Fusidic acid

Identification

Summary

Fusidic acid is a topical antibacterial agent used to prevent and treat mild to moderate skin infections caused by susceptible bacteria.

Brand Names
Fucibet, Fucidin, Fucithalmic
Generic Name
Fusidic acid
DrugBank Accession Number
DB02703
Background

An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed) It acts by inhibiting translocation during protein synthesis. It is often used topically in creams and eyedrops but is available in systemic formulations including tablets and injections.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 516.7092
Monoisotopic: 516.345089268
Chemical Formula
C31H48O6
Synonyms
  • Acide fusidique
  • Acido fusidico
  • Acidum fusidicum
  • Fucidate
  • Fucidin acid
  • Fusidate
  • Fusidic acid
  • Fusidine
  • Ramycin
External IDs
  • NSC-56192
  • SQ 16,603
  • SQ-16603

Pharmacology

Indication

For the treatment of bacterial infections.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Fusidic acid is a bacteriostatic antibiotic and helps prevent bacterial growth while the immune system clears the infection.

Mechanism of action

Fusidic acid works by interfering with bacterial protein synthesis, specifically by preventing the translocation of the elongation factor G (EF-G) from the ribosome. It also can inhibit chloramphenicol acetyltransferase enzymes.

TargetActionsOrganism
AElongation factor G
inhibitor
Thermus thermophilus
UChloramphenicol acetyltransferase
inhibitor
Salmonella typhi
UChloramphenicol acetyltransferase 3
inhibitor
Escherichia coli
Absorption

Sodium fusidic acid tablets have a 91% oral bioavailability. Absorption of the film-coated tablets is complete when compared to a solution, however oral absorption is variable. Oral fusidic acid hemihydrate (suspension) achieved a 22.5% bioavailability in pediatric patients following a 20 milligram/kilogram dose.

Volume of distribution

Not Available

Protein binding

97 to 99%

Metabolism

Metabolites include dicarboxylic ester/acid, 3-keto fusidic acid, hydroxy fusidic acid, glucuronide fusidic acid and a glycol metabolite.

Hover over products below to view reaction partners

Route of elimination

Not Available

Half-life

Approximately 5 to 6 hours in adults.

