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Identification
NameCyclosporine
Accession NumberDB00091  (BTD00003, BIOD00003)
TypeSmall Molecule
GroupsApproved, Investigational, Vet Approved
Description

A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. Cyclosporine is produced as a metabolite by the fungus species Cordyceps militaris. (From Martindale, The Extra Pharmacopoeia, 30th ed).

Structure
Thumb
Synonyms
Ciclosporin
CsA
CyA
Cyclosporin A
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cyclosporinecapsule25 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Neoralcapsule, liquid filled100 mg/1oralNovartis Pharmaceuticals Corporation1995-07-14Not applicableUs
Neoralcapsule, liquid filled25 mg/1oralNovartis Pharmaceuticals Corporation1995-07-14Not applicableUs
Neoralcapsule, liquid filled25 mg/1oralCardinal Health1995-07-14Not applicableUs
Neoralsolution100 mg/mLoralNovartis Pharmaceuticals Corporation1995-07-14Not applicableUs
Neoral 100mgcapsule100 mgoralNovartis Pharmaceuticals Canada Inc1995-12-31Not applicableCanada
Neoral 10mgcapsule10 mgoralNovartis Pharmaceuticals Canada Inc1998-10-02Not applicableCanada
Neoral 25mgcapsule25 mgoralNovartis Pharmaceuticals Canada Inc1995-12-31Not applicableCanada
Neoral 50mgcapsule50 mgoralNovartis Pharmaceuticals Canada Inc1995-12-31Not applicableCanada
Neoral Oral Solution 100mg/mlsolution100 mgoralNovartis Pharmaceuticals Canada Inc1995-12-31Not applicableCanada
Restasisemulsion.5 mg/mLophthalmicAllergan, Inc.2003-04-01Not applicableUs
Restasisemulsion0.05 %ophthalmicAllergan Inc2010-09-29Not applicableCanada
Restasisemulsion.5 mg/mLophthalmicPhysicians Total Care, Inc.2009-03-27Not applicableUs
Sandimmunecapsule, liquid filled100 mg/1oralNovartis Pharmaceuticals Corporation1990-03-02Not applicableUs
Sandimmunecapsule, liquid filled25 mg/1oralNovartis Pharmaceuticals Corporation1990-03-02Not applicableUs
Sandimmunesolution100 mg/mLoralNovartis Pharmaceuticals Corporation1983-11-14Not applicableUs
Sandimmuneinjection50 mg/mLintravenousNovartis Pharmaceuticals Corporation1983-11-14Not applicableUs
Sandimmune Cap 50mgcapsule50 mgoralSandoz Canada Inc1991-12-311996-11-14Canada
Sandimmune IV 50mg/mlliquid50 mgintravenousNovartis Pharmaceuticals Canada Inc1984-12-31Not applicableCanada
Sandimmune Oral Sol 100mg/mlliquid100 mgoralSandoz Canada Inc1984-12-311997-04-15Canada
Sandimmune Soft Gelatin Cap 100mgcapsule100 mgoralSandoz Canada Inc1988-12-311997-04-15Canada
Sandimmune Soft Gelatine Cap 25mgcapsule25 mgoralSandoz Canada Inc1988-12-311997-04-15Canada
Sandoz Cyclosporinecapsule50 mgoralSandoz Canada Incorporated2006-10-18Not applicableCanada
Sandoz Cyclosporinecapsule25 mgoralSandoz Canada Incorporated2005-05-16Not applicableCanada
Sandoz Cyclosporinecapsule100 mgoralSandoz Canada Incorporated2001-12-27Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-cyclosporine Oral Solutionsolution100 mgoralApotex Inc2002-07-30Not applicableCanada
Cyclosporinecapsule100 mg/1oralEon Labs, Inc.2000-01-13Not applicableUs
Cyclosporinecapsule100 mg/1oralAmerican Health Packaging2009-12-112015-12-29Us
Cyclosporinecapsule, liquid filled25 mg/1oralActavis Pharma, Inc.2008-12-01Not applicableUs
Cyclosporinecapsule25 mg/1oralEon Labs, Inc.2000-01-13Not applicableUs
Cyclosporinecapsule, liquid filled100 mg/1oralAmerican Health Packaging2015-03-30Not applicableUs
Cyclosporinesolution100 mg/mLoralIVAX Pharmaceuticals, Inc.2005-03-29Not applicableUs
Cyclosporinecapsule, liquid filled25 mg/1oralAmerican Health Packaging2014-12-15Not applicableUs
Cyclosporinecapsule, liquid filled100 mg/1oralPhysicians Total Care, Inc.2011-02-10Not applicableUs
Cyclosporinecapsule, gelatin coated100 mg/1oralApotex Corp.2002-05-29Not applicableUs
Cyclosporinecapsule, liquid filled100 mg/1oralPhysicians Total Care, Inc.2006-02-10Not applicableUs
Cyclosporinecapsule, gelatin coated25 mg/1oralApotex Corp.2002-05-29Not applicableUs
Cyclosporinesolution100 mg/mLoralActavis Pharma, Inc.2008-12-01Not applicableUs
Cyclosporinesolution100 mg/mLoralMorton Grove Pharmaceuticals, Inc.2005-02-09Not applicableUs
Cyclosporineinjection, solution50 mg/mLintravenousPerrigo Company2003-10-07Not applicableUs
Cyclosporinecapsule, liquid filled100 mg/1oralActavis Pharma, Inc.2008-12-01Not applicableUs
Cyclosporinecapsule, liquid filled100 mg/1oralCardinal Health2010-09-01Not applicableUs
Cyclosporine Modifiedcapsule, liquid filled50 mg/1oralTeva Pharmaceuticals USA Inc2015-06-01Not applicableUs
Cyclosporine Modifiedcapsule, liquid filled25 mg/1oralTeva Pharmaceuticals USA Inc2015-06-01Not applicableUs
Cyclosporine Modifiedcapsule, liquid filled100 mg/1oralIVAX Pharmaceuticals, Inc.2005-03-29Not applicableUs
Cyclosporine Modifiedcapsule, liquid filled50 mg/1oralIVAX Pharmaceuticals, Inc.2005-04-28Not applicableUs
Cyclosporine Modifiedcapsule, liquid filled25 mg/1oralIVAX Pharmaceuticals, Inc.2005-03-29Not applicableUs
Cyclosporine Modifiedcapsule, liquid filled100 mg/1oralTeva Pharmaceuticals USA Inc2015-06-01Not applicableUs
Gengrafcapsule25 mg/1oralAbb Vie Inc.2010-05-24Not applicableUs
Gengrafcapsule25 mg/1oralCardinal Health2010-05-24Not applicableUs
Gengrafcapsule100 mg/1oralCardinal Health2010-05-24Not applicableUs
Gengrafsolution100 mg/mLoralAbb Vie Inc.2010-05-25Not applicableUs
Gengrafcapsule100 mg/1oralAbb Vie Inc.2010-05-24Not applicableUs
Gengrafcapsule25 mg/1oralAbb Vie Inc.2010-05-24Not applicableUs
Gengrafcapsule100 mg/1oralAbb Vie Inc.2010-05-24Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
SangcyaNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII83HN0GTJ6D
CAS number59865-13-3
WeightAverage: 1202.6112
Monoisotopic: 1201.841368071
Chemical FormulaC62H111N11O12
InChI KeyInChIKey=PMATZTZNYRCHOR-IMVLJIQENA-N
InChI
InChI=1/C62H111N11O12/c1-25-27-28-40(15)52(75)51-56(79)65-43(26-2)58(81)67(18)33-48(74)68(19)44(29-34(3)4)55(78)66-49(38(11)12)61(84)69(20)45(30-35(5)6)54(77)63-41(16)53(76)64-42(17)57(80)70(21)46(31-36(7)8)59(82)71(22)47(32-37(9)10)60(83)72(23)50(39(13)14)62(85)73(51)24/h25,27,34-47,49-52,75H,26,28-33H2,1-24H3,(H,63,77)(H,64,76)(H,65,79)(H,66,78)/b27-25+
IUPAC Name
30-ethyl-14,17,23,32-tetrahydroxy-33-[(4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriaconta-13,16,22,31-tetraene-2,5,8,11,20,26,29-heptone
SMILES
CCC1NC(=O)C(C(O)C(C)C\C=C\C)N(C)C(=O)C(C(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(C)NC(=O)C(C)NC(=O)C(CC(C)C)N(C)C(=O)C(NC(=O)C(CC(C)C)N(C)C(=O)CN(C)C1=O)C(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.
KingdomOrganic compounds
Super ClassOrganic Polymers
ClassPolypeptides
Sub ClassNot Available
Direct ParentPolypeptides
Alternative Parents
Substituents
  • Polypeptide
  • Cyclosporin-backbone
  • Cyclic peptoid/peptide
  • Macrolactam
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Lactam
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External Descriptors
  • Non-ribosomal peptide/polyketide hybrids (C05086 )
Pharmacology
IndicationFor treatment of transplant (kidney, liver, and heart) rejection, rheumatoid arthritis, severe psoriasis.
PharmacodynamicsUsed in immunosuppression for prophylactic treatment of organ transplants, cyclosporine exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited. The T1-helper cell is the main target, although the T1-suppressor cell may also be suppressed. Sandimmune (cyclosporine) also inhibits lymphokine production and release including interleukin-2.
Mechanism of actionCyclosporine binds to cyclophilin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporine also inhibits lymphokine production and interleukin release. In ophthalmic applications, the precise mechanism of action is not known. Cyclosporine emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca.
Related Articles
AbsorptionThe absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. The extent of absorption is dependent on the individual patient, the patient population, and the formulation. The absolute bioavailability of cyclosproine administered as Sandimmune® is dependent on the patient population, estimated to be less than 10% in liver transplant patients and as great as 89% in some renal transplant patients. Compared to an intravenous infusion, the absolute bioavailability of the oral solution is approximately 30% based upon the results in 2 patients. The cyclosporine capsules and oral solution are bioequivalent. The time of peak blood concentrations (Tmax) following oral administration of cyclosporine [modified] ranged from 1.5 - 2.0 hours.
Volume of distribution

The steady state volume of distribution during intravenous dosing has been reported as 3 to 5 L/kg in solid organ transplant recipients. Cyclosporine is excreted in human milk.

Protein bindingIn the plasma, approximately 90% is bound to proteins, primarily lipoproteins. In blood, the distribution is concentration dependent. Approximately 33% to 47% is in plasma, 4% to 9% in lymphocytes, 5% to 12% in granulocytes, and 41% to 58% in erythrocytes.
Metabolism

Hepatic, extensively metabolized by the cytochrome P450 3A enzyme system in the liver. It is also metabolized in the gastrointestinal tract and kidney to a lesser degree. The metabolites are significantly less potent than the parent compound. The major metabolites (M1, M9, and M4N) result from oxidation at the 1-beta, 9-gamma, and 4-N-demethylated positions, respectively.

SubstrateEnzymesProduct
Cyclosporine
Metabolite AM1Details
Route of eliminationElimination is primarily biliary with only 6% of the dose (parent drug and metabolites) excreted in the urine. Only 0.1% of the dose is excreted in the urine as unchanged drug.
Half lifeBiphasic and variable, approximately 7 hours (range 7 to 19 hours) in children and approximately 19 hours (range 10 to 27 hours) in adults.
Clearance

Following intravenous administration, the blood clearance of cyclosporine (assay: HPLC) is approximately 5 to 7 mL/min/kg in adult recipients of renal or liver allografts. Blood cyclosporine clearance appears to be slightly slower in cardiac transplant patients. The following are clearance parameters (CL/F) for select patient populations:

  • 593 ± 204 mL/min [De novo renal transplant patients, 597±174 mg/day]
  • 492 ± 140 mL/min [Stable renal transplant patients, 344±122 mg/day]
  • 577 ± 309 mL/min [De novo liver transplant, 458±190 mg/day]
  • 613 ± 196 mL/min [De novo rheumatoid arthritis, 182±55.6 mg/day]
  • 723 ± 186 mL/min [De novo psoriasis, 189±69.8 mg/day]
  • 285 ± 94 mL/min [Stable Liver Transplant, Age 2 – 8, Dosed T.I.D 101±25 mg/day]
  • 378 ± 80 mL/min [Stable Liver Transplant, Age 8 – 15, Dosed B.I.D 188±55 mg/day]
  • 171 mL/min [Stable liver transplant, Age 3, Dosed B.I.D 120 mg/day]
  • 328 ± 121 mL/min [Stable liver transplant, Age 8 – 15, Dosed B.I.D 158±55 mg/day]
  • 418 ± 143 mL/min [Stable renal transplant, Age 7 – 15, Dosed B.I.D 328±83 mg/day]
ToxicityThe oral LD50 is 2329 mg/kg in mice, 1480 mg/kg in rats, and > 1000 mg/kg in rabbits. The I.V. LD50 is 148 mg/kg in mice, 104 mg/kg in rats, and 46 mg/kg in rabbits.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Cytotoxic T-lymphocyte protein 4
Gene symbol: CTLA4
UniProt: P16410
rs231775 Not AvailableA AlleleGingival overgrowth, periodontal disease18021981
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8727
Blood Brain Barrier-0.9659
Caco-2 permeable-0.6994
P-glycoprotein substrateSubstrate0.8463
P-glycoprotein inhibitor IInhibitor0.8685
P-glycoprotein inhibitor IINon-inhibitor0.5992
Renal organic cation transporterNon-inhibitor0.9485
CYP450 2C9 substrateNon-substrate0.8628
CYP450 2D6 substrateNon-substrate0.8823
CYP450 3A4 substrateSubstrate0.6407
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.923
CYP450 2D6 inhibitorNon-inhibitor0.9265
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.6112
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9968
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.8948
BiodegradationNot ready biodegradable0.9244
Rat acute toxicity2.8788 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9815
hERG inhibition (predictor II)Non-inhibitor0.9214
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Apotex inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Pliva inc
  • Sandoz inc
  • Abbott laboratories
  • Novartis pharmaceuticals corp
  • Allergan inc
  • Bedford laboratories div ben venue laboratories inc
  • Pharmaforce inc
  • Novex pharma
  • Watson laboratories inc
  • Wockhardt eu operations (swiss) ag
Packagers
Dosage forms
FormRouteStrength
Capsule, gelatin coatedoral100 mg/1
Capsule, gelatin coatedoral25 mg/1
Injection, solutionintravenous50 mg/mL
Capsule, liquid filledoral50 mg/1
Capsuleoral100 mg/1
Capsuleoral25 mg/1
Solutionoral100 mg/mL
Capsuleoral100 mg
Capsuleoral10 mg
Capsuleoral25 mg
Capsuleoral50 mg
Solutionoral100 mg
Emulsionophthalmic.5 mg/mL
Emulsionophthalmic0.05 %
Capsule, liquid filledoral100 mg/1
Capsule, liquid filledoral25 mg/1
Injectionintravenous50 mg/mL
Liquidintravenous50 mg
Liquidoral100 mg
Prices
Unit descriptionCostUnit
SandIMMUNE 100 mg/ml Solution 50ml Bottle499.62USD bottle
Neoral 100 mg/ml Solution 50ml Bottle346.14USD bottle
CycloSPORINE Modified 100 mg/ml Solution 50ml Bottle311.53USD bottle
SandIMMUNE 30 100 mg capsule Box308.69USD box
Restasis 30 0.05% Emulsion 1 Box = 30 Containers205.99USD box
Neoral 30 100 mg capsule Box190.54USD box
CycloSPORINE Modified 30 100 mg capsule Box171.48USD box
Gengraf 30 100 mg capsule Box159.94USD box
SandIMMUNE 30 25 mg capsule Box77.33USD box
Neoral 30 25 mg capsule Box47.69USD box
SandIMMUNE 50 mg/ml Solution 5ml Ampule46.38USD ampule
Gengraf 30 25 mg capsule Box42.99USD box
CycloSPORINE Modified 30 25 mg capsule Box42.9USD box
Cyclosporine a powder25.2USD g
Sandimmune 100 mg capsule9.89USD capsule
Sandimmune 50 mg/ml ampul7.71USD ml
Cyclosporine 100 mg capsule6.46USD capsule
Neoral 100 mg gelatn capsule6.11USD capsule
Cyclosporine 100 mg softgel5.5USD softgel capsule
Cyclosporine modif 100 mg softgel5.5USD softgel capsule
Cyclosporine modif 100 mg capsule5.49USD capsule
Cyclosporine 50 mg/ml amp5.45USD ml
Cyclosporine 50 mg/ml vial5.28USD ml
Gengraf 100 mg capsule5.28USD capsule
Restasis 0.05% eye emulsion4.49USD each
Cyclosporine 50 mg softgel2.74USD softgel capsule
Sandimmune 25 mg capsule2.48USD capsule
Cyclosporine 25 mg capsule1.56USD capsule
Neoral 25 mg gelatin capsule1.53USD capsule
Cyclosporine 25 mg softgel1.38USD softgel capsule
Gengraf 25 mg capsule1.32USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1332150 No1994-09-272011-09-27Canada
CA2108018 No2003-04-152012-04-16Canada
US4839342 No1992-08-022009-08-02Us
US5985321 No1994-09-262014-09-26Us
US8629111 No2004-08-272024-08-27Us
US8633162 No2004-08-272024-08-27Us
US8642556 No2004-08-272024-08-27Us
US8648048 No2004-08-272024-08-27Us
US8685930 No2004-08-272024-08-27Us
US9248191 No2004-08-272024-08-27Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point148-151 °CNot Available
Caco2 permeability-6.05ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00581 mg/mLALOGPS
logP4.37ALOGPS
logP6.92ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)3.69ChemAxon
pKa (Strongest Basic)1.94ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count16ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area292.76 Å2ChemAxon
Rotatable Bond Count15ChemAxon
Refractivity329.23 m3·mol-1ChemAxon
Polarizability131.92 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Hans Dietl, “Pharmaceutical preparation containing cyclosporine(s) for intravenous administration and a process for its production.” U.S. Patent US5527537, issued October, 1990.

US5527537
General References
  1. Lichtiger S, Present DH, Kornbluth A, Gelernt I, Bauer J, Galler G, Michelassi F, Hanauer S: Cyclosporine in severe ulcerative colitis refractory to steroid therapy. N Engl J Med. 1994 Jun 30;330(26):1841-5. [PubMed:8196726 ]
  2. Husi H, Schorgendorfer K, Stempfer G, Taylor P, Walkinshaw MD: Prediction of substrate-specific pockets in cyclosporin synthetase. FEBS Lett. 1997 Sep 15;414(3):532-6. [PubMed:9323029 ]
  3. Link [Link]
External Links
ATC CodesL04AD01S01XA18
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (176 KB)
MSDSDownload (83.2 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Cyclosporine can be increased when combined with Acetaminophen.
AcetazolamideThe serum concentration of Cyclosporine can be increased when it is combined with Acetazolamide.
AdalimumabThe serum concentration of Cyclosporine can be decreased when it is combined with Adalimumab.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Cyclosporine.
AliskirenThe serum concentration of Aliskiren can be increased when it is combined with Cyclosporine.
AmbrisentanThe serum concentration of ambrisentan can be increased when it is combined with Cyclosporine.
AmikacinAmikacin may increase the nephrotoxic activities of Cyclosporine.
AmilorideAmiloride may increase the hyperkalemic activities of Cyclosporine.
AmiodaroneThe metabolism of Cyclosporine can be decreased when combined with Amiodarone.
AmlodipineThe metabolism of Amlodipine can be decreased when combined with Cyclosporine.
AmobarbitalThe metabolism of Cyclosporine can be increased when combined with Amobarbital.
Amphotericin BAmphotericin B may increase the nephrotoxic activities of Cyclosporine.
AprepitantThe serum concentration of Cyclosporine can be increased when it is combined with Aprepitant.
ArbekacinArbekacin may increase the nephrotoxic activities of Cyclosporine.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Cyclosporine.
ArmodafinilThe serum concentration of Cyclosporine can be decreased when it is combined with Armodafinil.
AtazanavirThe serum concentration of Cyclosporine can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Cyclosporine.
Atracurium besylateCyclosporine may increase the neuromuscular blocking activities of Atracurium besylate.
Azilsartan medoxomilAzilsartan medoxomil may increase the hyperkalemic activities of Cyclosporine.
AzithromycinThe metabolism of Cyclosporine can be decreased when combined with Azithromycin.
BatimastatThe serum concentration of Cyclosporine can be increased when it is combined with Batimastat.
BepridilThe metabolism of Cyclosporine can be decreased when combined with Bepridil.
BexaroteneThe serum concentration of Cyclosporine can be decreased when it is combined with Bexarotene.
