Avibactam
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Overview
- Description
- An antibiotic medication used to treat various bacterial infections in the body with ceftazidime, another antibiotic drug.
- Description
- An antibiotic medication used to treat various bacterial infections in the body with ceftazidime, another antibiotic drug.
- DrugBank ID
- DB09060
- Type
- Small Molecule
- Clinical Trials
- Phase 0
- 0
- Phase 1
- 19
- Phase 2
- 10
- Phase 3
- 8
- Phase 4
- 5
- Mechanism of Action
Identification
- Summary
Avibactam is a non-β-lactam β-lactamase inhibitor used in combination with ceftazidime for the treatment of complicated intra-abdominal infections, complicated urinary tract infections, and hospital or ventilator-acquired pneumonia.
- Brand Names
- Avycaz, Zavicefta
- Generic Name
- Avibactam
- DrugBank Accession Number
- DB09060
- Background
Avibactam is a non-β-lactam β-lactamase inhibitor that is available in combination with ceftazidime (Avycaz). This combination was approved by the FDA on February 25, 2015 for the treatment of complicated intra-abdominal infections in combination with metronidazole, and the treatment of complicated urinary tract infections, including pyelonephritis caused by antibiotic resistant-pathogens, including those caused by multi-drug resistant gram-negative bacterial pathogens. As there is limited clinical safety and efficacy data, Avycaz should be reserved for patients over 18 years old who have limited or not alternative treatment options.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 265.24
Monoisotopic: 265.03685626 - Chemical Formula
- C7H11N3O6S
- Synonyms
- Avibactam
- External IDs
- NXL 104
- NXL-104
- NXL104
Pharmacology
- Indication
AVYCAZ (ceftazidime-avibactam), in combination with metronidazole, is indicated for the treatment of complicated intra-abdominal infections caused by the following susceptible microorganisms: Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Providencia stuartii, Enterobacter cloacae, Klebsiella oxytoca, and Pseudomonas aeruginosa in patients 18 years or older. AVYCAZ is also indicated for the treatment of complicated urinary tract infections including pyelonephritis caused by the following susceptible microorganisms: Escherichia coli, Klebsiella pneumoniae, Citrobacter koseri, Enterobacter aerogenes, Enterobacter cloacae, Citrobacter freundii, Proteus spp., and Pseudomonas aeruginosa in patients 18 years or older.
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 Used in combination to treat Bacterial infections Regimen in combination with: Metronidazole (DB00916), Ceftazidime (DB00438) •••••••••••• Used in combination to treat Complicated intra-abdominal infections Regimen in combination with: Metronidazole (DB00916), Ceftazidime (DB00438) •••••••••••• Used in combination to treat Complicated urinary tract infections Combination Product in combination with: Ceftazidime (DB00438) •••••••••••• Used in combination to treat Nosocomial pneumonia Combination Product in combination with: Ceftazidime (DB00438) •••••••••••• ••••• Used in combination to treat Ventilator associated bacterial pneumonia Combination Product in combination with: Ceftazidime (DB00438) •••••••••••• ••••• - 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
Not Available
- Mechanism of action
Avibactam is a non-β lactam β-lactamase inhibitor that inactivates some β-lactamases (Ambler class A β-lactamases, including Klebsiella pneumoniae carbapenemases, Ambler class C and some Ambler class D β-lactamases) by a unique covalent and reversible mechanism, and protects ceftazidime from degradation by certain β-lactamases. Avibactam rapidly reaches the periplasm of bacteria at high enough concentrations to restore activity of ceftazidime against ceftazidime-resistant, β-lactamase-producing strains. Avibactam does not decrease the activity of ceftazidime against ceftazidime susceptible organisms.
