Identification

Summary

Fusidic acidis a topical antibacterial agent used to prevent and treat mild to moderate skin infections caused by susceptible bacteria.

Brand Names
Fucibet, Fucidin, Fucithalmic
Generic Name
Fusidic acid
DrugBank Accession Number
DB02703
Background

An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed) It acts by inhibiting translocation during protein synthesis. It is often used topically in creams and eyedrops but is available in systemic formulations including tablets and injections.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 516.7092
Monoisotopic: 516.345089268
Chemical Formula
C3.1H48O6
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.

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Associated Conditions
Contraindications & Blackbox Warnings
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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 殖器官nism
AElongation factor G
inhibitor
Thermus thermophilus
UChloramphenicol acetyltransferase
inhibitor
Salmonella typhi
UChloramphenicol acetyltransferase 3
inhibitor
Escherichia 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
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction
1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Fusidic acid.
Abametapir The serum concentration of Fusidic acid can be increased when it is combined with Abametapir.
Abatacept The metabolism of Fusidic acid can be increased when combined with Abatacept.
Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Fusidic acid.
Abiraterone The metabolism of Fusidic acid can be decreased when combined with Abiraterone.
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 Acetaminophen can be decreased when combined with Fusidic acid.
Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Fusidic acid is combined with Acipimox.
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Food Interactions
  • Take with food. Food reduces irritation.

