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
Structure for Fusidic acid (DB02703)
- 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.
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 Bacterial conjunctivitis •••••••••••• •••••••• • ••••• Treatment of Bacterial conjunctivitis •••••••••••• •••••••••• Treatment of Eye and eyelid infections •••••••••••• •••••••• • ••••• Used in combination to treat Fungal skin infection Combination Product in combination with: Ketoconazole (DB01026), Dexamethasone (DB01234) ••• ••• ••••• Treatment of Skin infections caused by corynebacterium minutissimum infection •••••••••••• •••••• •••••••• - 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
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.
Target Actions Organism AElongation factor G inhibitorThermus thermophilus UChloramphenicol acetyltransferase inhibitorSalmonella typhi UChloramphenicol acetyltransferase 3 inhibitorEscherichia 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
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
Not Available
- 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 software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Fusidic acid. Abametapir The serum concentration of Fusidic acid can be increased when it is combined with Abametapir. Abatacept The metabolism of Fusidic acid can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Fusidic acid. Abiraterone The metabolism of Fusidic acid can be decreased when combined with Abiraterone. - Food Interactions
- Take with food. Food reduces irritation.
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 Fucidate sodium J7P3696BCQ 751-94-0 HJHVQCXHVMGZNC-JCJNLNMISA-M Fusidic acid hemihydrate W540G73230 172343-30-5 CSXHKOSAWQTJBT-YDYKLMMDSA-N - International/Other Brands
- Fucidine / Fudic / Taksta
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fucidin Cream 2% Cream 2 % Topical Leo Pharma 1984-12-31 Not applicable Canada 
Fucidin Film Coated Tab 250mg Tablet 250 mg Oral Leo Pharma 1991-12-31 2009-06-05 Canada Fucidin Intertulle 2% Dressing 2 % Topical Leo Pharma 1984-12-31 2004-07-23 Canada Fucidin Leo Sus 246mg/5ml Suspension 246 mg / 5 mL Oral Leo Pharma 1980-12-31 2004-07-23 Canada Fucidin Ointment 2% Ointment 2 % Topical Leo Pharma 1984-12-31 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Taro-fusidic Acid Cream 2 % w/w Topical Taro Pharmaceuticals, Inc. Not applicable Not applicable Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image DIFUSIN Ointment 2 %w/w Topical บริษัท ฟาร์มาแลนด์ (1982) จำกัด 2007-03-20 2020-09-29 Thailand 
Fucidin Ointment 20 mg/1g Topical OASIS TRADING 2018-11-21 Not applicable US 
Fucidin Ointment 20 mg/1g Topical I World Pharmaceutical Co., Ltd. 2019-10-08 Not applicable US Fucidin Ointment 20 mg/1g Topical Lydia Co., Ltd. 2019-10-08 Not applicable US ฟิวซิดิน Ointment 2 %w/w Topical บริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด 2010-03-11 Not applicable Thailand - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image DEFUZIN-B CREAM Fusidic acid (20 mg/g) + Betamethasone (1 mg/g) Cream Topical APEX PHARMA MARKETING PTE. LTD. 2019-05-13 Not applicable Singapore 
DEFUZIN-B CREAM Fusidic acid (2 % w/w) + Betamethasone valerate (0.1 % w/w) Cream Topical XEPA-SOUL PATTINSON (MALAYSIA) SDN BHD 2020-09-08 Not applicable Malaysia 
DERMOMYCIN CORT Fusidic acid (2 %) + Triamcinolone (0.03 %) Cream Topical Alfasigma s.p.a. 2014-10-06 2023-02-23 Italy 
DERMOMYCIN CORT Fusidic acid (2 g/100g) + Triamcinolone (0.03 g/100g) Cream Topical Alfasigma s.p.a. 2014-07-08 2022-05-20 Italy DERMOMYCIN CORT Fusidic acid (2 %) + Triamcinolone (0.03 %) Cream Topical Alfasigma s.p.a. 2014-07-08 2023-02-23 Italy - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image FUCIBEST % 2 20 GR KREM Fusidic acid (2 %) Cream Topical TRİOZER İLAÇ KİM. KOZMETİK SAĞ. HİZM. SAN. VE TİC. LTD. ŞTİ. 2020-08-14 Not applicable Turkey 
Fucidin Fucidate sodium (20 mg/1g) Ointment Topical OASIS TRADING 2018-11-21 Not applicable US Fucidin Fucidate sodium (20 mg/1g) Ointment Topical I World Pharmaceutical Co., Ltd. 2019-10-08 Not applicable US Fucidin Fucidate sodium (20 mg/1g) Ointment Topical Lydia Co., Ltd. 2019-10-08 Not applicable US
Categories
- ATC Codes
- S01AA13 — Fusidic acidD09AA02 — Fusidic acid
- D09AA — Medicated dressings with antiinfectives
- D09A — MEDICATED DRESSINGS
- D09 — MEDICATED DRESSINGS
- D — DERMATOLOGICALS
- J01XC — Steroid antibacterials
- J01X — OTHER ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Agents Causing Muscle Toxicity
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antibiotics for Topical Use
- Antiinfectives for Systemic Use
- BCRP/ABCG2 Inhibitors
- BSEP/ABCB11 Inhibitors
- Cholestadienes
- Cholestadienols
- Cholestanes
- Cholestenes
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (moderate)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dermatologicals
- Enzyme Inhibitors
- Fused-Ring Compounds
- Lipids
- Medicated Dressings
- Medicated Dressings With Antiinfectives
- Membrane Lipids
- OATP1B1/SLCO1B1 Inhibitors
- Ophthalmologicals
- Other Miscellaneous Antibacterial Agents
- Protein Synthesis Inhibitors
- Sensory Organs
- Steroid Antibacterials
- Steroids
- Sterols