BezafibrateCyclosporine may increase the nephrotoxic activities of Bezafibrate.
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Cyclosporine.
BosentanThe serum concentration of Bosentan can be increased when it is combined with Cyclosporine.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Cyclosporine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Cyclosporine.
BromocriptineThe serum concentration of Cyclosporine can be increased when it is combined with Bromocriptine.
BumetanideThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Bumetanide.
ButabarbitalThe metabolism of Cyclosporine can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Cyclosporine can be increased when combined with Butalbital.
ButethalThe metabolism of Cyclosporine can be increased when combined with Butethal.
CaffeineThe metabolism of Cyclosporine can be increased when combined with Caffeine.
CandesartanCandesartan may increase the hyperkalemic activities of Cyclosporine.
CarbamazepineThe serum concentration of Cyclosporine can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Cyclosporine can be increased when it is combined with Carvedilol.
CaspofunginThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Caspofungin.
CelecoxibCelecoxib may increase the nephrotoxic activities of Cyclosporine.
ChloramphenicolThe serum concentration of Cyclosporine can be increased when it is combined with Chloramphenicol.
Cholic AcidCyclosporine may decrease the excretion rate of Cholic Acid which could result in a lower serum level and potentially a reduction in efficacy.
CilastatinCyclosporine may increase the neurotoxic activities of Cilastatin.
Cisatracurium besylateCyclosporine may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe metabolism of Cyclosporine can be decreased when combined with Clarithromycin.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Cyclosporine.
ColesevelamThe serum concentration of Cyclosporine can be decreased when it is combined with Colesevelam.
ConivaptanThe serum concentration of Cyclosporine can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Cyclosporine can be increased when it is combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the immunosuppressive activities of Cyclosporine.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Cyclosporine.
DabrafenibThe serum concentration of Cyclosporine can be decreased when it is combined with Dabrafenib.
DalfopristinThe serum concentration of Cyclosporine can be increased when it is combined with Dalfopristin.
DanazolDanazol may increase the hepatotoxic activities of Cyclosporine.
DarunavirThe serum concentration of Cyclosporine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Cyclosporine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Cyclosporine can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Cyclosporine.
DexamethasoneThe serum concentration of Cyclosporine can be decreased when it is combined with Dexamethasone.
DiclofenacDiclofenac may increase the nephrotoxic activities of Cyclosporine.
DiflunisalDiflunisal may increase the nephrotoxic activities of Cyclosporine.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Cyclosporine.
DihydrotestosteroneDihydrotestosterone may increase the hepatotoxic activities of Cyclosporine.
DiltiazemThe metabolism of Cyclosporine can be decreased when combined with Diltiazem.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Cyclosporine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Cyclosporine.
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Cyclosporine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Cyclosporine.
EfavirenzThe serum concentration of Cyclosporine can be decreased when it is combined with Efavirenz.
EluxadolineThe serum concentration of Eluxadoline can be increased when it is combined with Cyclosporine.
EnzalutamideThe serum concentration of Cyclosporine can be decreased when it is combined with Enzalutamide.
EplerenoneEplerenone may increase the hyperkalemic activities of Cyclosporine.
EprosartanEprosartan may increase the hyperkalemic activities of Cyclosporine.
ErythromycinThe metabolism of Cyclosporine can be decreased when combined with Erythromycin.
Etacrynic acidThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Ethacrynic acid.
EtodolacEtodolac may increase the nephrotoxic activities of Cyclosporine.
EtoposideThe metabolism of Etoposide can be decreased when combined with Cyclosporine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Cyclosporine.
EzetimibeThe serum concentration of Cyclosporine can be increased when it is combined with Ezetimibe.
FelodipineThe metabolism of Felodipine can be decreased when combined with Cyclosporine.
FenofibrateCyclosporine may increase the nephrotoxic activities of Fenofibrate.
FenoprofenFenoprofen may increase the nephrotoxic activities of Cyclosporine.
FimasartanThe serum concentration of Fimasartan can be increased when it is combined with Cyclosporine.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Cyclosporine.
FloctafenineFloctafenine may increase the nephrotoxic activities of Cyclosporine.
FluconazoleThe serum concentration of Cyclosporine can be increased when it is combined with Fluconazole.
FluoxymesteroneFluoxymesterone may increase the hepatotoxic activities of Cyclosporine.
FlurbiprofenFlurbiprofen may increase the nephrotoxic activities of Cyclosporine.
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Cyclosporine.
FosamprenavirThe serum concentration of Cyclosporine can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Cyclosporine can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the nephrotoxic activities of Cyclosporine.
FosphenytoinThe serum concentration of Cyclosporine can be decreased when it is combined with Fosphenytoin.
FramycetinFramycetin may increase the nephrotoxic activities of Cyclosporine.
FurosemideThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Furosemide.
Fusidic AcidThe serum concentration of Cyclosporine can be increased when it is combined with Fusidic Acid.
GemfibrozilCyclosporine may increase the nephrotoxic activities of Gemfibrozil.
GentamicinGentamicin may increase the nephrotoxic activities of Cyclosporine.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Cyclosporine.
GriseofulvinThe serum concentration of Cyclosporine can be decreased when it is combined with Griseofulvin.
HeptabarbitalThe metabolism of Cyclosporine can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Cyclosporine can be increased when combined with Hexobarbital.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Cyclosporine.
IbuprofenIbuprofen may increase the nephrotoxic activities of Cyclosporine.
IdelalisibThe serum concentration of Cyclosporine can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Cyclosporine can be increased when it is combined with Imatinib.
ImipenemCyclosporine may increase the neurotoxic activities of Imipenem.
IndinavirThe serum concentration of Cyclosporine can be increased when it is combined with Indinavir.
IndomethacinIndomethacin may increase the nephrotoxic activities of Cyclosporine.
InfliximabInfliximab may increase the nephrotoxic activities of Cyclosporine.
IrbesartanIrbesartan may increase the hyperkalemic activities of Cyclosporine.
IsoflurophateThe serum concentration of Cyclosporine can be increased when it is combined with Isoflurophate.
IsradipineThe metabolism of Isradipine can be decreased when combined with Cyclosporine.
ItraconazoleThe metabolism of Cyclosporine can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Cyclosporine can be increased when it is combined with Ivacaftor.
KanamycinKanamycin may increase the nephrotoxic activities of Cyclosporine.
KetoconazoleThe metabolism of Cyclosporine can be decreased when combined with Ketoconazole.
KetoprofenKetoprofen may increase the nephrotoxic activities of Cyclosporine.
KetorolacKetorolac may increase the nephrotoxic activities of Cyclosporine.
L-PhenylalanineL-Phenylalanine may increase the nephrotoxic activities of Cyclosporine.
LanreotideThe serum concentration of Cyclosporine can be decreased when it is combined with Lanreotide.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Cyclosporine.
LeflunomideThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Leflunomide.
LercanidipineThe serum concentration of Cyclosporine can be increased when it is combined with Lercanidipine.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Cyclosporine.
LopinavirThe serum concentration of Cyclosporine can be increased when it is combined with Lopinavir.
LosartanLosartan may increase the hyperkalemic activities of Cyclosporine.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Cyclosporine.
LuliconazoleThe serum concentration of Cyclosporine can be increased when it is combined with Luliconazole.
Mefenamic acidMefenamic acid may increase the nephrotoxic activities of Cyclosporine.
MeloxicamMeloxicam may increase the nephrotoxic activities of Cyclosporine.
MelphalanMelphalan may increase the nephrotoxic activities of Cyclosporine.
MethohexitalThe metabolism of Cyclosporine can be increased when combined with Methohexital.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Cyclosporine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Cyclosporine.
MethyltestosteroneMethyltestosterone may increase the hepatotoxic activities of Cyclosporine.
MetoclopramideMetoclopramide can cause an increase in the absorption of Cyclosporine resulting in an increased serum concentration and potentially a worsening of adverse effects.
MetreleptinThe serum concentration of Cyclosporine can be decreased when it is combined with Metreleptin.
MifepristoneThe serum concentration of Cyclosporine can be increased when it is combined with Mifepristone.
MinoxidilThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Minoxidil.
MitotaneThe serum concentration of Cyclosporine can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Cyclosporine.
ModafinilThe serum concentration of Cyclosporine can be decreased when it is combined with Modafinil.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be decreased when it is combined with Cyclosporine.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Cyclosporine.
NabumetoneNabumetone may increase the nephrotoxic activities of Cyclosporine.
NafcillinThe metabolism of Cyclosporine can be increased when combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Cyclosporine.
NaproxenNaproxen may increase the nephrotoxic activities of Cyclosporine.
NatalizumabThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Natalizumab.
NelfinavirThe serum concentration of Cyclosporine can be increased when it is combined with Nelfinavir.
NeomycinNeomycin may increase the nephrotoxic activities of Cyclosporine.
NetilmicinNetilmicin may increase the nephrotoxic activities of Cyclosporine.
NetupitantThe serum concentration of Cyclosporine can be increased when it is combined with Netupitant.
NicardipineThe metabolism of Nicardipine can be decreased when combined with Cyclosporine.
NifedipineThe metabolism of Nifedipine can be decreased when combined with Cyclosporine.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Cyclosporine.
NisoldipineThe metabolism of Nisoldipine can be decreased when combined with Cyclosporine.
NorfloxacinThe metabolism of Cyclosporine can be decreased when combined with Norfloxacin.
OctreotideThe serum concentration of Cyclosporine can be decreased when it is combined with Octreotide.
OlmesartanOlmesartan may increase the hyperkalemic activities of Cyclosporine.
OmeprazoleThe serum concentration of Cyclosporine can be increased when it is combined with Omeprazole.
OrlistatThe serum concentration of Cyclosporine can be decreased when it is combined with Orlistat.
OxandroloneOxandrolone may increase the hepatotoxic activities of Cyclosporine.
OxaprozinOxaprozin may increase the nephrotoxic activities of Cyclosporine.
Oxymetholoneoxymetholone may increase the hepatotoxic activities of Cyclosporine.
PalbociclibThe serum concentration of Cyclosporine can be increased when it is combined with Palbociclib.
PancuroniumCyclosporine may increase the neuromuscular blocking activities of Pancuronium.
PasireotideThe serum concentration of Cyclosporine can be decreased when it is combined with Pasireotide.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Cyclosporine.
PentobarbitalThe metabolism of Cyclosporine can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Cyclosporine can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Cyclosporine can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cyclosporine.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Cyclosporine.
PiroxicamPiroxicam may increase the nephrotoxic activities of Cyclosporine.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Cyclosporine.
PosaconazoleThe metabolism of Cyclosporine can be decreased when combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Cyclosporine.
PrednisoloneThe serum concentration of Cyclosporine can be decreased when it is combined with Prednisolone.
PrednisoneThe serum concentration of the active metabolites of Prednisone can be increased when Prednisone is used in combination with Cyclosporine.
PrimidoneThe metabolism of Cyclosporine can be increased when combined with Primidone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Cyclosporine.
PyrazinamideThe serum concentration of Cyclosporine can be increased when it is combined with Pyrazinamide.
QuinupristinThe serum concentration of Cyclosporine can be increased when it is combined with Quinupristin.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Cyclosporine.
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Cyclosporine.
RibostamycinRibostamycin may increase the nephrotoxic activities of Cyclosporine.
RifabutinThe metabolism of Cyclosporine can be increased when combined with Rifabutin.
RifampicinThe metabolism of Cyclosporine can be increased when combined with Rifampicin.
RifapentineThe metabolism of Cyclosporine can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Cyclosporine.
RitonavirThe serum concentration of Cyclosporine can be increased when it is combined with Ritonavir.
RocuroniumCyclosporine may increase the neuromuscular blocking activities of Rocuronium.
RoflumilastRoflumilast may increase the immunosuppressive activities of Cyclosporine.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Cyclosporine.
SaquinavirThe serum concentration of Cyclosporine can be increased when it is combined with Saquinavir.
SecobarbitalThe metabolism of Cyclosporine can be increased when combined with Secobarbital.
SevelamerThe serum concentration of Cyclosporine can be decreased when it is combined with Sevelamer.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Cyclosporine.
SiltuximabThe serum concentration of Cyclosporine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Cyclosporine can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Cyclosporine.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Cyclosporine.
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Cyclosporine.
SitaxentanThe serum concentration of Sitaxentan can be increased when it is combined with Cyclosporine.
SpectinomycinSpectinomycin may increase the nephrotoxic activities of Cyclosporine.
SpironolactoneSpironolactone may increase the hyperkalemic activities of Cyclosporine.
St. John's WortThe serum concentration of Cyclosporine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Cyclosporine can be increased when it is combined with Stiripentol.
StreptomycinStreptomycin may increase the nephrotoxic activities of Cyclosporine.
SuccinylcholineCyclosporine may increase the neuromuscular blocking activities of Succinylcholine.
SulfadiazineSulfadiazine may increase the nephrotoxic activities of Cyclosporine.
SulfamethoxazoleSulfamethoxazole may increase the nephrotoxic activities of Cyclosporine.
SulfinpyrazoneThe serum concentration of Cyclosporine can be decreased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Cyclosporine can be decreased when combined with Sulfisoxazole.
SulindacSulindac may increase the nephrotoxic activities of Cyclosporine.
TacrolimusTacrolimus may increase the nephrotoxic activities of Cyclosporine.
TelaprevirThe serum concentration of Cyclosporine can be increased when it is combined with Telaprevir.
TelmisartanTelmisartan may increase the hyperkalemic activities of Cyclosporine.
TemsirolimusThe risk or severity of adverse effects can be increased when Temsirolimus is combined with Cyclosporine.
TesmilifeneThe serum concentration of Cyclosporine can be decreased when it is combined with Tesmilifene.
TestosteroneTestosterone may increase the hepatotoxic activities of Cyclosporine.
Tiaprofenic acidTiaprofenic acid may increase the nephrotoxic activities of Cyclosporine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Cyclosporine.
TipranavirThe serum concentration of Cyclosporine can be increased when it is combined with Tipranavir.
TobramycinTobramycin may increase the nephrotoxic activities of Cyclosporine.
TocilizumabThe serum concentration of Cyclosporine can be decreased when it is combined with Tocilizumab.
TofacitinibCyclosporine may increase the immunosuppressive activities of Tofacitinib.
TolmetinTolmetin may increase the nephrotoxic activities of Cyclosporine.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Cyclosporine.
TorasemideThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Torasemide.
TrastuzumabTrastuzumab may increase the neutropenic activities of Cyclosporine.
TriamtereneTriamterene may increase the hyperkalemic activities of Cyclosporine.
TrimethoprimTrimethoprim may increase the nephrotoxic activities of Cyclosporine.
ValsartanValsartan may increase the hyperkalemic activities of Cyclosporine.
VecuroniumCyclosporine may increase the neuromuscular blocking activities of Vecuronium.
VerapamilThe serum concentration of Cyclosporine can be increased when it is combined with Verapamil.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Cyclosporine.
Vitamin CThe serum concentration of Cyclosporine can be decreased when it is combined with Vitamin C.
Vitamin EThe serum concentration of Cyclosporine can be decreased when it is combined with Vitamin E.
VoriconazoleThe metabolism of Cyclosporine can be decreased when combined with Voriconazole.
Food Interactions
  • Avoid salt substitutes containing potassium.
  • Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
  • Red wine may reduce cyclosporine levels due to increased metabolism, therefore it appears prudent to avoid red wine (white wine does not appear to affect cyclosporine metabolism).
  • When taken with a meal, AUC and Cmax of cyclosporine modified decreased.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
binder
General Function:
Not Available
Specific Function:
Likely involved in the mobilization of calcium as a result of the TCR/CD3 complex interaction. Binds to cyclophilin B.
Gene Name:
CAMLG
Uniprot ID:
P49069
Molecular Weight:
32952.255 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
  3. Bernasconi R, Solda T, Galli C, Pertel T, Luban J, Molinari M: Cyclosporine A-sensitive, cyclophilin B-dependent endoplasmic reticulum-associated degradation. PLoS One. 2010 Sep 28;5(9). pii: e13008. doi: 10.1371/journal.pone.0013008. [PubMed:20927389 ]
  4. Yamashita H, Ito T, Kato H, Asai S, Tanaka H, Nagai H, Inagaki N: Comparison of the efficacy of tacrolimus and cyclosporine A in a murine model of dinitrofluorobenzene-induced atopic dermatitis. Eur J Pharmacol. 2010 Oct 25;645(1-3):171-6. doi: 10.1016/j.ejphar.2010.07.031. Epub 2010 Aug 3. [PubMed:20674565 ]
  5. Galat A, Bua J: Molecular aspects of cyclophilins mediating therapeutic actions of their ligands. Cell Mol Life Sci. 2010 Oct;67(20):3467-88. doi: 10.1007/s00018-010-0437-0. Epub 2010 Jul 4. [PubMed:20602248 ]
  6. Lee J, Kim SS: Current implications of cyclophilins in human cancers. J Exp Clin Cancer Res. 2010 Jul 19;29:97. doi: 10.1186/1756-9966-29-97. [PubMed:20637127 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Calcium ion binding
Specific Function:
Regulatory subunit of calcineurin, a calcium-dependent, calmodulin stimulated protein phosphatase. Confers calcium sensitivity (By similarity).
Gene Name:
PPP3R2
Uniprot ID:
Q96LZ3
Molecular Weight:
19533.065 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
  3. Yamashita H, Ito T, Kato H, Asai S, Tanaka H, Nagai H, Inagaki N: Comparison of the efficacy of tacrolimus and cyclosporine A in a murine model of dinitrofluorobenzene-induced atopic dermatitis. Eur J Pharmacol. 2010 Oct 25;645(1-3):171-6. doi: 10.1016/j.ejphar.2010.07.031. Epub 2010 Aug 3. [PubMed:20674565 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Virion binding
Specific Function:
PPIases accelerate the folding of proteins. It catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides.
Gene Name:
PPIA
Uniprot ID:
P62937
Molecular Weight:
18012.42 Da
References
  1. Keckesova Z, Ylinen LM, Towers GJ: Cyclophilin A renders human immunodeficiency virus type 1 sensitive to Old World monkey but not human TRIM5 alpha antiviral activity. J Virol. 2006 May;80(10):4683-90. [PubMed:16641261 ]
  2. Patwardhan AM, Jeske NA, Price TJ, Gamper N, Akopian AN, Hargreaves KM: The cannabinoid WIN 55,212-2 inhibits transient receptor potential vanilloid 1 (TRPV1) and evokes peripheral antihyperalgesia via calcineurin. Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11393-8. Epub 2006 Jul 18. [PubMed:16849427 ]
  3. Redell JB, Zhao J, Dash PK: Acutely increased cyclophilin a expression after brain injury: a role in blood-brain barrier function and tissue preservation. J Neurosci Res. 2007 Jul;85(9):1980-8. [PubMed:17461417 ]
  4. Schaller T, Ylinen LM, Webb BL, Singh S, Towers GJ: Fusion of cyclophilin A to Fv1 enables cyclosporine-sensitive restriction of human and feline immunodeficiency viruses. J Virol. 2007 Sep;81(18):10055-63. Epub 2007 Jul 3. [PubMed:17609268 ]
  5. Lee J, Kim SS: Current implications of cyclophilins in human cancers. J Exp Clin Cancer Res. 2010 Jul 19;29:97. doi: 10.1186/1756-9966-29-97. [PubMed:20637127 ]
  6. Stegmann CM, Luhrmann R, Wahl MC: The crystal structure of PPIL1 bound to cyclosporine A suggests a binding mode for a linear epitope of the SKIP protein. PLoS One. 2010 Apr 2;5(4):e10013. doi: 10.1371/journal.pone.0010013. [PubMed:20368803 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Peptidyl-prolyl cis-trans isomerase activity
Specific Function:
PPIases accelerate the folding of proteins. It catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides. Involved in regulation of the mitochondrial permeability transition pore (mPTP). It is proposed that its association with the mPTP is masking a binding site for inhibiting inorganic phosphate (Pi) and promotes the open probability of the mPTP leading to apoptosi...
Gene Name:
PPIF
Uniprot ID:
P30405
Molecular Weight:
22040.09 Da
References
  1. Handschumacher RE, Harding MW, Rice J, Drugge RJ, Speicher DW: Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [PubMed:6238408 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [PubMed:10490933 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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
Molecular Weight:
141477.255 Da
References
  1. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. [PubMed:12387747 ]
  2. Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, Kim RB: Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab Dispos. 2000 Jun;28(6):655-60. [PubMed:10820137 ]
  3. Tiberghien F, Kurome T, Takesako K, Didier A, Wenandy T, Loor F: Aureobasidins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC-transporter. J Med Chem. 2000 Jun 29;43(13):2547-56. [PubMed:10891114 ]
  4. Gao J, Murase O, Schowen RL, Aube J, Borchardt RT: A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells. Pharm Res. 2001 Feb;18(2):171-6. [PubMed:11405287 ]
  5. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  6. Leonessa F, Kim JH, Ghiorghis A, Kulawiec RJ, Hammer C, Talebian A, Clarke R: C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. J Med Chem. 2002 Jan 17;45(2):390-8. [PubMed:11784143 ]
  7. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [PubMed:11961113 ]
  8. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):765-72. [PubMed:12134945 ]
  9. Kumar S, Kwei GY, Poon GK, Iliff SA, Wang Y, Chen Q, Franklin RB, Didolkar V, Wang RW, Yamazaki M, Chiu SH, Lin JH, Pearson PG, Baillie TA: Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein. J Pharmacol Exp Ther. 2003 Mar;304(3):1161-71. [PubMed:12604693 ]
  10. Horie K, Tang F, Borchardt RT: Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter. Pharm Res. 2003 Feb;20(2):161-8. [PubMed:12636153 ]
  11. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389 ]
  12. Atkinson DE, Greenwood SL, Sibley CP, Glazier JD, Fairbairn LJ: Role of MDR1 and MRP1 in trophoblast cells, elucidated using retroviral gene transfer. Am J Physiol Cell Physiol. 2003 Sep;285(3):C584-91. Epub 2003 Apr 30. [PubMed:12724138 ]
  13. Hamada A, Miyano H, Watanabe H, Saito H: Interaction of imatinib mesilate with human P-glycoprotein. J Pharmacol Exp Ther. 2003 Nov;307(2):824-8. Epub 2003 Sep 15. [PubMed:12975485 ]
  14. Corea G, Fattorusso E, Lanzotti V, Taglialatela-Scafati O, Appendino G, Ballero M, Simon PN, Dumontet C, Di Pietro A: Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L. Bioorg Med Chem. 2003 Nov 17;11(23):5221-7. [PubMed:14604686 ]
  15. Rao US, Scarborough GA: Direct demonstration of high affinity interactions of immunosuppressant drugs with the drug binding site of the human P-glycoprotein. Mol Pharmacol. 1994 Apr;45(4):773-6. [PubMed:7514263 ]
  16. Pouliot JF, L'Heureux F, Liu Z, Prichard RK, Georges E: Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. Biochem Pharmacol. 1997 Jan 10;53(1):17-25. [PubMed:8960059 ]
  17. Kuhnel JM, Perrot JY, Faussat AM, Marie JP, Schwaller MA: Functional assay of multidrug resistant cells using JC-1, a carbocyanine fluorescent probe. Leukemia. 1997 Jul;11(7):1147-55. [PubMed:9205004 ]
  18. Ito T, Yano I, Tanaka K, Inui KI: Transport of quinolone antibacterial drugs by human P-glycoprotein expressed in a kidney epithelial cell line, LLC-PK1. J Pharmacol Exp Ther. 1997 Aug;282(2):955-60. [PubMed:9262363 ]
  19. Kim AE, Dintaman JM, Waddell DS, Silverman JA: Saquinavir, an HIV protease inhibitor, is transported by P-glycoprotein. J Pharmacol Exp Ther. 1998 Sep;286(3):1439-45. [PubMed:9732409 ]
  20. Kusunoki N, Takara K, Tanigawara Y, Yamauchi A, Ueda K, Komada F, Ku Y, Kuroda Y, Saitoh Y, Okumura K: Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein. Jpn J Cancer Res. 1998 Nov;89(11):1220-8. [PubMed:9914792 ]
  21. Golstein PE, Boom A, van Geffel J, Jacobs P, Masereel B, Beauwens R: P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999 Apr;437(5):652-60. [PubMed:10087141 ]
  22. Wigler PW: PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts. Biochem Biophys Res Commun. 1999 Apr 13;257(2):410-3. [PubMed:10198227 ]
  23. Hochman JH, Chiba M, Nishime J, Yamazaki M, Lin JH: Influence of P-glycoprotein on the transport and metabolism of indinavir in Caco-2 cells expressing cytochrome P-450 3A4. J Pharmacol Exp Ther. 2000 Jan;292(1):310-8. [PubMed:10604964 ]
  24. Asakura E, Nakayama H, Sugie M, Zhao YL, Nadai M, Kitaichi K, Shimizu A, Miyoshi M, Takagi K, Takagi K, Hasegawa T: Azithromycin reverses anticancer drug resistance and modifies hepatobiliary excretion of doxorubicin in rats. Eur J Pharmacol. 2004 Jan 26;484(2-3):333-9. [PubMed:14744620 ]
  25. D'Emanuele A, Jevprasesphant R, Penny J, Attwood D: The use of a dendrimer-propranolol prodrug to bypass efflux transporters and enhance oral bioavailability. J Control Release. 2004 Mar 24;95(3):447-53. [PubMed:15023456 ]
  26. Honda Y, Ushigome F, Koyabu N, Morimoto S, Shoyama Y, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. Br J Pharmacol. 2004 Dec;143(7):856-64. Epub 2004 Oct 25. [PubMed:15504753 ]
  27. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
  28. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267 ]
  29. Kugawa F, Suzuki T, Miyata M, Tomono K, Tamanoi F: Construction of a model cell line for the assay of MDR1 (multi drug resistance gene-1) substrates/inhibitors using HeLa cells. Pharmazie. 2009 May;64(5):296-300. [PubMed:19530439 ]
  30. Dahan A, Sabit H, Amidon GL: The H2 receptor antagonist nizatidine is a P-glycoprotein substrate: characterization of its intestinal epithelial cell efflux transport. AAPS J. 2009 Jun;11(2):205-13. doi: 10.1208/s12248-009-9092-5. Epub 2009 Mar 25. [PubMed:19319690 ]
  31. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674 ]
  32. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684 ]
  33. Seeballuck F, Ashford MB, O'Driscoll CM: The effects of pluronics block copolymers and Cremophor EL on intestinal lipoprotein processing and the potential link with P-glycoprotein in Caco-2 cells. Pharm Res. 2003 Jul;20(7):1085-92. [PubMed:12880295 ]
  34. Troutman MD, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res. 2003 Aug;20(8):1210-24. [PubMed:12948019 ]
  35. Saeki T, Ueda K, Tanigawara Y, Hori R, Komano T: Human P-glycoprotein transports cyclosporin A and FK506. J Biol Chem. 1993 Mar 25;268(9):6077-80. [PubMed:7681059 ]
  36. Fricker G, Drewe J, Huwyler J, Gutmann H, Beglinger C: Relevance of p-glycoprotein for the enteral absorption of cyclosporin A: in vitro-in vivo correlation. Br J Pharmacol. 1996 Aug;118(7):1841-7. [PubMed:8842452 ]
  37. Lown KS, Mayo RR, Leichtman AB, Hsiao HL, Turgeon DK, Schmiedlin-Ren P, Brown MB, Guo W, Rossi SJ, Benet LZ, Watkins PB: Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther. 1997 Sep;62(3):248-60. [PubMed:9333100 ]
  38. Soldner A, Christians U, Susanto M, Wacher VJ, Silverman JA, Benet LZ: Grapefruit juice activates P-glycoprotein-mediated drug transport. Pharm Res. 1999 Apr;16(4):478-85. [PubMed:10227700 ]
  39. Baltes S, Gastens AM, Fedrowitz M, Potschka H, Kaever V, Loscher W: Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. Neuropharmacology. 2007 Feb;52(2):333-46. Epub 2006 Oct 10. [PubMed:17045309 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Zeng H, Chen ZS, Belinsky MG, Rea PA, Kruh GD: Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32. [PubMed:11585759 ]
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
Molecular Weight:
146405.83 Da
References
  1. Byrne JA, Strautnieks SS, Mieli-Vergani G, Higgins CF, Linton KJ, Thompson RJ: The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. Gastroenterology. 2002 Nov;123(5):1649-58. [PubMed:12404239 ]
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [PubMed:12739759 ]
  3. Noe J, Hagenbuch B, Meier PJ, St-Pierre MV: Characterization of the mouse bile salt export pump overexpressed in the baculovirus system. Hepatology. 2001 May;33(5):1223-31. [PubMed:11343252 ]
  4. Lecureur V, Sun D, Hargrove P, Schuetz EG, Kim RB, Lan LB, Schuetz JD: Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. Mol Pharmacol. 2000 Jan;57(1):24-35. [PubMed:10617675 ]
  5. Stieger B, Fattinger K, Madon J, Kullak-Ublick GA, Meier PJ: Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver. Gastroenterology. 2000 Feb;118(2):422-30. [PubMed:10648470 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
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, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Pec MK, Aguirre A, Fernandez JJ, Souto ML, Dorta JF, Villar J: Dehydrothyrsiferol does not modulate multidrug resistance-associated protein 1 resistance: a functional screening system for MRP1 substrates. Int J Mol Med. 2002 Nov;10(5):605-8. [PubMed:12373300 ]
  2. Leier I, Jedlitschky G, Buchholz U, Cole SP, Deeley RG, Keppler D: The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates. J Biol Chem. 1994 Nov 11;269(45):27807-10. [PubMed:7961706 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Shitara Y, Sugiyama D, Kusuhara H, Kato Y, Abe T, Meier PJ, Itoh T, Sugiyama Y: Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharm Res. 2002 Feb;19(2):147-53. [PubMed:11883641 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Bile acid:sodium symporter activity
Specific Function:
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
Gene Name:
SLC10A2
Uniprot ID:
Q12908
Molecular Weight:
37713.405 Da
References
  1. Craddock AL, Love MW, Daniel RW, Kirby LC, Walters HC, Wong MH, Dawson PA: Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter. Am J Physiol. 1998 Jan;274(1 Pt 1):G157-69. [PubMed:9458785 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Virus receptor activity
Specific Function:
The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presence of sodium.(Microbial infection) Acts as a receptor for hepatitis B virus.
Gene Name:
SLC10A1
Uniprot ID:
Q14973
Molecular Weight:
38118.64 Da
References
  1. Schroeder A, Eckhardt U, Stieger B, Tynes R, Schteingart CD, Hofmann AF, Meier PJ, Hagenbuch B: Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am J Physiol. 1998 Feb;274(2 Pt 1):G370-5. [PubMed:9486191 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Sweet DH, Wolff NA, Pritchard JB: Expression cloning and characterization of ROAT1. The basolateral organic anion transporter in rat kidney. J Biol Chem. 1997 Nov 28;272(48):30088-95. [PubMed:9374486 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
ATP-dependent transporter probably involved in cellular detoxification through lipophilic anion extrusion.
Gene Name:
ABCC10
Uniprot ID:
Q5T3U5
Molecular Weight:
161627.375 Da
References
  1. Chen ZS, Hopper-Borge E, Belinsky MG, Shchaveleva I, Kotova E, Kruh GD: Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). Mol Pharmacol. 2003 Feb;63(2):351-8. [PubMed:12527806 ]
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
Molecular Weight:
174205.64 Da
References
  1. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):773-9. [PubMed:12134946 ]
  2. Hong J, Lambert JD, Lee SH, Sinko PJ, Yang CS: Involvement of multidrug resistance-associated proteins in regulating cellular levels of (-)-epigallocatechin-3-gallate and its methyl metabolites. Biochem Biophys Res Commun. 2003 Oct 10;310(1):222-7. [PubMed:14511674 ]
  3. Kamisako T, Leier I, Cui Y, Konig J, Buchholz U, Hummel-Eisenbeiss J, Keppler D: Transport of monoglucuronosyl and bisglucuronosyl bilirubin by recombinant human and rat multidrug resistance protein 2. Hepatology. 1999 Aug;30(2):485-90. [PubMed:10421658 ]
  4. Chen ZS, Kawabe T, Ono M, Aoki S, Sumizawa T, Furukawa T, Uchiumi T, Wada M, Kuwano M, Akiyama SI: Effect of multidrug resistance-reversing agents on transporting activity of human canalicular multispecific organic anion transporter. Mol Pharmacol. 1999 Dec;56(6):1219-28. [PubMed:10570049 ]
  5. Horikawa M, Kato Y, Tyson CA, Sugiyama Y: The potential for an interaction between MRP2 (ABCC2) and various therapeutic agents: probenecid as a candidate inhibitor of the biliary excretion of irinotecan metabolites. Drug Metab Pharmacokinet. 2002;17(1):23-33. [PubMed:15618649 ]
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 from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Ozvegy C, Litman T, Szakacs G, Nagy Z, Bates S, Varadi A, Sarkadi B: Functional characterization of the human multidrug transporter, ABCG2, expressed in insect cells. Biochem Biophys Res Commun. 2001 Jul 6;285(1):111-7. [PubMed:11437380 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Tirona RG, Leake BF, Wolkoff AW, Kim RB: Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. J Pharmacol Exp Ther. 2003 Jan;304(1):223-8. [PubMed:12490595 ]
  2. Shitara Y, Itoh T, Sato H, Li AP, Sugiyama Y: Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. J Pharmacol Exp Ther. 2003 Feb;304(2):610-6. [PubMed:12538813 ]
  3. Nozawa T, Tamai I, Sai Y, Nezu J, Tsuji A: Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin. J Pharm Pharmacol. 2003 Jul;55(7):1013-20. [PubMed:12906759 ]
  4. Fehrenbach T, Cui Y, Faulstich H, Keppler D: Characterization of the transport of the bicyclic peptide phalloidin by human hepatic transport proteins. Naunyn Schmiedebergs Arch Pharmacol. 2003 Nov;368(5):415-20. Epub 2003 Oct 3. [PubMed:14530907 ]
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Drug created on June 13, 2005 07:24 / Updated on July 24, 2016 01:52