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

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
1,2-BenzodiazepineThe metabolism of 1,2-Benzodiazepine can be decreased when combined with Fusidic acid.
AbametapirThe serum concentration of Fusidic acid can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Fusidic acid can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Fusidic acid.
AbirateroneThe metabolism of Fusidic acid can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Fusidic acid.
AcebutololThe metabolism of Acebutolol can be decreased when combined with Fusidic acid.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Fusidic acid.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Fusidic acid.
AcipimoxThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Fusidic acid is combined with Acipimox.
Interactions
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Food Interactions
  • Take with food. Food reduces irritation.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Fucidate sodiumJ7P3696BCQ751-94-0HJHVQCXHVMGZNC-JCJNLNMISA-M
Fusidic acid hemihydrateW540G73230172343-30-5CSXHKOSAWQTJBT-YDYKLMMDSA-N
International/Other Brands
Fucidine / Fudic / Taksta
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Fucidin Cream 2%Cream2 %TopicalLeo Pharma1984-12-31Not applicableCanada flag
Fucidin Film Coated Tab 250mgTablet250 mgOralLeo Pharma1991-12-312009-06-05Canada flag
Fucidin Intertulle 2%Dressing2 %TopicalLeo Pharma1984-12-312004-07-23Canada flag
Fucidin Leo Sus 246mg/5mlSuspension246 mg / 5 mLOralLeo Pharma1980-12-312004-07-23Canada flag
Fucidin Ointment 2%Ointment2 %TopicalLeo Pharma1984-12-31Not applicableCanada flag
FucithalmicSolution / drops1 % w/wOphthalmicAmdipharm Limited2001-08-072017-07-17Canada flag
FucithalmicSolution / drops1 % w/wOphthalmicAmdipharm Limited2001-08-29Not applicableCanada flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DIFUSINOintment2 %w/wTopicalบริษัท ฟาร์มาแลนด์ (1982) จำกัด2007-03-202020-09-29Thailand flag
FucidinOintment20 mg/1gTopicalI World Pharmaceutical Co., Ltd.2019-10-08Not applicableUS flag
FucidinOintment20 mg/1gTopicalLydia Co., Ltd.2019-10-08Not applicableUS flag
FucidinOintment20 mg/1gTopicalOASIS TRADING2018-11-21Not applicableUS flag
ฟิวซิดินOintment2 %w/wTopicalบริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด2010-03-11Not applicableThailand flag
ฟิวซิดินCream2 %w/wTopicalบริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด2010-03-11Not applicableThailand flag
ลูซิน่าร์ ครีมCream2 %w/wTopicalบริษัท สหการโอสถ (1996) จำกัด จำกัด2008-12-21Not applicableThailand flag
เจิมมีดิก (ครีม)Cream2 %w/wTopicalบริษัท โรงงานเภสัชกรรมแอตแลนติค จำกัด2015-10-05Not applicableThailand flag
แอ็กเซล ฟูซิดิก แอซิด ครีมCream2 %w/wTopicalบริษัท ฟาร์มาแลนด์ (1982) จำกัด2018-03-19Not applicableThailand flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
DEFUZIN-B CREAMFusidic acid (2 % w/w) + Betamethasone valerate (0.1 % w/w)CreamTopicalXEPA-SOUL PATTINSON (MALAYSIA) SDN BHD2020-09-08Not applicableMalaysia flag
DERMOTRIZOL ®Fusidic acid (2.04 g) + Dexamethasone (0.054 g) + Ketoconazole (2.04 g)CreamTopicalCOLOMPACK S.A.2018-05-02Not applicableColombia flag
FucibetFusidic acid (2 % w/w) + Betamethasone (0.1 % w/w)CreamTopicalLeo Pharma2018-10-03Not applicableCanada flag
FUCICORT 20 MG/G + 1 MG/G KREM, 30 GFusidic acid (20 mg/g) + Betamethasone valerate (1 mg/g)CreamTopicalABDİ İBRAHİM İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
FUCICORT(R)Fusidic acid (2 g/100g) + Betamethasone valerate (100 mg/100g)Creamบริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด2010-03-11Not applicableThailand flag
FUCICORT® CREMAFusidic acid hemihydrate (2 g) + Betamethasone valerate (0.1 g)CreamTopicalLABORATORIOS BIOPAS S.A2006-11-102011-02-17Colombia flag
Fucidin HFusidic acid (2 %) + Hydrocortisone acetate (1 %)CreamTopicalLeo Pharma1998-11-11Not applicableCanada flag
FUCIDIN HFusidic acid (20 MG/1G) + Hydrocortisone (10 MG/1G)CreamTopicalบริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด2010-03-11Not applicableThailand flag
FUCIDIN H %2 + %1 KREM, 30 GFusidic acid (2 %) + Hydrocortisone acetate (1 %)CreamTopicalABDİ İBRAHİM İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
Fucidin Leo Injection KitFucidate sodium (500 mg / kit) + Sodium phosphate, dibasic (10 mL / kit)KitIntravenousLeo Pharma1984-12-312004-08-01Canada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
FUCIBEST % 2 20 GR KREMFusidic acid (2 %)CreamTopicalTRİOZER İLAÇ KİM. KOZMETİK SAĞ. HİZM. SAN. VE TİC. LTD. ŞTİ.2020-08-14Not applicableTurkey flag
FucidinFucidate sodium (20 mg/1g)OintmentTopicalI World Pharmaceutical Co., Ltd.2019-10-08Not applicableUS flag
FucidinFucidate sodium (20 mg/1g)OintmentTopicalLydia Co., Ltd.2019-10-08Not applicableUS flag
FucidinFucidate sodium (20 mg/1g)OintmentTopicalOASIS TRADING2018-11-21Not applicableUS flag

