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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
- ácido fusídico
- Fucidate
- Fucidin acid
- Fusidate
- 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 (R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Fusidic Acid. (S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Fusidic Acid. 3,5-diiodothyropropionic acid The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Fusidic Acid. 4-hydroxycoumarin The metabolism of 4-hydroxycoumarin can be decreased when combined with Fusidic Acid. 4-Methoxyamphetamine The metabolism of 4-Methoxyamphetamine can be decreased when combined with Fusidic Acid. 5-androstenedione The metabolism of 5-androstenedione can be decreased when combined with Fusidic Acid. 6-Deoxyerythronolide B The metabolism of Fusidic Acid can be decreased when combined with 6-Deoxyerythronolide B. 6-O-benzylguanine The metabolism of 6-O-benzylguanine can be decreased when combined with Fusidic Acid. Abemaciclib Fusidic Acid may decrease the excretion rate of Abemaciclib which could result in a higher serum level. Abiraterone The metabolism of Fusidic Acid can be decreased when combined with Abiraterone. - 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
- D06AX — Other antibiotics for topical use
- D06A — ANTIBIOTICS FOR TOPICAL USE
- D06 — ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE
- D — DERMATOLOGICALS
- D09AA — Medicated dressings with antiinfectives
- D09A — MEDICATED DRESSINGS
- D09 — MEDICATED DRESSINGS
- 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 November 20, 2018 00:54