Avibactam

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
US Approved
YES
Other Approved
YES
Clinical Trials
Phase 0
0
Phase 1
19
Phase 2
10
Phase 3
8
Phase 4
5
Therapeutic Categories
  • beta-Lactamase Inhibitors

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.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatBacterial infectionsRegimen in combination with: Metronidazole (DB00916), Ceftazidime (DB00438)••••••••••••
Used in combination to treatComplicated intra-abdominal infectionsRegimen in combination with: Metronidazole (DB00916), Ceftazidime (DB00438)••••••••••••
Used in combination to treatComplicated urinary tract infectionsCombination Product in combination with: Ceftazidime (DB00438)••••••••••••
Used in combination to treatNosocomial pneumoniaCombination Product in combination with: Ceftazidime (DB00438)•••••••••••••••••
Used in combination to treatVentilator associated bacterial pneumoniaCombination Product in combination with: Ceftazidime (DB00438)•••••••••••••••••
Contraindications & Blackbox Warnings
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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.

TargetActionsOrganism
ABeta-lactamase TEM
inhibitor
Escherichia coli
ABeta-lactamase CTX-M
inhibitor
Escherichia coli
ABeta-lactamase
inhibitor
Enterobacter cloacae
ABeta-lactamase SHV-1
inhibitor
Escherichia coli
ABeta-lactamase SHV-2
inhibitor
Escherichia coli
ABeta-lactamase SHV-1
inhibitor
Klebsiella pneumoniae
AClass D OXA-48 carbapenemase
inhibitor
Klebsiella pneumoniae
ACarbapenem-hydrolyzing beta-lactamase KPC
inhibitor
Klebsiella pneumoniae
ABeta-lactamase UOE-1
inhibitor
Escherichia coli
AExtended-spectrum beta-lactamase PER-1
inhibitor
Pseudomonas 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
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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.
DrugInteraction
Acetylsalicylic acidThe excretion of Avibactam can be decreased when combined with Acetylsalicylic acid.
AcyclovirThe excretion of Avibactam can be decreased when combined with Acyclovir.
Aminohippuric acidThe excretion of Avibactam can be decreased when combined with Aminohippuric acid.
ApalutamideThe excretion of Avibactam can be decreased when combined with Apalutamide.
AtalurenThe excretion of Avibactam can be decreased when combined with Ataluren.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Avibactam sodium9V824P8TAI1192491-61-4RTCIKUMODPANKX-JBUOLDKXSA-M
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AvycazAvibactam sodium (0.5 g/1) + Ceftazidime pentahydrate (2 g/1)Powder, for solutionIntravenousAllergan, Inc.2014-12-26Not applicableUS flag
EmblaveoAvibactam sodium (0.5 g) + Aztreonam (1.5 g)Injection, powder, for solutionIntravenousPfizer Europe Ma Eeig2024-07-10Not applicableEU flag
ZAVICEFTAAvibactam sodium (543.5 mg) + Ceftazidime pentahydrate (2329.7 mg)Injection, powder, for solutionPfizer Italia S.R.L.2020-07-292025-07-29Indonesia flag
ZaviceftaAvibactam sodium (500 mg) + Ceftazidime pentahydrate (2000 mg)Injection, powder, for solutionIntravenousPFİZER İLAÇLARI LTD. ŞTİ.2016-09-08Not applicableEU flag
ZAVICEFTAAvibactam (0.5 g) + Ceftazidime (2 g)Injection, powder, for solutionIntravenous; ParenteralPFİZER İLAÇLARI LTD. ŞTİ.2016-10-12Not applicableItaly flag

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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. 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]
PubChem Compound
9835049
PubChem Substance
310264997
ChemSpider
8010770
BindingDB
50339145
RxNav
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
PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
Not AvailableActive Not RecruitingNot AvailableSevere Sepsis1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableBacterial Infections1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableCarbapenem Resistant Enterobacteriaceae Infection1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableGram-Negative Bacterial Infections1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableVentilator Associated Bacterial Pneumonia (VABP)1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for solutionIntravenous
Injection, powder, for solution
Injection, powder, for solutionIntravenous
Injection, powder, for solutionIntravenous; Parenteral
Powder, for solutionIntravenous0.5 g
SolutionIntravenous
Injection, powder, for solutionIntravenous500 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US7112592No2006-09-262022-02-24US flag
US8178554No2012-05-152021-07-24US flag
US7612087No2009-11-032026-11-12US flag
US8471025No2013-06-252031-08-12US flag
US8835455No2014-09-162030-10-08US flag
US8969566No2015-03-032032-06-15US flag
US9284314No2016-03-152032-06-15US flag
US9695122No2017-07-042032-06-15US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility15.0 mg/mLALOGPS
logP-1.8ALOGPS
logP-3.6Chemaxon
logS-1.2ALOGPS
pKa (Strongest Acidic)-2Chemaxon
pKa (Strongest Basic)-3.9Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area130.24 Å2Chemaxon
Rotatable Bond Count3Chemaxon
Refractivity52.48 m3·mol-1Chemaxon
Polarizability22.32 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0059-9620000000-f8a2f4394fba4476b607
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-014j-0090000000-5c66b542ecc17d91917b
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-01ox-8090000000-47d8ead2503f76d18311
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-9300000000-b696a055b2d233a7410b
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-016r-0900000000-3e9f69bd4fd12930f934
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-000e-9130000000-3f608706316e9e1238f0
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-005d-5900000000-e2951531cd02ae3582cb
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-145.63405
predicted
DeepCCS 1.0 (2019)
[M+H]+147.45894
predicted
DeepCCS 1.0 (2019)
[M+Na]+153.06476
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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