Property Value Source Water Solubility 0.21 mg/mL ALOGPS logP 0.85 ALOGPS logP -2.3 Chemaxon logS -3.2 ALOGPS pKa (Strongest Acidic) 2.83 Chemaxon pKa (Strongest Basic) 7.23 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 112.73 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 89.56 m3·mol-1 Chemaxon Polarizability 35.11 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 No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.8839 Blood Brain Barrier - 0.9817 Caco-2 permeable - 0.8239 P-glycoprotein substrate Substrate 0.6569 P-glycoprotein inhibitor I Non-inhibitor 0.9413 P-glycoprotein inhibitor II Non-inhibitor 0.9955 Renal organic cation transporter Non-inhibitor 0.9369 CYP450 2C9 substrate Non-substrate 0.8314 CYP450 2D6 substrate Non-substrate 0.8361 CYP450 3A4 substrate Non-substrate 0.5597 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9236 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.831 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9193 Ames test Non AMES toxic 0.6676 Carcinogenicity Non-carcinogens 0.8489 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 1.2960 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9966 hERG inhibition (predictor II) Non-inhibitor 0.85
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 194.2090831 predictedDarkChem Lite v0.1.0 [M-H]- 177.34715 predictedDeepCCS 1.0 (2019) [M+H]+ 195.2894831 predictedDarkChem Lite v0.1.0 [M+H]+ 179.70515 predictedDeepCCS 1.0 (2019) [M+Na]+ 195.4826831 predictedDarkChem Lite v0.1.0 [M+Na]+ 186.41856 predictedDeepCCS 1.0 (2019)
Targets
- 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
- Chambers HF, Miick C: Characterization of penicillin-binding protein 2 of Staphylococcus aureus: deacylation reaction and identification of two penicillin-binding peptides. Antimicrob Agents Chemother. 1992 Mar;36(3):656-61. [Article]
- 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
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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. [Article]
- Chambers HF, Miick C: Characterization of penicillin-binding protein 2 of Staphylococcus aureus: deacylation reaction and identification of two penicillin-binding peptides. Antimicrob Agents Chemother. 1992 Mar;36(3):656-61. [Article]
- Li M, Anderson GD, Phillips BR, Kong W, Shen DD, Wang J: Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters. Drug Metab Dispos. 2006 Apr;34(4):547-55. Epub 2006 Jan 24. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Peroxidase activity
- Specific Function
- Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
- Gene Name
- MPO
- Uniprot ID
- P05164
- Uniprot Name
- Myeloperoxidase
- Molecular Weight
- 83867.71 Da
References
- Zuccotti G, Dauria E, Torcoletti M, Lodi F, Bernardo L, Riva E: Clinical and pro-host effects of cefaclor in prophylaxis of recurrent otitis media in HIV-infected children. J Int Med Res. 2001 Jul-Aug;29(4):349-54. [Article]
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
- Han HK, Rhie JK, Oh DM, Saito G, Hsu CP, Stewart BH, Amidon GL: CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs. J Pharm Sci. 1999 Mar;88(3):347-50. [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]
- Li M, Anderson GD, Phillips BR, Kong W, Shen DD, Wang J: Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters. Drug Metab Dispos. 2006 Apr;34(4):547-55. Epub 2006 Jan 24. [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
- 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]
- Li M, Anderson GD, Phillips BR, Kong W, Shen DD, Wang J: Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters. Drug Metab Dispos. 2006 Apr;34(4):547-55. Epub 2006 Jan 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Substrate and inhibitor activity was demonstrated 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54