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Identification
NameRifampicin
Accession NumberDB01045  (APRD00207, EXPT02777)
TypeSmall Molecule
GroupsApproved
Description

A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)

Structure
Thumb
Synonyms
3-(((4-Methyl-1-piperazinyl)imino)methyl)rifamycin sv
RFP
Rifampicina
Rifampicinum
Rifampin
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rifadincapsule300 mg/1oralSanofi Aventis U.S. Llc1971-05-21Not applicableUs
Rifadincapsule300 mgoralSanofi Aventis Canada Inc1995-12-31Not applicableCanada
Rifadincapsule150 mgoralSanofi Aventis Canada Inc1995-12-31Not applicableCanada
Rifadin Cap 300mgcapsule300 mgoralMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1988-12-311996-09-09Canada
Rifadin IVinjection, powder, lyophilized, for solution600 mg/10mLintravenousSanofi Aventis U.S. Llc1989-05-25Not applicableUs
Rofact 150mgcapsule150 mgoralValeant Canada Lp Valeant Canada S.E.C.1977-12-31Not applicableCanada
Rofact 300mgcapsule300 mgoralValeant Canada Lp Valeant Canada S.E.C.1977-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rifadincapsule150 mg/1oralSanofi Aventis U.S. Llc1981-07-15Not applicableUs
Rifampincapsule150 mg/1oralLupin Pharmaceuticals, Inc.2013-10-28Not applicableUs
Rifampincapsule300 mg/1oralVersa Pharm Incorporated2001-07-01Not applicableUs
Rifampincapsule, coated300 mg/1oralH.J. Harkins Company, Inc.2001-07-01Not applicableUs
Rifampincapsule300 mg/1oralMylan Institutional Inc.1999-12-15Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousAkorn, Inc.2012-06-01Not applicableUs
Rifampincapsule300 mg/1oralLupin Pharmaceuticals, Inc.2013-10-28Not applicableUs
Rifampincapsule300 mg/1oral; oralMajor Pharmaceuticals2009-10-07Not applicableUs
Rifampincapsule, coated300 mg/1oralCarilion Materials Management2001-07-01Not applicableUs
Rifampincapsule150 mg/1oralVersa Pharm Incorporated2001-07-01Not applicableUs
Rifampincapsule150 mg/1oralREMEDYREPACK INC.2011-08-03Not applicableUs
Rifampincapsule300 mg/1oralAmerican Health Packaging2009-09-25Not applicableUs
Rifampincapsule300 mg/1oralClinical Solutions Wholesale, Llc2008-04-20Not applicableUs
Rifampincapsule150 mg/1oralREMEDYREPACK INC.2011-06-20Not applicableUs
Rifampincapsule150 mg/1oralLannett Company, Inc.2008-04-20Not applicableUs
Rifampincapsule150 mg/1oralAmerican Health Packaging2009-09-25Not applicableUs
Rifampincapsule, coated300 mg/1oralCardinal Health2001-03-14Not applicableUs
Rifampincapsule300 mg/1oralREMEDYREPACK INC.2011-03-28Not applicableUs
Rifampincapsule300 mg/1oralLannett Company, Inc.2008-04-20Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousMylan Institutional LLC2008-05-23Not applicableUs
Rifampincapsule300 mg/1oralCardinal Health2011-05-20Not applicableUs
Rifampincapsule300 mg/1oralRebel Distributors Corp2008-04-20Not applicableUs
Rifampincapsule150 mg/1oralEon Labs, Inc.1998-01-02Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/1intravenousWest Ward Pharmaceuticals Corp2016-03-03Not applicableUs
Rifampincapsule300 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2006-11-30Not applicableUs
Rifampincapsule150 mg/1oralPhysicians Total Care, Inc.2008-04-20Not applicableUs
Rifampincapsule, coated300 mg/1oralREMEDYREPACK INC.2013-10-29Not applicableUs
Rifampincapsule300 mg/1oralEon Labs, Inc.1997-05-28Not applicableUs
Rifampincapsule150 mg/1oralDepartment Of State Health Services, Pharmacy Branch2001-07-01Not applicableUs
Rifampincapsule300 mg/1oralbryant ranch prepack1997-05-28Not applicableUs
Rifampincapsule300 mg/1oralPhysicians Total Care, Inc.2008-04-20Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousHeritage Pharmaceuticals Inc.2014-08-18Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousPfizer Laboratories Div Pfizer Inc2011-05-10Not applicableUs
Rifampincapsule300 mg/1oralDepartment Of State Health Services, Pharmacy Branch2001-07-01Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/1intravenousFresenius Kabi USA, LLC2014-08-21Not applicableUs
Rifampincapsule, coated300 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Rifampincapsule300 mg/1oralRebel Distributors Corp1997-05-28Not applicableUs
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousPfizer Laboratories Div Pfizer Inc2011-05-10Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
RifadineNot Available
RifaldinNot Available
RifoldinNot Available
RimactanNot Available
