Identification

Name
Clofazimine
Accession Number
DB00845
Description

Clofazimine is a highly lipophilic antimicrobial riminophenazine dye used in combination with other agents, such as dapsone, for the treatment of leprosy. It was originally described in 1957 and was the prototypical riminophenazine dye - a bright-red dye that, in its clinical use, results in long-lasting discoloration of the skin and bodily fluids.2 Although it carries in vitro activity against other mycobacterium, such as Mycobacterium tuberculosis, it is generally considered an ineffective treatment in comparison to classic tuberculosis treatments such as rifampicin and isoniazid.2

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 473.396
Monoisotopic: 472.122152138
Chemical Formula
C27H22Cl2N4
Synonyms
  • Clofazimin
  • Clofazimina
  • Clofazimine
  • Clofaziminum
  • Riminophenazine
External IDs
  • B 663
  • G 30320
  • G-30320
  • NSC 141046
  • NSC-141046

Pharmacology

Indication

Clofazimine is indicated for the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum.5 To prevent the development of drug resistance, it should be used only in combination with other antimycobacterial leprosy treatments.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Clofazimine exerts a slow bactericidal effect on Mycobacterium leprae (Hansen's bacillus) due primarily to its action on the bacterial outer membrane, though there is some evidence that activity on the bacterial respiratory chain and ion transporters may play a role.2 It also exerts anti-inflammatory properties due to the suppression of T-lymphocyte activity. Clofazimine has a relatively long duration of action owing to its long residence time in the body, but is still administered daily.

Approximately 75-100% of patients receiving clofazimine will experience an orange-pink to brownish-black discoloration of the skin, conjunctivae, and bodily fluids.5 Skin discoloration may take several months or years to reverse following the cessation of therapy. Clofazimine has also been implicated in abdominal obstruction, in some cases fatal, due to the deposition of drug and formation of crystals in the intestinal mucosa - complaints of abdominal pain and nausea/vomiting should be investigated promptly, and the doses of clofazimine should be lowered or discontinued if it is found to be the culprit.5

Its use should be avoided in patients with hepatic dysfunction.5

Mechanism of action

Although the precise mechanism(s) of action of clofazimine have not been elucidated, its antimicrobial activity appears to be membrane-directed. It was previously thought that, due to its lipophilicity, clofazimine participated in the generation of intracellular reactive oxygen species (ROS) via redox cycling, specifically H2O2 and superoxide, which then exerted an antimicrobial effect.2 A more recent and compelling theory involves clofazimine interacting with bacterial membrane phospholipids to generate antimicrobial lysophospholipids - bactericidal efficacy may, then, arise from the combined membrane-destabilizing effects of both clofazimine and lysophospholipids, which interfere with K+ uptake and, ultimately, ATP production.2,5

The anti-inflammatory activity of clofazimine is the result of its inhibition of T-lymphocyte activation and proliferation.5 Several mechanisms have been proposed, including direct antagonism of T-cell Kv 1.3 potassium channels and indirect action by promoting the release of E-series prostaglandins and reactive oxygen species from bystander neutrophils and monocytes.

TargetActionsOrganism
UPeroxisome proliferator-activated receptor gamma
modulator
Humans
UPotassium voltage-gated channel subfamily A member 3
antagonist
Humans
Absorption

Absorption varies from 45 to 62% following oral administration in leprosy patients.5 Co-administration of a 200mg dose of clofazimine with food resulted in a Cmax of 0.41 mg/L with a Tmax of 8 h; administered in a fasting state, the corresponding Cmax was 30% lower while the time to Cmax was 12 h.4

Volume of distribution

Clofazimine is highly lipophilic and therefore deposits primarily in fatty tissues and cells of the reticuloendothelial system, where it is taken up by macrophages and further distributed throughout the body. Crystalized deposits have been found in the mesenteric lymph nodes, adrenals, subcutaneous fat, liver, bile, gall bladder, spleen, small intestine, muscles, bones, and skin.5

Protein binding

Clofazimine is bound primarily to beta-lipoproteins (and, to a lesser extent, alpha-lipoproteins) in the serum. This binding was saturable at concentrations of ~10 µg/mL. Binding to gamma-globulin and albumin is negligible.5

Metabolism

Three metabolites have been identified in the urine following repeated oral doses of clofazimine.5 It is unclear whether these metabolites are pharmacologically active. Metabolite I may be the result of the hydrolytic dehalogenation of clofazimine and metabolite II presumably is formed by a hydrolytic deamination reaction followed by glucuronidation.4

Route of elimination

Part of an ingested dose of clofazimine is found in the feces, which may represent excretion in the bile, and a small amount is also eliminated in the sputum, sebum, and sweat.5 Excretion of unchanged drug and metabolites in a 24-hour urine collection was negligible.