Products

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Product Ingredients
Ingredient UNII CAS InChI Key
Fucidate sodium J7P3696BCQ 751-94-0 HJHVQCXHVMGZNC-JCJNLNMISA-M
Fusidic acid hemihydrate W540G73230 172343-30-5 CSXHKOSAWQTJBT-YDYKLMMDSA-N
International/Other Brands
Fucidine/Fudic/Taksta
品牌名称的处方产品
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Fucidin Cream 2% Cream 2 % Topical Leo Pharma 1984-12-31 Not applicable Canada flag
Fucidin Film Coated Tab 250mg Tablet 250 mg Oral Leo Pharma 1991-12-31 2009-06-05 Canada flag
Fucidin Intertulle 2% Dressing 2 % Topical Leo Pharma 1984-12-31 2004-07-23 Canada flag
Fucidin Leo Sus 246mg/5ml 奥sion 246 mg / 5 mL Oral Leo Pharma 1980-12-31 2004-07-23 Canada flag
Fucidin Ointment 2% Ointment 2 % Topical Leo Pharma 1984-12-31 Not applicable Canada flag
Fucithalmic Solution / drops 1 % w/w Ophthalmic Amdipharm Limited 2001-08-07 2017-07-17 Canada flag
Fucithalmic Solution / drops 1 % w/w Ophthalmic Amdipharm Limited 2001-08-29 Not applicable Canada flag
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Taro-fusidic Acid Cream 2 % w/w Topical Taro Pharmaceuticals, Inc. Not applicable Not applicable Canada flag
Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
DIFUSIN Ointment 2 %w/w Topical บริษัท ฟาร์มาแลนด์ (1982) จำกัด 2007-03-20 2020-09-29 Thailand flag
Fucidin Ointment 20 mg/1g Topical Lydia Co., Ltd. 2019-10-08 Not applicable US flag
Fucidin Ointment 20 mg/1g Topical OASIS TRADING 2018-11-21 Not applicable US flag
Fucidin Ointment 20 mg/1g Topical I World Pharmaceutical Co., Ltd. 2019-10-08 Not applicable US flag
ฟิวซิดิน Ointment 2 %w/w Topical บริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด 2010-03-11 Not applicable Thailand flag
ฟิวซิดิน Cream 2 %w/w Topical บริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด 2010-03-11 Not applicable Thailand flag
ลูซิน่าร์ ครีม Cream 2 %w/w Topical บริษัท สหการโอสถ (1996) จำกัด จำกัด 2008-12-21 Not applicable Thailand flag
เจิมมีดิก (ครีม) Cream 2 %w/w Topical บริษัท โรงงานเภสัชกรรมแอตแลนติค จำกัด 2015-10-05 Not applicable Thailand flag
แอ็กเซล ฟูซิดิก แอซิด ครีม Cream 2 %w/w Topical บริษัท ฟาร์มาแลนด์ (1982) จำกัด 2018-03-19 Not applicable Thailand flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
DEFUZIN-B CREAM Fusidic acid(20 mg/g)+Betamethasone(1 mg/g) Cream Topical APEX PHARMA MARKETING PTE. LTD. 2019-05-13 Not applicable
DEFUZIN-B CREAM Fusidic acid(2 % w/w)+Betamethasone valerate(0.1 % w/w) Cream Topical XEPA-SOUL PATTINSON (MALAYSIA) SDN BHD 2020-09-08 Not applicable Malaysia flag
DERMOTRIZOL ® Fusidic acid(2.04 g)+Dexamethasone(0.054 g)+Ketoconazole(2.04 g) Cream Topical COLOMPACK S.A. 2018-05-02 Not applicable Colombia flag
FOBANCORT CREAM Fusidic acid(2 % w/w)+Betamethasone(0.05 % w/w) Cream Topical ZUELLIG PHARMA PTE. LTD. 2001-10-22 Not applicable
FOBANCORT OINTMENT Fucidate sodium(2 % w/w)+Betamethasone dipropionate(0.064 % w/w) Ointment Topical ZUELLIG PHARMA PTE. LTD. 2001-05-10 Not applicable
Fucibet Fusidic acid(2 % w/w)+Betamethasone valerate(0.1 % w/w) Cream Topical Leo Pharma 2018-10-03 Not applicable Canada flag
Fucibet Lipid 20 mg/g + 1 mg/g Creme Fusidic acid(20 mg/g)+Betamethasone(1 mg/g) Cream Topical Leo Pharma 2015-12-30 Not applicable Austria flag
FUCICORT 20 MG/G + 1 MG/G KREM, 30 G Fusidic acid(20 mg/g)+Betamethasone valerate(1 mg/g) Cream Topical ABDİ İBRAHİM İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
FUCICORT CREAM Fusidic acid(20 mg/g)+Betamethasone valerate(1 mg/g) Cream Topical LEO PHARMA ASIA PTE LTD 1988-03-05 Not applicable
FUCICORT(R) Fusidic acid(2 g/100g)+Betamethasone valerate(100 mg/100g) Cream บริษัท ดีเคเอสเอช (ประเทศไทย) จำกัด 2010-03-11 Not applicable Thailand flag
Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
FUCIBEST % 2 20 GR KREM Fusidic acid(2 %) Cream Topical TRİOZER İLAÇ KİM. KOZMETİK SAĞ. HİZM. SAN. VE TİC. LTD. ŞTİ. 2020-08-14 Not applicable Turkey flag
Fucidin Fucidate sodium(20毫克/ 1 g) Ointment Topical Lydia Co., Ltd. 2019-10-08 Not applicable US flag
Fucidin Fucidate sodium(20毫克/ 1 g) Ointment Topical OASIS TRADING 2018-11-21 Not applicable US flag
Fucidin Fucidate sodium(20毫克/ 1 g) Ointment Topical I World Pharmaceutical Co., Ltd. 2019-10-08 Not applicable US flag

Categories

ATC Codes
S01AA13 — Fusidic acid D09AA02 — Fusidic acid J01XC01 — Fusidic acid D06AX01 — Fusidic acid
Drug Categories
Chemical TaxonomyProvided byClassyfire
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
殖器官nic 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
3.alpha-hydroxy steroid, alpha,beta-unsaturated monocarboxylic acid, sterol ester, steroid acid, 11alpha-hydroxy steroid, steroid antibiotic (CHEBI:29013)/Prostostane and fusidane triterpenoids (LMPR0106040001)
Affected organisms
  • Enteric bacteria and other eubacteria