Target Actions Organism ABeta-lactamase TEM inhibitorEscherichia coli ABeta-lactamase CTX-M inhibitorEscherichia coli ABeta-lactamase inhibitorEnterobacter cloacae ABeta-lactamase SHV-1 inhibitorEscherichia coli ABeta-lactamase SHV-2 inhibitorEscherichia coli ABeta-lactamase SHV-1 inhibitorKlebsiella pneumoniae AClass D OXA-48 carbapenemase inhibitorKlebsiella pneumoniae ACarbapenem-hydrolyzing beta-lactamase KPC inhibitorKlebsiella pneumoniae ABeta-lactamase UOE-1 inhibitorEscherichia coli AExtended-spectrum beta-lactamase PER-1 inhibitorPseudomonas aeruginosa - Absorption
Not Available
- Volume of distribution
The steady state volumes of distribution of avibactam and ceftazidime is 22.2L and 17L respectively.
- Protein binding
5.7%-8.2% of avibactam is bound to plasma protein, and less than 10% of ceftazidime is protein bound.
- Metabolism
No metabolism of avibactam was observed in human liver preparations. Unchanged avibactam is the major drug-related component in human plasma and urine. 80-90% of ceftazidime is eliminated as unchanged .
- Route of elimination
Avibactam and ceftazidime are excreted mainly by the kidneys.
- Half-life
Ceftazidime-avibactam has a half life of ~2.7-3.0 hours.
- Clearance
Avibactam and ceftazidime has a clearance of ~12L/h and ~7L/h respectively.
- 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
Avycaz is contraindicated in patients with known serious hypersensitivity to avibactam-containing products, ceftazidime or other members of the cephalosporin class.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcetylsalicylic acid The excretion of Avibactam can be decreased when combined with Acetylsalicylic acid. Acyclovir The excretion of Avibactam can be decreased when combined with Acyclovir. Aminohippuric acid The excretion of Avibactam can be decreased when combined with Aminohippuric acid. Apalutamide The excretion of Avibactam can be decreased when combined with Apalutamide. Ataluren The excretion of Avibactam can be decreased when combined with Ataluren. - Food Interactions
- No interactions found.
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 Avibactam sodium 9V824P8TAI 1192491-61-4 RTCIKUMODPANKX-JBUOLDKXSA-M - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Avycaz Avibactam sodium (0.5 g/1) + Ceftazidime pentahydrate (2 g/1) Powder, for solution Intravenous Allergan, Inc. 2014-12-26 Not applicable US Emblaveo Avibactam sodium (0.5 g) + Aztreonam (1.5 g) Injection, powder, for solution Intravenous Pfizer Europe Ma Eeig 2024-07-10 Not applicable EU ZAVICEFTA Avibactam sodium (543.5 mg) + Ceftazidime pentahydrate (2329.7 mg) Injection, powder, for solution Pfizer Italia S.R.L. 2020-07-29 2025-07-29 Indonesia Zavicefta Avibactam sodium (500 mg) + Ceftazidime pentahydrate (2000 mg) Injection, powder, for solution Intravenous PFİZER İLAÇLARI LTD. ŞTİ. 2016-09-08 Not applicable EU ZAVICEFTA Avibactam (0.5 g) + Ceftazidime (2 g) Injection, powder, for solution Intravenous; Parenteral PFİZER İLAÇLARI LTD. ŞTİ. 2016-10-12 Not applicable Italy
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Alpha amino acid amides
- Alternative Parents
- Piperidinecarboxamides / 1,3-diazepanes / Imidazolidinones / Organic sulfuric acids and derivatives / Primary carboxylic acid amides / Organic carbonic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides show 2 more
- Substituents
- 1,3-diazepane / 2-piperidinecarboxamide / Aliphatic heteropolycyclic compound / Alpha-amino acid amide / Azacycle / Carbonic acid derivative / Carbonyl group / Carboxamide group / Diazepane / Hydrocarbon derivative show 13 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- azabicycloalkane, ureas, monocarboxylic acid amide, hydroxylamine O-sulfonic acid (CHEBI:85984)