Half-life

The mean elimination half-life is approximately 25 days.5

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

The reported oral LD50 of clofazimine in rats and mice is 8400 mg/kg and >5000 mg/kg, respectively.6

No specific data are available regarding the treatment of clofazimine overdosage.5 In cases of overdose consider gastrointestinal decontamination via gastric lavage or induced vomiting. Employ symptomatic and supportive measures as clinically indicated.

Affected organisms
  • Mycobacteria
  • Mycobacterium leprae
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.
DrugInteraction
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Clofazimine.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Clofazimine.
AcebutololThe risk or severity of QTc prolongation can be increased when Clofazimine is combined with Acebutolol.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Clofazimine.
AcrivastineThe risk or severity of QTc prolongation can be increased when Clofazimine is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Clofazimine is combined with Adenosine.
AjmalineThe risk or severity of QTc prolongation can be increased when Clofazimine is combined with Ajmaline.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Clofazimine.
AlectinibThe metabolism of Alectinib can be decreased when combined with Clofazimine.
AlfentanilThe metabolism of Alfentanil can be decreased when combined with Clofazimine.
Additional Data Available
  • Extended Description
    Extended Description

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

    Learn more
  • Severity
    Severity

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

    Learn more
  • Evidence Level
    Evidence Level

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

    Learn more
  • Action
    Action

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

    Learn more
Food Interactions
  • Take with food. Prescribing information for clofazimine recommends its administration with a meal.

Products

International/Other Brands
Clofozine (AstraZeneca) / Hansepran (Abbott) / Lamcoin (Pond's Chemical) / Lampren (Novartis) / Lamprène (Novartis)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LampreneCapsule, gelatin coated50 mg/1OralNovartis Pharmaceuticals Corporation1986-12-152009-12-15Us
Additional Data Available
  • Application Number
    Application Number

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

    Learn more
  • Product Code
    Product Code

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

    Learn more

Categories

ATC Codes
J04BA01 — Clofazimine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenazines and derivatives. These are polycyclic aromatic compounds containing a phenazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a pyrazine ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazanaphthalenes
Sub Class
Benzodiazines
Direct Parent
Phenazines and derivatives
Alternative Parents
Aniline and substituted anilines / Chlorobenzenes / Pyrazines / Aryl chlorides / Secondary ketimines / Heteroaromatic compounds / Secondary amines / Azacyclic compounds / Organopnictogen compounds / Organochlorides
show 1 more
Substituents
Amine / Aniline or substituted anilines / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Chlorobenzene / Halobenzene / Heteroaromatic compound
show 11 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
phenazines, monochlorobenzenes (CHEBI:3749)

Chemical Identifiers

UNII
D959AE5USF
CAS number
2030-63-9
InChI Key
WDQPAMHFFCXSNU-BGABXYSRSA-N
InChI
InChI=1S/C27H22Cl2N4/c1-17(2)30-24-16-27-25(15-23(24)31-20-11-7-18(28)8-12-20)32-22-5-3-4-6-26(22)33(27)21-13-9-19(29)10-14-21/h3-17,31H,1-2H3/b30-24+
IUPAC Name
N,5-bis(4-chlorophenyl)-3-[(propan-2-yl)imino]-3,5-dihydrophenazin-2-amine
SMILES
CC(C)N=C1C=C2N(C3=CC=C(Cl)C=C3)C3=C(C=CC=C3)N=C2C=C1NC1=CC=C(Cl)C=C1