Chemical Identifiers

UNII
59XE10C19C
CAS number
6990-06-3
InChI Key
IECPWNUMDGFDKC-MZJAQBGESA-N
InChI
InChI=1S/C31H48O6/c1-17(2)9-8-10-20(28(35)36)26-22-15-24(34)27-29(5)13-12-23(33)18(3)21(29)11-14-30(27,6)31(22,7)16-25(26)37-19(4)32/h9,18,21-25,27,33-34H,8,10-16H2,1-7H3,(H,35,36)/b26-20-/t18-,21-,22-,23+,24+,25-,27-,29-,30-,31-/m0/s1
IUPAC Name
2-[(1Z,2S,3aS,3bS,5aS,6S,7R,9aS,9bS,10R,11aR)-2-(acetyloxy)-7,10-dihydroxy-3a,3b,6,9a-tetramethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-1-ylidene]-6-methylhept-5-enoic acid
SMILES
[H][C@@]12C[C@@H](O)[C@@]3([H])[C@@]4(C)CC[C@@H](O)[C@@H](C)[C@]4([H])CC[C@]3(C)[C@@]1(C)C[C@H](OC(C)=O)\C2=C(\CCC=C(C)C)C(O)=O

References

Synthesis Reference

Vanangamudi Subramaniam Sulur, Madhavan Srinivasan, Neelakandan Narayanan Chulliel, Haridas Sankar, Selvaraj Balkrishnan, " PROCESS TO MAKE FUSIDIC ACID CREAM." U.S. Patent US20110301138, issued December 08, 2011.

US20110301138
一般引用
  1. Health Canada Product Monograph: Fucidin (fucidic acid) for topical use [Link]
Human Metabolome Database
HMDB0015570
KEGG Drug
D04281
KEGG Compound
C06694
PubChem Compound
3.000226
PubChem Substance
46505364
ChemSpider
2271900
BindingDB
58924
RxNav
113608
ChEBI
29013
ChEMBL
CHEMBL374975
ZINC
ZINC000008143796
Therapeutic Targets Database
DAP001008
PharmGKB
PA164749648
PDBe Ligand
FUA
Wikipedia
Fusidic_acid
PDB Entries
1q23/1qca/2vuf/4v5f/4v5m/4v5n/4v7b/4v8u/4v9l/4v9m
show 12 more