- Affected organisms
- Pseudomonas aeruginosa
- Escherichia coli
- Proteus vulgaris
- Klebsiella
- Enterobacter
- Citrobacter
- Proteus mirabilis
- Providencia stuartii
Chemical Identifiers
- UNII
- 7352665165
- CAS number
- 1192500-31-4
- InChI Key
- NDCUAPJVLWFHHB-UHNVWZDZSA-N
- InChI
- InChI=1S/C7H11N3O6S/c8-6(11)5-2-1-4-3-9(5)7(12)10(4)16-17(13,14)15/h4-5H,1-3H2,(H2,8,11)(H,13,14,15)/t4-,5+/m1/s1
- IUPAC Name
- [(2S,5R)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl]oxidanesulfonic acid
- SMILES
- NC(=O)[C@@H]1CC[C@@H]2CN1C(=O)N2OS(O)(=O)=O
References
- General References
- Stachyra T, Levasseur P, Pechereau MC, Girard AM, Claudon M, Miossec C, Black MT: In vitro activity of the {beta}-lactamase inhibitor NXL104 against KPC-2 carbapenemase and Enterobacteriaceae expressing KPC carbapenemases. J Antimicrob Chemother. 2009 Aug;64(2):326-9. doi: 10.1093/jac/dkp197. Epub 2009 Jun 2. [Article]
- Das S, Li J, Armstrong J, Learoyd M, Edeki T: Randomized pharmacokinetic and drug-drug interaction studies of ceftazidime, avibactam, and metronidazole in healthy subjects. Pharmacol Res Perspect. 2015 Oct;3(5):e00172. doi: 10.1002/prp2.172. Epub 2015 Aug 25. [Article]
- MacVane SH, Crandon JL, Nichols WW, Nicolau DP: In vivo efficacy of humanized exposures of Ceftazidime-Avibactam in comparison with Ceftazidime against contemporary Enterobacteriaceae isolates. Antimicrob Agents Chemother. 2014 Nov;58(11):6913-9. doi: 10.1128/AAC.03267-14. Epub 2014 Sep 15. [Article]
- Pages JM, Peslier S, Keating TA, Lavigne JP, Nichols WW: Role of the Outer Membrane and Porins in Susceptibility of beta-Lactamase-Producing Enterobacteriaceae to Ceftazidime-Avibactam. Antimicrob Agents Chemother. 2015 Dec 14;60(3):1349-59. doi: 10.1128/AAC.01585-15. [Article]
- Ehmann DE, Jahic H, Ross PL, Gu RF, Hu J, Kern G, Walkup GK, Fisher SL: Avibactam is a covalent, reversible, non-beta-lactam beta-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8. doi: 10.1073/pnas.1205073109. Epub 2012 Jul 2. [Article]
- Ehmann DE, Jahic H, Ross PL, Gu RF, Hu J, Durand-Reville TF, Lahiri S, Thresher J, Livchak S, Gao N, Palmer T, Walkup GK, Fisher SL: Kinetics of avibactam inhibition against Class A, C, and D beta-lactamases. J Biol Chem. 2013 Sep 27;288(39):27960-71. doi: 10.1074/jbc.M113.485979. Epub 2013 Aug 2. [Article]
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- External Links
- PubChem Compound
- 9835049
- PubChem Substance
- 310264997
- ChemSpider
- 8010770
- BindingDB
- 50339145
- 1603834
- ChEBI
- 85984
- ChEMBL
- CHEMBL1689063
- ZINC
- ZINC000009302239
- PDBe Ligand
- FYG
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Avibactam
- PDB Entries
- 7kep / 7keq / 7ker
- FDA label
- Download (301 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Severe Sepsis 1 somestatus stop reason just information to hide Not Available Completed Not Available Bacterial Infections 1 somestatus stop reason just information to hide Not Available Completed Not Available Carbapenem Resistant Enterobacteriaceae Infection 1 somestatus stop reason just information to hide Not Available Completed Not Available Gram-Negative Bacterial Infections 1 somestatus stop reason just information to hide Not Available Completed Not Available Ventilator Associated Bacterial Pneumonia (VABP) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder, for solution Intravenous Injection, powder, for solution Injection, powder, for solution Intravenous Injection, powder, for solution Intravenous; Parenteral Powder, for solution Intravenous 0.5 g Solution Intravenous Injection, powder, for solution