References

General References
  1. Kumar H, Chattopadhyay S, Das N, Shree S, Patel D, Mohapatra J, Gurjar A, Kushwaha S, Singh AK, Dubey S, Lata K, Kushwaha R, Mohammed R, Dastidar KG, Yadav N, Vishwakarma AL, Gayen JR, Bandyopadhyay S, Chatterjee A, Jain MR, Tripathi AK, Trivedi AK, Chattopadhyay N, Ramachandran R, Sanyal S: Leprosy drug clofazimine activates peroxisome proliferator-activated receptor-gamma and synergizes with imatinib to inhibit chronic myeloid leukemia cells. Haematologica. 2020 Apr;105(4):971-986. doi: 10.3324/haematol.2018.194910. Epub 2019 Aug 1. [PubMed:31371410]
  2. Cholo MC, Steel HC, Fourie PB, Germishuizen WA, Anderson R: Clofazimine: current status and future prospects. J Antimicrob Chemother. 2012 Feb;67(2):290-8. doi: 10.1093/jac/dkr444. Epub 2011 Oct 20. [PubMed:22020137]
  3. Te Brake LH, Russel FG, van den Heuvel JJ, de Knegt GJ, de Steenwinkel JE, Burger DM, Aarnoutse RE, Koenderink JB: Inhibitory potential of tuberculosis drugs on ATP-binding cassette drug transporters. Tuberculosis (Edinb). 2016 Jan;96:150-7. doi: 10.1016/j.tube.2015.08.004. Epub 2015 Oct 9. [PubMed:26682943]
  4. Feng PC, Fenselau CC, Jacobson RR: Metabolism of clofazimine in leprosy patients. Drug Metab Dispos. 1981 Nov-Dec;9(6):521-4. [PubMed:6120809]
  5. FDA Approved Drug Products: Lamprene (clofazimine) oral capsules [Link]
  6. CaymanChem: Clofazimine MSDS [Link]
KEGG Drug
D00278
KEGG Compound
C06915
PubChem Compound
2794
PubChem Substance
46508174
ChemSpider
2692
BindingDB
50378783
RxNav
2592
ChEBI
3749
ChEMBL
CHEMBL1292
ZINC
ZINC000100037101
Therapeutic Targets Database
DAP000789
PharmGKB
PA164748759
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Clofazimine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionBorderline Lepromatous Leprosy / Leprosy, Lepromatous1
4CompletedTreatmentHansen's Disease1
4WithdrawnTreatmentCrohn's Disease (CD)1
3Active Not RecruitingTreatmentMulti-Drug Resistant Tuberculosis1
3CompletedTreatmentCrohn's Disease (CD)1
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Infection, Mycobacterium Avium-Intracellulare1
3RecruitingTreatmentBacterial Infections / Infections, Gram-Positive Bacterial / Mycobacterial Infections / Pulmonary Tuberculoses / Tuberculosis (TB) / Tuberculosis, Multidrug Resistant1
3RecruitingTreatmentBacterial Infections / Pulmonary Tuberculoses / Tuberculosis, Multidrug Resistant1
3RecruitingTreatmentExtensively Drug Resistant Tuberculosis / Multi Drug Resistant Tuberculosis / Pre-XDR-TB / Rifampicin Resistant Tuberculosis / Tuberculosis (TB)1
3WithdrawnTreatmentTuberculosis, Multidrug Resistant1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
Packagers
  • Ciba Geigy Ltd.
  • Novartis AG
  • Physicians Total Care Inc.
  • Professional Co.
  • R.P. Scherer GmbH and Co. KG
Dosage Forms
FormRouteStrength
CapsuleOral
Capsule, gelatin coatedOral50 mg/1
Prices
Unit descriptionCostUnit
Clofazimine powder187.2USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)210-212 °CPhysProp
water solubility0.225 mg/L (virtually insoluble)Not Available
logP7.66QUIGLEY,JM ET AL. (1990)
pKa8.51QUIGLEY,JM ET AL. (1990)
Predicted Properties
PropertyValueSource
Water Solubility0.00151 mg/mLALOGPS
logP7.39ALOGPS
logP7.3ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)16.15ChemAxon
pKa (Strongest Basic)9.29ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area39.99 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity142.55 m3·mol-1ChemAxon
Polarizability51.52 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9881
Blood Brain Barrier+0.7616
Caco-2 permeable+0.6769
P-glycoprotein substrateNon-substrate0.5905
P-glycoprotein inhibitor IInhibitor0.642
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterNon-inhibitor0.6719
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6032
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9292
Ames testAMES toxic0.649
CarcinogenicityNon-carcinogens0.7244
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.7821 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9805
hERG inhibition (predictor II)Inhibitor0.5826
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00fr-0000900000-e6674066d4ff0d54220f