RimactaneNot Available
RofactNot Available
TubocinNot Available
Brand mixtures
NameLabellerIngredients
IsonarifVersa Pharm Incorporated
RifamateSanofi Aventis U.S. Llc
RifaterSanofi Aventis U.S. Llc
Salts
Name/CASStructureProperties
Rifampicin sodium
ThumbNot applicableDBSALT001014
Categories
UNIIVJT6J7R4TR
CAS number13292-46-1
WeightAverage: 822.9402
Monoisotopic: 822.40512334
Chemical FormulaC43H58N4O12
InChI KeyInChIKey=JQXXHWHPUNPDRT-WLSIYKJHSA-N
InChI
InChI=1S/C43H58N4O12/c1-21-12-11-13-22(2)42(55)45-33-28(20-44-47-17-15-46(9)16-18-47)37(52)30-31(38(33)53)36(51)26(6)40-32(30)41(54)43(8,59-40)57-19-14-29(56-10)23(3)39(58-27(7)48)25(5)35(50)24(4)34(21)49/h11-14,19-21,23-25,29,34-35,39,49-53H,15-18H2,1-10H3,(H,45,55)/b12-11+,19-14+,22-13-,44-20+/t21-,23+,24+,25+,29-,34-,35+,39+,43-/m0/s1
IUPAC Name
(7S,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-[(1E)-[(4-methylpiperazin-1-yl)imino]methyl]-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1⁴,⁷.0⁵,²⁸]triaconta-1(29),2,4,9,19,21,25,27-octaen-13-yl acetate
SMILES
CO[[email protected]]1\C=C\O[C@@]2(C)OC3=C(C2=O)C2=C(O)C(\C=N\N4CCN(C)CC4)=C(NC(=O)\C(C)=C/C=C/[[email protected]](C)[[email protected]](O)[C@@H](C)[C@@H](O)[C@@H](C)[[email protected]](OC(C)=O)[C@@H]1C)C(O)=C2C(O)=C3C
Taxonomy
ClassificationNot classified
Pharmacology
IndicationFor the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections.
PharmacodynamicsRifampin is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifampin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency.
Mechanism of actionRifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
Related Articles
AbsorptionWell absorbed from gastrointestinal tract.
Volume of distributionNot Available
Protein binding89%
Metabolism

Primarily hepatic, rapidly deacetylated.

Route of eliminationLess than 30% of the dose is excreted in the urine as rifampin or metabolites.
Half life3.35 (+/- 0.66) hours
Clearance
  • 0.19 +/- 0.06 L/hr/kg [300 mg IV]
  • 0.14 +/- 0.03 L/hr/kg [600 mg IV]
ToxicityLD50=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness
Affected organisms
  • Mycobacteria
  • Mycobacterium tuberculosis
  • Various gram-negative and gram-positive eubacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.5553
Blood Brain Barrier-0.974
Caco-2 permeable-0.7123
P-glycoprotein substrateSubstrate0.9308
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IINon-inhibitor0.6049
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8508
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7296
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8432
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9099
Ames testNon AMES toxic0.5803
CarcinogenicityNon-carcinogens0.8493
BiodegradationNot ready biodegradable0.9962
Rat acute toxicity2.6875 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.908
hERG inhibition (predictor II)Non-inhibitor0.5486
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral150 mg/1
Capsuleoral150 mg
Capsuleoral300 mg/1
Capsuleoral300 mg
Injection, powder, lyophilized, for solutionintravenous600 mg/10mL
Capsuleoral
Capsuleoral; oral300 mg/1
Capsule, coatedoral300 mg/1
Injection, powder, lyophilized, for solutionintravenous600 mg/1
Tabletoral
Tablet, sugar coatedoral
Prices
Unit descriptionCostUnit
Rifadin iv 600 mg vial140.9USD vial
Rifampin iv 600 mg vial136.3USD vial
Rifampin crystals6.72USD g
Rifampin powder3.98USD g
Rifadin 300 mg capsule3.09USD capsule
Rifadin 150 mg capsule2.57USD capsule
Rifampin 300 mg capsule2.37USD capsule
Rimactane 300 mg capsule2.35USD capsule
Rifampin 150 mg capsule2.27USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point183 °CNot Available
water solubility1400 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.7Not Available
pKa1.7SANGSTER (2004)
Predicted Properties
PropertyValueSource
Water Solubility0.0413 mg/mLALOGPS
logP3.85ALOGPS
logP2.77ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)6.9ChemAxon
pKa (Strongest Basic)7.53ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count14ChemAxon
Hydrogen Donor Count6ChemAxon
Polar Surface Area220.15 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity225.58 m3·mol-1ChemAxon
Polarizability86.46 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Klaus Jurgen, Joachim Seydel, “Combination preparations containing rifampicin and thioacetazon.” U.S. Patent US5104875, issued August, 1973.