Intravenous 500 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7112592 No 2006-09-26 2022-02-24 US US8178554 No 2012-05-15 2021-07-24 US US7612087 No 2009-11-03 2026-11-12 US US8471025 No 2013-06-25 2031-08-12 US US8835455 No 2014-09-16 2030-10-08 US US8969566 No 2015-03-03 2032-06-15 US US9284314 No 2016-03-15 2032-06-15 US US9695122 No 2017-07-04 2032-06-15 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 15.0 mg/mL ALOGPS logP -1.8 ALOGPS logP -3.6 Chemaxon logS -1.2 ALOGPS pKa (Strongest Acidic) -2 Chemaxon pKa (Strongest Basic) -3.9 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 130.24 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 52.48 m3·mol-1 Chemaxon Polarizability 22.32 Å3 Chemaxon Number of Rings 2 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
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0059-9620000000-f8a2f4394fba4476b607 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014j-0090000000-5c66b542ecc17d91917b Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-01ox-8090000000-47d8ead2503f76d18311 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-9300000000-b696a055b2d233a7410b Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-016r-0900000000-3e9f69bd4fd12930f934 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-000e-9130000000-3f608706316e9e1238f0 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-005d-5900000000-e2951531cd02ae3582cb Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 145.63405 predictedDeepCCS 1.0 (2019) [M+H]+ 147.45894 predictedDeepCCS 1.0 (2019) [M+Na]+ 153.06476 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Escherichia coli
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- TEM-type are the most prevalent beta-lactamases in enterobacteria; they hydrolyze the beta-lactam bond in susceptible beta-lactam antibiotics, thus conferring resistance to penicillins and cephalosporins. TEM-3 and TEM-4 are capable of hydrolyzing cefotaxime and ceftazidime. TEM-5 is capable of hydrolyzing ceftazidime. TEM-6 is capable of hydrolyzing ceftazidime and aztreonam. TEM-8/CAZ-2, TEM-16/CAZ-7 and TEM-24/CAZ-6 are markedly active against ceftazidime. IRT-4 shows resistance to beta-lactamase inhibitors.
- Specific Function
- beta-lactamase activity
- Gene Name
- bla
- Uniprot ID
- P62593
- Uniprot Name
- Beta-lactamase TEM
- Molecular Weight
- 31514.865 Da
References
- Ehmann DE, Jahic H, Ross PL, Gu RF, Hu J, Kern G, Walkup GK, Fisher SL: Avibactam is a covalent, reversible, non-beta-lactam beta-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8. doi: 10.1073/pnas.1205073109. Epub 2012 Jul 2. [Article]
- Kind
- Protein group
- Organism
- Escherichia coli
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Not Available
- Specific Function
- beta-lactamase activity
Components:
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Enterobacter cloacae
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- This protein is a serine beta-lactamase with a substrate specificity for cephalosporins.
- Specific Function
- beta-lactamase activity
- Gene Name
- ampC
- Uniprot ID
- P05364
- Uniprot Name
- Beta-lactamase
- Molecular Weight
- 41301.33 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Escherichia coli
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Not Available
- Specific Function
- beta-lactamase activity
- Gene Name
- bla
- Uniprot ID
- P0AD63
- Uniprot Name
- Beta-lactamase SHV-1
- Molecular Weight
- 31223.635 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Escherichia coli
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- This enzyme hydrolyzes cefotaxime, ceftazidime and other broad spectrum cephalosporins.