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Completed Treatment Diabetes Mellitus 1
4 Not Yet Recruiting Treatment Infective Endocarditis (IE) 1
4 Terminated Treatment Impetigo 1
4 Unknown Status Treatment Inflammation of the Eyelids 1
3. Completed Treatment Acute Bacterial Skin and Skin Structure Infection (ABSSSI) 1
3. Completed Treatment Non-Small Cell Lung Cancer, Lung Cancer, Cancer 1
3. Terminated Treatment Infected Atopic Dermatitis/Eczema 1
3. Unknown Status Prevention Keloids Scars/Scars, Hypertrophic 1
2 Completed Treatment Bacterial skin infections 1
2 Not Yet Recruiting Treatment Cystic Fibrosis (CF)/Cystic Fibrosis Pulmonary Exacerbation 1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Form Route Strength
Powder, for suspension Oral 5 g
Solution Conjunctival; Ophthalmic 10 mg
Cream Topical 2 g
Cream Topical 2.0 % W/W
Cream Topical 2.00 % w/w
Capsule 250 MG
Ointment Topical 2 %w/w
Cream Topical 2.03 % w/w
Ointment Topical 2.04 % w/w
Cream Topical 2 % w/w
Ointment Topical 2 % w/w
Cream Topical 0.05 % w/w
Ointment Topical
Ointment Topical 20 mg/g
Cream Topical
Cream Topical 0.1 g
Cream Topical 20 MG/G
Ointment Topical 20 mg/1g
Tablet, film coated Oral 250 mg
Tablet, film coated Oral 500 mg
Tablet, film coated Oral
Cream Topical 2 %
Tablet Oral 250 mg
Cream Cutaneous
Cream Topical 20 mg/g
Dressing Topical 2 %
Kit Intravenous
奥sion Oral 246 mg / 5 mL
Ointment Topical 2 %
Tablet Oral
Ointment Topical 2 g
Drug delivery system Topical 3.0 mg
Ointment Topical 20 mg
Cream Topical 2 mg
奥sion / drops Ophthalmic 1 %
Solution / drops Ophthalmic 1 % w/w
Solution / drops Ophthalmic 1 %
Gel Ophthalmic 10 mg/g
Solution Ophthalmic 10 mg/g
奥sion / drops Ophthalmic
奥sion Ophthalmic 10 mg
Ointment Topical
Solution / drops Ophthalmic 1.02 %
Cream Topical 20 mg
Cream Topical
Injection, solution, concentrate Intravenous
Gel Ophthalmic
Solution / drops Ophthalmic
Solution / drops Ophthalmic 50 mg
Injection Intravenous 500 mg
Pill
Tablet, coated Oral
奥sion Topical 20 mg
Injection, solution Intravenous
Cream
Tablet, coated Oral 250 mg
Cream Topical 2 %w/w
Prices
Unit description Cost Unit
Fucidin 2 % Cream 0.66USD g
Fucidin 2 % Ointment 0.66USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 192.5 °C PhysProp
pKa 5.35 MERCK INDEX (1996)
Predicted Properties
Property Value Source
Water Solubility 0.00521 mg/mL ALOGPS
logP 4.97 ALOGPS
logP 4.42 Chemaxon
logS -5 ALOGPS
pKa (Strongest Acidic) 4.46 Chemaxon
pKa (Strongest Basic) -0.2 Chemaxon
Physiological Charge -1 Chemaxon
Hydrogen Acceptor Count 5 Chemaxon
Hydrogen Donor Count 3. Chemaxon
Polar Surface Area 104.06 Å2 Chemaxon
Rotatable Bond Count 6 Chemaxon
Refractivity 144.12 m3.·mol-1 Chemaxon
Polarizability 59.76 Å3. Chemaxon
Number of Rings 4 Chemaxon
Bioavailability 1 Chemaxon
Rule of Five No Chemaxon
Ghose Filter No Chemaxon
Veber's Rule No Chemaxon
MDDR-like Rule Yes Chemaxon
Predicted ADMET Features
Property Value Probability
Human Intestinal Absorption + 0.9691
Blood Brain Barrier + 0.7909
Caco-2 permeable - 0.6089
P-glycoprotein substrate Substrate 0.8165
我22抑制剂 Non-inhibitor 0.6004
我22抑制剂I 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 usingadmetSAR, 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

Targets

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insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
殖器官nism
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
分子量
76878.69 Da
References
  1. Lannergard J, Norstrom T, Hughes D: Genetic determinants of resistance to fusidic acid among clinical bacteremia isolates of Staphylococcus aureus. Antimicrob Agents Chemother. 2009 May;53(5):2059-65. doi: 10.1128/AAC.00871-08. Epub 2009 Mar 16. [Article]
  2. Chen Y, Koripella RK, Sanyal S, Selmer M: Staphylococcus aureus elongation factor G--structure and analysis of a target for fusidic acid. FEBS J. 2010 Sep;277(18):3789-803. doi: 10.1111/j.1742-4658.2010.07780.x. Epub 2010 Aug 13. [Article]
  3. Gao YG, Selmer M, Dunham CM, Weixlbaumer A, Kelley AC, Ramakrishnan V: The structure of the ribosome with elongation factor G trapped in the posttranslocational state. Science. 2009 Oct 30;326(5953):694-9. doi: 10.1126/science.1179709. [Article]
Kind
Protein
殖器官nism
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
分子量
25663.08 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Murray IA, Cann PA, Day PJ, Derrick JP, Sutcliffe MJ, Shaw WV, Leslie AG: Steroid recognition by chloramphenicol acetyltransferase: engineering and structural analysis of a high affinity fusidic acid binding site. J Mol Biol. 1995 Dec 15;254(5):993-1005. [Article]
  4. Bennett AD, Shaw WV: Resistance to fusidic acid in Escherichia coli mediated by the type I variant of chloramphenicol acetyltransferase. A plasmid-encoded mechanism involving antibiotic binding. Biochem J. 1983 Oct 1;215(1):29-38. [Article]
  5. Day PJ, Murray IA, Shaw WV: Properties of hybrid active sites in oligomeric proteins: kinetic and ligand binding studies with chloramphenicol acetyltransferase trimers. Biochemistry. 1995 May 16;34(19):6416-22. [Article]
Kind
Protein
殖器官nism
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
分子量
24993.32 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Murray IA, Cann PA, Day PJ, Derrick JP, Sutcliffe MJ, Shaw WV, Leslie AG: Steroid recognition by chloramphenicol acetyltransferase: engineering and structural analysis of a high affinity fusidic acid binding site. J Mol Biol. 1995 Dec 15;254(5):993-1005. [Article]
  4. Bennett AD, Shaw WV: Resistance to fusidic acid in Escherichia coli mediated by the type I variant of chloramphenicol acetyltransferase. A plasmid-encoded mechanism involving antibiotic binding. Biochem J. 1983 Oct 1;215(1):29-38. [Article]
  5. Day PJ, Murray IA, Shaw WV: Properties of hybrid active sites in oligomeric proteins: kinetic and ligand binding studies with chloramphenicol acetyltransferase trimers. Biochemistry. 1995 May 16;34(19):6416-22. [Article]

Enzymes

Kind
Protein
殖器官nism
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
分子量
55768.94 Da
References
  1. Lin XX, Lian GH, Xu Y, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: The potent mechanism-based inactivation of CYP2D6 and CYP3A4 with fusidic acid in in vivo bioaccumulation. Xenobiotica. 2018 Oct;48(10):999-1005. doi: 10.1080/00498254.2017.1390628. Epub 2017 Nov 10. [Article]
  2. Chen D, Lin XX, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: Screening of drug metabolizing enzymes for fusidic acid and its interactions with isoform-selective substrates in vitro. Xenobiotica. 2017 Sep;47(9):778-784. doi: 10.1080/00498254.2016.1230795. Epub 2016 Nov 15. [Article]
Kind
Protein
殖器官nism
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
分子量
57342.67 Da
References
  1. Lin XX, Lian GH, Xu Y, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: The potent mechanism-based inactivation of CYP2D6 and CYP3A4 with fusidic acid in in vivo bioaccumulation. Xenobiotica. 2018 Oct;48(10):999-1005. doi: 10.1080/00498254.2017.1390628. Epub 2017 Nov 10. [Article]
  2. Chen D, Lin XX, Zhao Q, Xiao J, Peng SF, Xiao MF, Ouyang DS, Tan ZR, Wang YC, Peng JB, Zhang W, Chen Y: Screening of drug metabolizing enzymes for fusidic acid and its interactions with isoform-selective substrates in vitro. Xenobiotica. 2017 Sep;47(9):778-784. doi: 10.1080/00498254.2016.1230795. Epub 2016 Nov 15. [Article]
  3. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]
Kind
Protein
殖器官nism
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
分子量
59590.91 Da
References
  1. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]

Transporters

Kind
Protein
殖器官nism
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
分子量
146405.83 Da
References
  1. Bode KA, Donner MG, Leier I, Keppler D: Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate. Biochem Pharmacol. 2002 Jul 1;64(1):151-8. [Article]
Kind
Protein
殖器官nism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
有机离子跨膜转运体活动
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
分子量
174205.64 Da
References
  1. Bode KA, Donner MG, Leier I, Keppler D: Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate. Biochem Pharmacol. 2002 Jul 1;64(1):151-8. [Article]
Kind
Protein
殖器官nism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
高容量尿酸盐出口国r功能enal 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
分子量
72313.47 Da
References
  1. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]
Kind
Protein
殖器官nism
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
分子量
76447.99 Da
References
  1. Gupta A, Harris JJ, Lin J, Bulgarelli JP, Birmingham BK, Grimm SW: Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94. doi: 10.1128/AAC.01335-16. Print 2016 Oct. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 19, 2023 09:30