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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Fusidic Acid
- Accession Number
- DB02703 (EXPT01507)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed) It acts by inhibiting translocation during protein synthesis.
- Structure
Structure for Fusidic Acid (DB02703)
- Synonyms
- Fucidate
- Fucidin acid
- Fusidate
- Fusidic acid
- Fusidine
- Ramycin
- External IDs
- NSC-56192 / SQ 16,603 / SQ-16603
- Product Ingredients
Ingredient UNII CAS InChI Key Fucidate Sodium J7P3696BCQ 751-94-0 HJHVQCXHVMGZNC-JCJNLNMISA-M - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End 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 Oral Leo Pharma 1980-12-31 2004-07-23 Canada Fucidin Ointment 2% Ointment 2 % Topical Leo Pharma 1984-12-31 Not applicable Canada Fucithalmic Solution / drops 1 % Ophthalmic Amdipharm Limited 2001-08-29 Not applicable Canada Fucithalmic Solution / drops 1 % Ophthalmic Amdipharm Limited 2001-08-07 2017-07-17 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Fucibet Fusidic Acid (2 %) + Betamethasone (0.1 %) Cream Topical Leo Pharma Not applicable 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 - International/Other Brands
- Fucidin / Fucidine / Fudic / Taksta
- Categories
- 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
- Dermatologicals
- Enzyme Inhibitors
- 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
- UNII
- 59XE10C19C
- CAS number
- 6990-06-3
- Weight
- Average: 516.7092
Monoisotopic: 516.345089268 - Chemical Formula
- C31H48O6
- 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-[(1S,2S,5R,6S,7S,10S,11S,13S,14Z,15R,17R)-13-(acetyloxy)-5,17-dihydroxy-2,6,10,11-tetramethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-14-ylidene]-6-methylhept-5-enoic acid
- SMILES
- O[C@@H]1CC[C@@]2(C)[C@@]([H])(CC[C@@]3(C)[C@@]2([H])[C@H](O)C[C@@]2([H])\C([C@@H](OC(=O)C)C[C@]32C)=C(/CCC=C(C)C)C(O)=O)[C@@H]1C
Pharmacology
- Indication
For the treatment of bacterial infections.
- Associated Conditions
- Pharmacodynamics
Fusidic acid is a bacteriostatic antibiotic that is often used topically in creams and eyedrops, but may also be given systemically as tablets or injections.
- 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.
- Route of elimination
- Not Available
- Half life
Approximately 5 to 6 hours in adults.
- Clearance
- Not Available
- Toxicity
- Not Available
- Affected organisms
- Enteric bacteria and other eubacteria
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Fusidic Acid. Abiraterone The serum concentration of Abiraterone can be increased when it is combined with Fusidic Acid. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Fusidic Acid. Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Fusidic Acid. Acetazolamide The metabolism of Fusidic Acid can be decreased when combined with Acetazolamide. Adenine The metabolism of Fusidic Acid can be decreased when combined with Adenine. Adinazolam The serum concentration of Adinazolam can be increased when it is combined with Fusidic Acid. Agmatine The serum concentration of Agmatine can be increased when it is combined with Fusidic Acid. Albendazole The metabolism of Albendazole can be decreased when combined with Fusidic Acid. Alclometasone The metabolism of Alclometasone can be decreased when combined with Fusidic Acid. - Food Interactions
- Take with food to reduce irritation.
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
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015570
- KEGG Drug
- D04281
- KEGG Compound
- C06694
- PubChem Compound
- 3000226
- PubChem Substance
- 46505364
- ChemSpider
- 2271900
- BindingDB
- 58924
- ChEBI
- 29013
- ChEMBL
- CHEMBL374975
- Therapeutic Targets Database
- DAP001008
- PharmGKB
- PA164749648
- HET
- FUA
- Wikipedia
- Fusidic_acid
- ATC Codes
- J01XC01 — Fusidic acid
- J01XC — Steroid antibacterials
- J01X — OTHER ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- D09AA — Medicated dressings with antiinfectives
- D09A — MEDICATED DRESSINGS
- D09 — MEDICATED DRESSINGS
- D — DERMATOLOGICALS
- D06AX — Other antibiotics for topical use
- D06A — ANTIBIOTICS FOR TOPICAL USE
- D06 — ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE
- D — DERMATOLOGICALS
- 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 2 more
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 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 Active Not Recruiting Treatment Refractory Bone or Joint Infections 1 3 Completed Treatment Lung Cancer Non-Small Cell Cancer (NSCLC) 1 3 Recruiting Treatment Infected Atopic Dermatitis/Eczema 1 3 Unknown Status Prevention Hypertrophic Scars / Keloid Scars 1 4 Enrolling by Invitation Treatment Inflammation of the Eyelids 1 4 Terminated Treatment Impetigo 1 Not Available Completed Not Available Impetigo 1 Not Available Recruiting Prevention Motility Disorders / Staphylococcus Aureus 1 Not Available Recruiting Treatment Prosthetic Joint Infection 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
Form Route Strength Cream Topical 2 % Tablet Oral 250 mg Cream Topical Dressing Topical 2 % Kit Intravenous Suspension Oral 246 mg Ointment Topical 2 % Solution / drops Ophthalmic 1 % - 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) 4.66 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 59.77 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
Taxonomy
- 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
- Steroid ester / 3-hydroxysteroid / 3-alpha-hydroxysteroid / 11-hydroxysteroid / 11-alpha-hydroxysteroid / Hydroxysteroid / Medium-chain fatty acid / Branched fatty acid / Methyl-branched fatty acid / Hydroxy fatty acid 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)
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
- Human
- 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
- Human
- 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
- Human
- 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
- Human
- 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
- Human
- 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
- Human
- 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
- Human
- 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 October 16, 2018 08:37