- Specific Function
- beta-lactamase activity
- Gene Name
- bla
- Uniprot ID
- P0A9Z7
- Uniprot Name
- Beta-lactamase SHV-2
- Molecular Weight
- 31253.655 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Klebsiella pneumoniae
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Broad-spectrum beta-lactamase which confers resistance to penicillins, as well as first- and third-generation cephalosporins (PubMed:10639363, PubMed:18955486, PubMed:19351161, PubMed:22908166, PubMed:23145056, PubMed:23252553). Has nitrocefin-hydrolyzing activity (PubMed:10231522, PubMed:19351161, PubMed:23252553). Inactive against the cephalosporins, cefotaxime and cefoxitin, and the carbapenem, meropenem (PubMed:10639363, PubMed:19351161).
- Specific Function
- beta-lactamase activity
- Gene Name
- bla
- Uniprot ID
- P0AD64
- Uniprot Name
- Beta-lactamase SHV-1
- Molecular Weight
- 31223.635 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Klebsiella pneumoniae
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Not Available
- Specific Function
- penicillin binding
- Gene Name
- OXA-48
- Uniprot ID
- A0A023W3H0
- Uniprot Name
- Class D OXA-48 carbapenemase
- Molecular Weight
- 16920.07 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Klebsiella pneumoniae
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Hydrolyzes carbapenems, penicillins, cephalosporins and monobactams with varying efficiency.
- Specific Function
- beta-lactamase activity
- Gene Name
- bla
- Uniprot ID
- Q9F663
- Uniprot Name
- Carbapenem-hydrolyzing beta-lactamase KPC
- Molecular Weight
- 31114.99 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Escherichia coli
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Not Available
- Specific Function
- beta-lactamase activity
- Gene Name
- blaUOE-1
- Uniprot ID
- Q9EXV5
- Uniprot Name
- Beta-lactamase UOE-1
- Molecular Weight
- 31143.3 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
- Kind
- Protein
- Organism
- Pseudomonas aeruginosa
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Not Available
- Specific Function
- beta-lactamase activity
- Gene Name
- per1
- Uniprot ID
- P37321
- Uniprot Name
- Extended-spectrum beta-lactamase PER-1
- Molecular Weight
- 33572.575 Da
References
- Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- ATP-dependent transporter of the ATP-binding cassette (ABC) family that binds and hydrolyzes ATP to enable active transport of various substrates including many drugs, toxicants and endogenous compound across cell membranes. Transports a wide variety of conjugated organic anions such as sulfate-, glucuronide- and glutathione (GSH)-conjugates of endo- and xenobiotics substrates (PubMed:10220572, PubMed:10421658, PubMed:11500505, PubMed:16332456). Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification (PubMed:10421658). Mediates also hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 (PubMed:11500505). Transports sulfated bile salt such as taurolithocholate sulfate (PubMed:16332456). Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors (PubMed:10220572, PubMed:11500505, PubMed:12441801). Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine (PubMed:10220572, PubMed:11500505)
- Specific Function
- ABC-type glutathione S-conjugate transporter activity
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- ATP-binding cassette sub-family C member 2
- Molecular Weight
- 174205.64 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient (PubMed:14586168, PubMed:15644426, PubMed:15846473, PubMed:16455804, PubMed:31553721). Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) (PubMed:14586168, PubMed:15846473, PubMed:15864504, PubMed:22108572, PubMed:23832370). Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain (PubMed:11306713, PubMed:14586168, PubMed:15846473). E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange (PubMed:26377792). Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule (PubMed:11907186). Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate (PubMed:22108572, PubMed:23832370). Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins (PubMed:28534121). May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside (PubMed:15644426). May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate (PubMed:11669456, PubMed:15846473, PubMed:16455804). Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) (PubMed:14675047). May contribute to the release of cortisol in the adrenals (PubMed:15864504). Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB). In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
- Specific Function
- organic anion transmembrane transporter activity
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Organic anion transporter 3
- Molecular Weight
- 59855.585 Da
Drug created at May 11, 2015 21:50 / Updated at February 21, 2021 18:52