Categories

ATC Codes
S01AA13 — Fusidic acidD09AA02 — Fusidic acidJ01XC01 — Fusidic acidD06AX01 — Fusidic acid
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Steroid esters
Direct Parent
Steroid esters
Alternative Parents
3-alpha-hydroxysteroids / 11-alpha-hydroxysteroids / Medium-chain fatty acids / Methyl-branched fatty acids / Hydroxy fatty acids / Unsaturated fatty acids / Dicarboxylic acids and derivatives / Secondary alcohols / Cyclic alcohols and derivatives / Carboxylic acid esters
show 4 more
Substituents
11-alpha-hydroxysteroid / 11-hydroxysteroid / 3-alpha-hydroxysteroid / 3-hydroxysteroid / Alcohol / Aliphatic homopolycyclic compound / Branched fatty acid / Carbonyl group / Carboxylic acid / Carboxylic acid derivative
show 16 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
3alpha-hydroxy steroid, alpha,beta-unsaturated monocarboxylic acid, sterol ester, steroid acid, 11alpha-hydroxy steroid, steroid antibiotic (CHEBI:29013) / Prostostane and fusidane triterpenoids (LMPR0106040001)
Affected organisms
  • Enteric bacteria and other eubacteria

Chemical Identifiers

UNII
59XE10C19C
CAS number
6990-06-3
InChI Key
IECPWNUMDGFDKC-MZJAQBGESA-N
InChI
InChI=1S/C31H48O6/c1-17(2)9-8-10-20(28(35)36)26-22-15-24(34)27-29(5)13-12-23(33)18(3)21(29)11-14-30(27,6)31(22,7)16-25(26)37-19(4)32/h9,18,21-25,27,33-34H,8,10-16H2,1-7H3,(H,35,36)/b26-20-/t18-,21-,22-,23+,24+,25-,27-,29-,30-,31-/m0/s1
IUPAC Name
2-[(1Z,2S,3aS,3bS,5aS,6S,7R,9aS,9bS,10R,11aR)-2-(acetyloxy)-7,10-dihydroxy-3a,3b,6,9a-tetramethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-1-ylidene]-6-methylhept-5-enoic acid
SMILES
[H][C@@]12C[C@@H](O)[C@@]3([H])[C@@]4(C)CC[C@@H](O)[C@@H](C)[C@]4([H])CC[C@]3(C)[C@@]1(C)C[C@H](OC(C)=O)\C2=C(\CCC=C(C)C)C(O)=O

References

Synthesis Reference

Vanangamudi Subramaniam Sulur, Madhavan Srinivasan, Neelakandan Narayanan Chulliel, Haridas Sankar, Selvaraj Balkrishnan, " PROCESS TO MAKE FUSIDIC ACID CREAM." U.S. Patent US20110301138, issued December 08, 2011.

US20110301138
General References
  1. Health Canada Product Monograph: Fucidin (fucidic acid) for topical use [Link]
Human Metabolome Database
HMDB0015570
KEGG Drug
D04281
KEGG Compound
C06694
PubChem Compound
3000226
PubChem Substance
46505364
ChemSpider
2271900
BindingDB
58924
RxNav
113608
ChEBI
29013
ChEMBL
CHEMBL374975
ZINC
ZINC000008143796
Therapeutic Targets Database
DAP001008
PharmGKB
PA164749648
PDBe Ligand
FUA
Wikipedia
Fusidic_acid
PDB Entries
1q23 / 1qca / 2vuf / 4v5f / 4v5m / 4v5n / 4v7b / 4v8u / 4v9l / 4v9m
show 10 more