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Modulator
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE...
Gene Name
PPARG
Uniprot ID
P37231
Uniprot Name
Peroxisome proliferator-activated receptor gamma
Molecular Weight
57619.58 Da
References
  1. Kumar H, Chattopadhyay S, Das N, Shree S, Patel D, Mohapatra J, Gurjar A, Kushwaha S, Singh AK, Dubey S, Lata K, Kushwaha R, Mohammed R, Dastidar KG, Yadav N, Vishwakarma AL, Gayen JR, Bandyopadhyay S, Chatterjee A, Jain MR, Tripathi AK, Trivedi AK, Chattopadhyay N, Ramachandran R, Sanyal S: Leprosy drug clofazimine activates peroxisome proliferator-activated receptor-gamma and synergizes with imatinib to inhibit chronic myeloid leukemia cells. Haematologica. 2020 Apr;105(4):971-986. doi: 10.3324/haematol.2018.194910. Epub 2019 Aug 1. [PubMed:31371410]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated ion channel activity
Specific Function
Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein form...
Gene Name
KCNA3
Uniprot ID
P22001
Uniprot Name
Potassium voltage-gated channel subfamily A member 3
Molecular Weight
63841.09 Da
References
  1. Cholo MC, Steel HC, Fourie PB, Germishuizen WA, Anderson R: Clofazimine: current status and future prospects. J Antimicrob Chemother. 2012 Feb;67(2):290-8. doi: 10.1093/jac/dkr444. Epub 2011 Oct 20. [PubMed:22020137]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
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
  1. Horita Y, Doi N: Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein. Antimicrob Agents Chemother. 2014 Jun;58(6):3168-76. doi: 10.1128/AAC.02278-13. Epub 2014 Mar 24. [PubMed:24663015]
  2. Sangana R, Gu H, Chun DY, Einolf HJ: Evaluation of Clinical Drug Interaction Potential of Clofazimine Using Static and Dynamic Modeling Approaches. Drug Metab Dispos. 2018 Jan;46(1):26-32. doi: 10.1124/dmd.117.077834. Epub 2017 Oct 16. [PubMed:29038231]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Based on in vitro findings.
General Function
Oxygen binding
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 oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. FDA Approved Drug Products: Lamprene (clofazimine) oral capsules [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Based on in vitro findings.
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. FDA Approved Drug Products: Lamprene (clofazimine) oral capsules [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Based on in vitro findings.
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
  1. FDA Approved Drug Products: Lamprene (clofazimine) oral capsules [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
Curator comments
Binding is negligible.
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: Lamprene (clofazimine) oral capsules [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
P-gp inhibition has been observed in human lung cancer cells and erythroleukemia cells, but no effect was observed in human P-gp-expressing MDCK cells.
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Horita Y, Doi N: Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein. Antimicrob Agents Chemother. 2014 Jun;58(6):3168-76. doi: 10.1128/AAC.02278-13. Epub 2014 Mar 24. [PubMed:24663015]
  2. Te Brake LH, Russel FG, van den Heuvel JJ, de Knegt GJ, de Steenwinkel JE, Burger DM, Aarnoutse RE, Koenderink JB: Inhibitory potential of tuberculosis drugs on ATP-binding cassette drug transporters. Tuberculosis (Edinb). 2016 Jan;96:150-7. doi: 10.1016/j.tube.2015.08.004. Epub 2015 Oct 9. [PubMed:26682943]
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
  1. Te Brake LH, Russel FG, van den Heuvel JJ, de Knegt GJ, de Steenwinkel JE, Burger DM, Aarnoutse RE, Koenderink JB: Inhibitory potential of tuberculosis drugs on ATP-binding cassette drug transporters. Tuberculosis (Edinb). 2016 Jan;96:150-7. doi: 10.1016/j.tube.2015.08.004. Epub 2015 Oct 9. [PubMed:26682943]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
References
  1. Te Brake LH, Russel FG, van den Heuvel JJ, de Knegt GJ, de Steenwinkel JE, Burger DM, Aarnoutse RE, Koenderink JB: Inhibitory potential of tuberculosis drugs on ATP-binding cassette drug transporters. Tuberculosis (Edinb). 2016 Jan;96:150-7. doi: 10.1016/j.tube.2015.08.004. Epub 2015 Oct 9. [PubMed:26682943]

Drug created on June 13, 2005 07:24 / Updated on June 12, 2020 11:41

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates