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Fusidic acid
Identification
- Name
- Fusidic acid
- Accession Number
- DB02703
- Description
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.
- Associated Conditions
- Bacterial Conjunctivitis
- Skin Infections caused by Corynebacterium minutissimum infection
- Skin Infections caused by Staphylococcus Aureus
- Skin Infections caused by Streptococcus Infection
- Mild Atopic dermatitis
- Mild Dermatitis caused by Staphylococcus aureusis
- Moderate Atopic dermatitis
- Moderate Dermatitis caused by Staphylococcus aureusis
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Enteric bacteria and other eubacteria
- 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 Unlock Additional DataAbametapir 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 Fusidic acid may decrease the excretion rate of Abemaciclib which could result in a higher serum level. Abiraterone The metabolism of Abiraterone can be decreased when combined with Fusidic acid. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Fusidic acid. Acebutolol The metabolism of Acebutolol can be decreased when combined with Fusidic acid. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Fusidic acid. Acetaminophen The metabolism of Fusidic acid can be decreased when combined with Acetaminophen. Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Fusidic acid is combined with Acipimox. Adalimumab The metabolism of Fusidic acid can be increased when combined with Adalimumab. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Take with food. Food reduces irritation.
Products
- Product Ingredients
Ingredient UNII CAS InChI Key Fucidate sodium J7P3696BCQ 751-94-0 HJHVQCXHVMGZNC-JCJNLNMISA-M - International/Other Brands
- Fucidine / Fudic / Taksta
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataFucidin Cream 2% Cream Topical Leo Pharma 1984-12-31 Not applicable Canada 
Fucidin Film Coated Tab 250mg Tablet Oral Leo Pharma 1991-12-31 2009-06-05 Canada Fucidin Intertulle 2% Dressing Topical Leo Pharma 1984-12-31 2004-07-23 Canada Fucidin Leo Sus 246mg/5ml Suspension Oral Leo Pharma 1980-12-31 2004-07-23 Canada Fucidin Ointment 2% Ointment Topical Leo Pharma 1984-12-31 Not applicable Canada Fucithalmic Solution / drops Ophthalmic Amdipharm Limited 2001-08-29 Not applicable Canada Fucithalmic Solution / drops Ophthalmic Amdipharm Limited 2001-08-07 2017-07-17 Canada Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataFucidin 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 Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Fucibet Fusidic acid (2 %) + Betamethasone (0.1 %) Cream Topical Leo Pharma 2018-10-03 Not applicable Canada Fucidin H Fusidic acid (2 %) + Hydrocortisone acetate (1 %) Cream Topical Leo Pharma 1998-11-11 Not applicable Canada Fucidin Leo Injection Kit Fucidate sodium (500 mg) + Sodium phosphate, dibasic (10 ml) Kit Intravenous Leo Pharma 1984-12-31 2004-08-01 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 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)
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
- AHFS Codes
- 52:04.04 — Antibacterials
- 84:04.04 — Antibiotics
- 08:12.28.92 — Other Miscellaneous Antibacterial Agents*
- PDB Entries
- 1q23 / 1qca / 2vuf / 4v5f / 4v5m / 4v5n / 4v7b / 4v8u / 4v9l / 4v9m … show 5 more
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Diabetes Mellitus 1 4 Enrolling by Invitation Treatment Inflammation of the Eyelids 1 4 Terminated Treatment Impetigo 1 3 Completed Treatment Acute acute bacterial skin and skin structure infections 1 3 Completed Treatment Non-Small Cell Lung Carcinoma (NSCLC) 1 3 Terminated Treatment Infected Atopic Dermatitis/Eczema 1 3 Unknown Status Prevention Hypertrophic Scars / Keloid Scars 1 2 Completed Treatment Skin Diseases, Bacterial 1 2 Terminated Treatment Infected Spacers / Prosthetic Joint Infections of Hip / Prosthetic Joint Infections of Knee 1 2, 3 Completed Treatment Refractory Bone or Joint Infections 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Ointment Topical 20 mg/1g Cream Topical 20 MG/G Ointment 20 MG/G Cream Topical Tablet Oral Cream Topical Dressing Topical Kit Intravenous Suspension Oral Ointment Topical Solution / drops Ophthalmic - 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
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available MS/MS Spectrum - Linear Ion Trap , negative LC-MS/MS splash10-05fr-0002900000-512150f35d55c73b9e09 MS/MS Spectrum - Linear Ion Trap , positive LC-MS/MS splash10-004i-0000900000-eecd35dcbd3fede944c2 MS/MS Spectrum - Linear Ion Trap , positive LC-MS/MS splash10-0002-0000900000-4a266f99ada066a14539
Targets
- 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. [PubMed:19289529]
- 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. [PubMed:20718859]
- 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. [PubMed:19833919]
- 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. [PubMed:17139284]
- 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. [PubMed:17016423]
- 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. [PubMed:7500366]
- 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. [PubMed:6354181]
- 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. [PubMed:7756272]
- 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. [PubMed:17139284]
- 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. [PubMed:17016423]
- 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. [PubMed:7500366]
- 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. [PubMed:6354181]
- 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. [PubMed:7756272]
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. [PubMed:29027845]
- 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. [PubMed:27571049]
- 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. [PubMed:29027845]
- 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. [PubMed:27571049]
- 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. [PubMed:27458210]
- 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. [PubMed:27458210]
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. [PubMed:12106615]
- 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. [PubMed:12106615]
- 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. [PubMed:27458210]
- 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. [PubMed:27458210]
Drug created on June 13, 2005 07:24 / Updated on August 10, 2020 08:11
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