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentDiabetes Mellitus1
4TerminatedTreatmentImpetigo1
4Unknown StatusTreatmentInflammation of the Eyelids1
3CompletedTreatmentAcute Bacterial Skin and Skin Structure Infection (ABSSSI)1
3CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
3TerminatedTreatmentInfected Atopic Dermatitis/Eczema1
3Unknown StatusPreventionKeloids Scars / Scars, Hypertrophic1
2CompletedTreatmentSkin Diseases, Bacterial1
2TerminatedTreatmentInfected Spacers / Prosthetic Joint Infections of Hip / Prosthetic Joint Infections of Knee1
2, 3CompletedTreatmentRefractory Bone or Joint Infections1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for suspensionOral5 g
SolutionConjunctival; Ophthalmic10 mg
Capsule250 MG
CreamTopical2 %
OintmentTopical2 %w/w
OintmentTopical
CreamTopical
CreamTopical20 mg
CreamTopical20 MG/G
OintmentTopical20 mg/1g
Tablet, film coatedOral
OintmentTopical
OintmentTopical20 MG/G
TabletOral250 mg
CreamCutaneous
DressingTopical2 %
DressingTopical
KitIntravenous
SuspensionOral246 mg / 5 mL
OintmentTopical2 %
TabletOral
Tablet, film coatedOral250 mg
OintmentTopical2 g
Drug delivery systemTopical30 mg
OintmentTopical20 mg
CreamTopical2 mg
Solution / dropsOphthalmic1 % w/w
Solution / dropsOphthalmic1 %
GelOphthalmic
Suspension / dropsOphthalmic
SuspensionOphthalmic10 mg
CreamTopical
CreamTopical2 g
Injection, solution, concentrateIntravenous
Solution / dropsOphthalmic
InjectionIntravenous
Pill
Tablet, coatedOral
SuspensionTopical20 mg
Injection, solutionIntravenous
Cream
Tablet, coatedOral250 mg
CreamTopical2 %w/w
Prices
Unit descriptionCostUnit
Fucidin 2 % Cream0.66USD g
Fucidin 2 % Ointment0.66USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)192.5 °CPhysProp
pKa5.35MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.00521 mg/mLALOGPS
logP4.97ALOGPS
logP4.42ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)4.46ChemAxon
pKa (Strongest Basic)-0.2ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area104.06 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity144.12 m3·mol-1ChemAxon
Polarizability59.76 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9691
Blood Brain Barrier+0.7909
Caco-2 permeable-0.6089
P-glycoprotein substrateSubstrate0.8165
P-glycoprotein inhibitor INon-inhibitor0.6004
P-glycoprotein inhibitor IIInhibitor0.7848
Renal organic cation transporterNon-inhibitor0.8424
CYP450 2C9 substrateNon-substrate0.8218
CYP450 2D6 substrateNon-substrate0.9349
CYP450 3A4 substrateSubstrate0.798
CYP450 1A2 substrateNon-inhibitor0.9337
CYP450 2C9 inhibitorNon-inhibitor0.8834
CYP450 2D6 inhibitorNon-inhibitor0.9544
CYP450 2C19 inhibitorNon-inhibitor0.9347
CYP450 3A4 inhibitorNon-inhibitor0.76
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.819
Ames testNon AMES toxic0.8305
CarcinogenicityNon-carcinogens0.9508
BiodegradationNot ready biodegradable0.9753
Rat acute toxicity3.5929 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9403
hERG inhibition (predictor II)Non-inhibitor0.7564
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
MS/MS Spectrum - Linear Ion Trap , negativeLC-MS/MSsplash10-05fr-0002900000-512150f35d55c73b9e09
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-004i-0000900000-eecd35dcbd3fede944c2
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-0002-0000900000-4a266f99ada066a14539