- UGT1A1 Substrates
- 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
- Health Canada Product Monograph: Fucidin (fucidic acid) for topical use [Link]
- External Links
- Human Metabolome Database
- HMDB0015570
- KEGG Drug
- D04281
- KEGG Compound
- C06694
- PubChem Compound
- 3000226
- PubChem Substance
- 46505364
- ChemSpider
- 2271900
- BindingDB
- 58924
- 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 12 more
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 Completed Treatment Diabetes Mellitus 1 4 Not Yet Recruiting Treatment Infective Endocarditis (IE) 1 4 Terminated Treatment Impetigo 1 4 Unknown Status Treatment Inflammation of the Eyelids 1 3 Completed Treatment Acute Bacterial Skin and Skin Structure Infection (ABSSSI) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Cream Cutaneous 2.000 g Powder, for suspension Oral 5 g Solution Conjunctival; Ophthalmic 10 mg Cream Topical 2 g Cream Topical 20.000 mg Cream Topical 2.0 % W/W Cream Topical 2.00 % w/w Capsule 250 MG Ointment Topical 2 %w/w Cream Topical 2.03 % w/w Ointment Topical 2.04 % w/w Cream Topical 2 % w/w Ointment Topical 2 % w/w Cream Topical 0.05 % w/w Ointment Topical Ointment Topical 20 mg/g Cream Topical Cream Topical 20 MG/G Ointment Topical 20 mg/1g Tablet, film coated Oral 500 mg Tablet, film coated Oral Cream Topical 2 % Tablet Oral 250 mg Cream Cutaneous Cream Topical 20 mg/g Dressing Topical 2 % Kit Intravenous Suspension Oral 246 mg / 5 mL Ointment Topical 2 % Tablet, film coated Oral 250 mg Tablet Oral Ointment Topical 200000 g Drug delivery system Topical 30 mg Ointment Topical 20 mg Cream Topical 2 mg Suspension / drops Ophthalmic 1 % Solution / drops Ophthalmic 1 % Solution / drops Ophthalmic 1 % w/w Gel Ophthalmic 10 mg/g Solution Ophthalmic 10 mg/g Suspension / drops Ophthalmic Suspension Ophthalmic 10 mg Ointment Topical Cream Topical 200000 g Solution / drops Ophthalmic 1.02 % Cream Topical 20 mg Cream Topical Injection, solution, concentrate Intravenous 500 mg Gel Ophthalmic Solution / drops Ophthalmic Solution / drops Ophthalmic 50 mg Injection Intravenous 500 mg Pill Tablet, coated Oral Cream Topical 200000 g Suspension Topical 20 mg Ointment Topical 2 g Injection, solution Intravenous Cream Tablet, coated Oral 250 mg Cream Topical 2 %w/w - Prices
Unit description Cost Unit Fucidin 2 % Cream 0.66USD g Fucidin 2 % Ointment 0.66USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 192.5 °C PhysProp pKa 5.35 MERCK INDEX (1996) - Predicted Properties
Property Value Source Water Solubility 0.00521 mg/mL ALOGPS logP 4.97 ALOGPS logP 4.42 Chemaxon logS -5 ALOGPS pKa (Strongest Acidic) 4.46 Chemaxon pKa (Strongest Basic) -0.2 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 104.06 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 144.12 m3·mol-1 Chemaxon Polarizability 59.76 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9691 Blood Brain Barrier + 0.7909 Caco-2 permeable - 0.6089 P-glycoprotein substrate Substrate 0.8165 P-glycoprotein inhibitor I Non-inhibitor 0.6004 P-glycoprotein inhibitor II Inhibitor 0.7848 Renal organic cation transporter Non-inhibitor 0.8424 CYP450 2C9 substrate Non-substrate 0.8218 CYP450 2D6 substrate Non-substrate 0.9349 CYP450 3A4 substrate Substrate 0.798 CYP450 1A2 substrate Non-inhibitor 0.9337 CYP450 2C9 inhibitor Non-inhibitor 0.8834 CYP450 2D6 inhibitor Non-inhibitor 0.9544 CYP450 2C19 inhibitor Non-inhibitor 0.9347 CYP450 3A4 inhibitor Non-inhibitor 0.76 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.819 Ames test Non AMES toxic 0.8305 Carcinogenicity Non-carcinogens 0.9508 Biodegradation Not ready biodegradable 0.9753 Rat acute toxicity 3.5929 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9403 hERG inhibition (predictor II) Non-inhibitor 0.7564
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 242.0565122 predictedDarkChem Lite v0.1.0 [M-H]- 238.2484122 predictedDarkChem Lite v0.1.0 [M-H]- 240.2576122 predictedDarkChem Lite v0.1.0 [M-H]- 220.94836 predictedDeepCCS 1.0 (2019) [M+H]+ 240.9700122 predictedDarkChem Lite v0.1.0 [M+H]+ 237.4734122 predictedDarkChem Lite v0.1.0 [M+H]+ 242.7799122 predictedDarkChem Lite v0.1.0 [M+H]+ 222.67207 predictedDeepCCS 1.0 (2019) [M+Na]+ 242.6267122 predictedDarkChem Lite v0.1.0 [M+Na]+ 238.2524122 predictedDarkChem Lite v0.1.0 [M+Na]+ 240.8806122 predictedDarkChem Lite v0.1.0 [M+Na]+ 229.00102 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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
- SubstrateInhibitor
- 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
- 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]
- 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
- SubstrateInhibitor
- 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
- 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]
- 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]
- 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
- 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
- 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
- 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
- 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
- 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 at June 13, 2005 13:24 / Updated at February 20, 2024 23:54