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.

Structure

Similar Structures

Synonyms

ácido fusídico
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	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Fucidin Cream 2%	Cream	Topical	Leo Pharma	1984-12-31	Not applicable
Fucidin Film Coated Tab 250mg	Tablet	Oral	Leo Pharma	1991-12-31	2009-06-05
Fucidin Intertulle 2%	Dressing	Topical	Leo Pharma	1984-12-31	2004-07-23
Fucidin Leo Sus 246mg/5ml	Suspension	Oral	Leo Pharma	1980-12-31	2004-07-23
Fucidin Ointment 2%	Ointment	Topical	Leo Pharma	1984-12-31	Not applicable
Fucithalmic	Solution / drops	Ophthalmic	Amdipharm Limited	2001-08-29	Not applicable
Fucithalmic	Solution / drops	Ophthalmic	Amdipharm Limited	2001-08-07	2017-07-17

Additional Data Available

Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Fucidin	Ointment	20 mg/1g	Topical	OASIS TRADING	2018-11-21	Not applicable
Fucidin	Ointment	20 mg/1g	Topical	I World Pharmaceutical Co., Ltd.	2019-10-08	Not applicable
Fucidin	Ointment	20 mg/1g	Topical	Lydia Co., Ltd.	2019-10-08	Not applicable

Additional Data Available

Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Fucibet	Fusidic acid (2 %) + Betamethasone (0.1 %)	Cream	Topical	Leo Pharma	2018-10-03	Not applicable
Fucidin H	Fusidic acid (2 %) + Hydrocortisone acetate (1 %)	Cream	Topical	Leo Pharma	1998-11-11	Not applicable
Fucidin Leo Injection Kit	Fucidate Sodium (500 mg) + Sodium phosphate, dibasic (10 ml)	Kit	Intravenous	Leo Pharma	1984-12-31	2004-08-01

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Fucidin	Fucidate Sodium (20 mg/1g)	Ointment	Topical	OASIS TRADING	2018-11-21	Not applicable
Fucidin	Fucidate Sodium (20 mg/1g)	Ointment	Topical	I World Pharmaceutical Co., Ltd.	2019-10-08	Not applicable
Fucidin	Fucidate Sodium (20 mg/1g)	Ointment	Topical	Lydia Co., Ltd.	2019-10-08	Not applicable

International/Other Brands

Fucidine / Fudic / Taksta

Categories

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 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	inhibitor	Thermus thermophilus
UChloramphenicol acetyltransferase	inhibitor	Salmonella typhi
UChloramphenicol acetyltransferase 3	inhibitor	Escherichia coli

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Additional Data Available

Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available

Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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

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 Data
(R)-warfarin	The serum concentration of (R)-warfarin can be increased when it is combined with Fusidic acid.
(S)-Warfarin	The serum concentration of (S)-Warfarin can be increased when it is combined with Fusidic acid.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine	The metabolism of Fusidic acid can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
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-methoxy-N,N-dimethyltryptamine	The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Fusidic acid.
9-aminocamptothecin	The metabolism of 9-aminocamptothecin 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 Abiraterone can be decreased when combined with Fusidic acid.
Acebutolol	The metabolism of Acebutolol can be decreased when combined with Fusidic acid.

Additional Data Available

Extended Description

Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

A severity rating for each drug interaction, from minor to major.

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Evidence Level

A rating for the strength of the evidence supporting each drug interaction.

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Action

An effect category for each drug interaction. Know how this interaction affects the subject drug.

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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

S01AA13 — Fusidic acid

D09AA02 — Fusidic acid

J01XC01 — Fusidic acid

D06AX01 — 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
0	Not Yet Recruiting	Treatment	Diabetic Foot	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
3	Completed	Treatment	Lung Cancer Non-Small Cell Cancer (NSCLC)	1
3	Completed	Treatment	Acute acute bacterial skin and skin structure infections	1
3	Terminated	Treatment	Infected Atopic Dermatitis/Eczema	1
3	Unknown Status	Prevention	Hypertrophic Scars / Keloid Scars	1
4	Completed	Treatment	Diabetes Mellitus (DM)	1
4	Enrolling by Invitation	Treatment	Inflammation of the Eyelids	1
4	Terminated	Treatment	Impetigo	1
Not Available	Active Not Recruiting	Treatment	Prosthetic Joint Infection	1
Not Available	Completed	Not Available	Impetigo	1
Not Available	Recruiting	Prevention	Motility Disorders / Staphylococcus Aureus	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

Form	Route	Strength
Ointment	Topical	20 mg/1g
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)	4.66	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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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

Details1. Elongation factor G

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]

Details2. Chloramphenicol acetyltransferase

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]

Details3. Chloramphenicol acetyltransferase 3

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

Details1. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Steroid hydroxylase activity
Specific Function: Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name: CYP2D6
Uniprot ID: P10635
Uniprot Name: Cytochrome P450 2D6
Molecular Weight: 55768.94 Da

References

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]

Details2. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

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]

Details3. UDP-glucuronosyltransferase 1-1

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

Details1. Bile salt export pump

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]

Details2. Canalicular multispecific organic anion transporter 1

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]

Details3. ATP-binding cassette sub-family G member 2

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]

Details4. Solute carrier organic anion transporter family member 1B1

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 December 12, 2019 07:27

Fusidic acid

Identification

Structure for Fusidic acid (DB02703)

Pharmacology

Interactions

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

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Enzymes

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Transporters

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