Targets

Drugtargets2
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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
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Learn more
Kind
Protein
Organism
Thermus thermophilus
Pharmacological action
Yes
Actions
Inhibitor
General Function
Translation elongation factor activity
Specific Function
Catalyzes the GTP-dependent ribosomal translocation step during translation elongation. During this step, the ribosome changes from the pre-translocational (PRE) to the post-translocational (POST) ...
Gene Name
fusA
Uniprot ID
P13551
Uniprot Name
Elongation factor G
Molecular Weight
76878.69 Da
References
  1. Lannergard J, Norstrom T, Hughes D: Genetic determinants of resistance to fusidic acid among clinical bacteremia isolates of Staphylococcus aureus. Antimicrob Agents Chemother. 2009 May;53(5):2059-65. doi: 10.1128/AAC.00871-08. Epub 2009 Mar 16. [Article]
  2. Chen Y, Koripella RK, Sanyal S, Selmer M: Staphylococcus aureus elongation factor G--structure and analysis of a target for fusidic acid. FEBS J. 2010 Sep;277(18):3789-803. doi: 10.1111/j.1742-4658.2010.07780.x. Epub 2010 Aug 13. [Article]
  3. Gao YG, Selmer M, Dunham CM, Weixlbaumer A, Kelley AC, Ramakrishnan V: The structure of the ribosome with elongation factor G trapped in the posttranslocational state. Science. 2009 Oct 30;326(5953):694-9. doi: 10.1126/science.1179709. [Article]
Kind
Protein
Organism
Salmonella typhi
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Chloramphenicol o-acetyltransferase activity
Specific Function
This enzyme is an effector of chloramphenicol resistance in bacteria.
Gene Name
cat
Uniprot ID
P62580
Uniprot Name
Chloramphenicol acetyltransferase
Molecular Weight
25663.08 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. [Article]
  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. [Article]
  3. Murray IA, Cann PA, Day PJ, Derrick JP, Sutcliffe MJ, Shaw WV, Leslie AG: Steroid recognition by chloramphenicol acetyltransferase: engineering and structural analysis of a high affinity fusidic acid binding site. J Mol Biol. 1995 Dec 15;254(5):993-1005. [Article]
  4. Bennett AD, Shaw WV: Resistance to fusidic acid in Escherichia coli mediated by the type I variant of chloramphenicol acetyltransferase. A plasmid-encoded mechanism involving antibiotic binding. Biochem J. 1983 Oct 1;215(1):29-38. [Article]
  5. Day PJ, Murray IA, Shaw WV: Properties of hybrid active sites in oligomeric proteins: kinetic and ligand binding studies with chloramphenicol acetyltransferase trimers. Biochemistry. 1995 May 16;34(19):6416-22. [Article]
Kind
Protein
Organism
Escherichia coli
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Chloramphenicol o-acetyltransferase activity
Specific Function
This enzyme is an effector of chloramphenicol resistance in bacteria.
Gene Name
cat3
Uniprot ID
P00484
Uniprot Name
Chloramphenicol acetyltransferase 3
Molecular Weight
24993.32 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. [Article]
  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. [Article]
  3. Murray IA, Cann PA, Day PJ, Derrick JP, Sutcliffe MJ, Shaw WV, Leslie AG: Steroid recognition by chloramphenicol acetyltransferase: engineering and structural analysis of a high affinity fusidic acid binding site. J Mol Biol. 1995 Dec 15;254(5):993-1005. [Article]
  4. Bennett AD, Shaw WV: Resistance to fusidic acid in Escherichia coli mediated by the type I variant of chloramphenicol acetyltransferase. A plasmid-encoded mechanism involving antibiotic binding. Biochem J. 1983 Oct 1;215(1):29-38. [Article]
  5. Day PJ, Murray IA, Shaw WV: Properties of hybrid active sites in oligomeric proteins: kinetic and ligand binding studies with chloramphenicol acetyltransferase trimers. Biochemistry. 1995 May 16;34(19):6416-22. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Lin XX, Lian GH, Xu Y, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: The potent mechanism-based inactivation of CYP2D6 and CYP3A4 with fusidic acid in in vivo bioaccumulation. Xenobiotica. 2018 Oct;48(10):999-1005. doi: 10.1080/00498254.2017.1390628. Epub 2017 Nov 10. [Article]
  2. Chen D, Lin XX, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: Screening of drug metabolizing enzymes for fusidic acid and its interactions with isoform-selective substrates in vitro. Xenobiotica. 2017 Sep;47(9):778-784. doi: 10.1080/00498254.2016.1230795. Epub 2016 Nov 15. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Lin XX, Lian GH, Xu Y, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: The potent mechanism-based inactivation of CYP2D6 and CYP3A4 with fusidic acid in in vivo bioaccumulation. Xenobiotica. 2018 Oct;48(10):999-1005. doi: 10.1080/00498254.2017.1390628. Epub 2017 Nov 10. [Article]
  2. Chen D, Lin XX, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: Screening of drug metabolizing enzymes for fusidic acid and its interactions with isoform-selective substrates in vitro. Xenobiotica. 2017 Sep;47(9):778-784. doi: 10.1080/00498254.2016.1230795. Epub 2016 Nov 15. [Article]
  3. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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
  1. Bode KA, Donner MG, Leier I, Keppler D: Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate. Biochem Pharmacol. 2002 Jul 1;64(1):151-8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Bode KA, Donner MG, Leier I, Keppler D: Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate. Biochem Pharmacol. 2002 Jul 1;64(1):151-8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]

Drug created on June 13, 2005 13:24 / Updated on September 18, 2021 03:33