US5104875
General References
  1. Baysarowich J, Koteva K, Hughes DW, Ejim L, Griffiths E, Zhang K, Junop M, Wright GD: Rifamycin antibiotic resistance by ADP-ribosylation: Structure and diversity of Arr. Proc Natl Acad Sci U S A. 2008 Mar 25;105(12):4886-91. doi: 10.1073/pnas.0711939105. Epub 2008 Mar 18. [PubMed:18349144 ]
External Links
ATC CodesJ04AB02J04AM02J04AM05J04AM06
AHFS Codes
  • 08:16.04
PDB Entries
FDA labelDownload (43.3 KB)
MSDSDownload (86.7 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Abiraterone can be decreased when it is combined with Rifampicin.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Rifampicin.
AlfentanilThe serum concentration of Alfentanil can be decreased when it is combined with Rifampicin.
AmiodaroneThe serum concentration of the active metabolites of Amiodarone can be reduced when Amiodarone is used in combination with Rifampicin resulting in a loss in efficacy.
AmlodipineThe serum concentration of Amlodipine can be decreased when it is combined with Rifampicin.
AmrinoneThe serum concentration of Amrinone can be decreased when it is combined with Rifampicin.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Rifampicin.
ApremilastThe serum concentration of Apremilast can be decreased when it is combined with Rifampicin.
AprepitantThe serum concentration of Aprepitant can be decreased when it is combined with Rifampicin.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Rifampicin.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Rifampicin resulting in a loss in efficacy.
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Rifampicin.
AtovaquoneThe serum concentration of Atovaquone can be decreased when it is combined with Rifampicin.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Rifampicin.
BazedoxifeneThe serum concentration of Bazedoxifene can be decreased when it is combined with Rifampicin.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Rifampicin.
BendamustineThe serum concentration of Bendamustine can be decreased when it is combined with Rifampicin.
BepridilThe serum concentration of Bepridil can be decreased when it is combined with Rifampicin.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Rifampicin.
BortezomibThe serum concentration of Bortezomib can be decreased when it is combined with Rifampicin.
BosentanThe serum concentration of Bosentan can be decreased when it is combined with Rifampicin.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Rifampicin.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Rifampicin.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Rifampicin.
BuspironeThe serum concentration of Buspirone can be decreased when it is combined with Rifampicin.
ButabarbitalThe metabolism of Butabarbital can be increased when combined with Rifampicin.
ButethalThe metabolism of Butethal can be increased when combined with Rifampicin.
CabozantinibThe serum concentration of Cabozantinib can be decreased when it is combined with Rifampicin.
CanagliflozinThe serum concentration of Canagliflozin can be decreased when it is combined with Rifampicin.
CannabidiolThe serum concentration of Cannabidiol can be decreased when it is combined with Rifampicin.
CaspofunginThe serum concentration of Caspofungin can be decreased when it is combined with Rifampicin.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Rifampicin.
ChloramphenicolThe metabolism of Chloramphenicol can be increased when combined with Rifampicin.
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Rifampicin.
ChlorpropamideThe serum concentration of Chlorpropamide can be decreased when it is combined with Rifampicin.
CitalopramThe serum concentration of Citalopram can be decreased when it is combined with Rifampicin.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Rifampicin.
ClopidogrelThe risk or severity of adverse effects can be increased when Rifampicin is combined with Clopidogrel.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Rifampicin.
CobicistatThe serum concentration of Cobicistat can be decreased when it is combined with Rifampicin.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Rifampicin.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Rifampicin.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Rifampicin.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Rifampicin.
DapsoneThe metabolism of Dapsone can be increased when combined with Rifampicin.
DarunavirThe serum concentration of Darunavir can be decreased when it is combined with Rifampicin.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Rifampicin.
DeferasiroxThe serum concentration of Deferasirox can be decreased when it is combined with Rifampicin.
DelavirdineThe metabolism of Delavirdine can be increased when combined with Rifampicin.
DexamethasoneThe serum concentration of Dexamethasone can be decreased when it is combined with Rifampicin.
DiclofenacThe serum concentration of Diclofenac can be decreased when it is combined with Rifampicin.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Rifampicin.
DiltiazemThe serum concentration of Diltiazem can be decreased when it is combined with Rifampicin.
DisopyramideThe serum concentration of Disopyramide can be decreased when it is combined with Rifampicin.
DolutegravirThe serum concentration of Dolutegravir can be decreased when it is combined with Rifampicin.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Rifampicin.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Rifampicin.
DronabinolThe serum concentration of Dronabinol can be decreased when it is combined with Rifampicin.
DronedaroneThe serum concentration of Dronedarone can be decreased when it is combined with Rifampicin.
EdoxabanThe serum concentration of Edoxaban can be decreased when it is combined with Rifampicin.
EfavirenzThe serum concentration of Efavirenz can be decreased when it is combined with Rifampicin.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Rifampicin.
EltrombopagThe serum concentration of Rifampicin can be increased when it is combined with Eltrombopag.
EluxadolineThe serum concentration of Eluxadoline can be increased when it is combined with Rifampicin.
ElvitegravirThe serum concentration of Elvitegravir can be decreased when it is combined with Rifampicin.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Rifampicin.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Rifampicin.
EsomeprazoleThe serum concentration of Esomeprazole can be decreased when it is combined with Rifampicin.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Rifampicin.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Rifampicin.
EverolimusThe serum concentration of Everolimus can be decreased when it is combined with Rifampicin.
ExemestaneThe serum concentration of Exemestane can be decreased when it is combined with Rifampicin.
FelodipineThe serum concentration of Felodipine can be decreased when it is combined with Rifampicin.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Rifampicin.
FexofenadineThe serum concentration of Fexofenadine can be decreased when it is combined with Rifampicin.
FimasartanThe serum concentration of Fimasartan can be increased when it is combined with Rifampicin.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Rifampicin.
FludrocortisoneThe serum concentration of Fludrocortisone can be decreased when it is combined with Rifampicin.
FlunarizineThe serum concentration of Flunarizine can be decreased when it is combined with Rifampicin.
FlunisolideThe metabolism of Flunisolide can be increased when combined with Rifampicin.
FluvoxamineThe metabolism of Fluvoxamine can be increased when combined with Rifampicin.
FosamprenavirThe serum concentration of Fosamprenavir can be decreased when it is combined with Rifampicin.
FosaprepitantThe serum concentration of Fosaprepitant can be decreased when it is combined with Rifampicin.
FosphenytoinThe serum concentration of Fosphenytoin can be decreased when it is combined with Rifampicin.
GabapentinThe serum concentration of Gabapentin can be decreased when it is combined with Rifampicin.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Rifampicin.
GliclazideThe serum concentration of Gliclazide can be decreased when it is combined with Rifampicin.
GlimepirideThe serum concentration of Glimepiride can be decreased when it is combined with Rifampicin.
GlipizideThe serum concentration of Glipizide can be decreased when it is combined with Rifampicin.
GlyburideThe serum concentration of Glyburide can be decreased when it is combined with Rifampicin.
GuanfacineThe serum concentration of Guanfacine can be decreased when it is combined with Rifampicin.
HeptabarbitalThe metabolism of Heptabarbital can be increased when combined with Rifampicin.
HexobarbitalThe metabolism of Hexobarbital can be increased when combined with Rifampicin.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Rifampicin.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Rifampicin.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Rifampicin.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Rifampicin.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Rifampicin.
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Rifampicin.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Rifampicin resulting in a loss in efficacy.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be reduced when Isavuconazonium is used in combination with Rifampicin resulting in a loss in efficacy.
IsoniazidRifampicin may increase the hepatotoxic activities of Isoniazid.
IsradipineThe serum concentration of Isradipine can be decreased when it is combined with Rifampicin.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Rifampicin.
IvabradineThe serum concentration of Ivabradine can be decreased when it is combined with Rifampicin.
IvacaftorThe serum concentration of Ivacaftor can be decreased when it is combined with Rifampicin.
IxabepiloneThe serum concentration of Ixabepilone can be decreased when it is combined with Rifampicin.
KetoconazoleThe serum concentration of Rifampicin can be increased when it is combined with Ketoconazole.
LamotrigineThe metabolism of Lamotrigine can be increased when combined with Rifampicin.
LapatinibThe serum concentration of Lapatinib can be decreased when it is combined with Rifampicin.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Rifampicin.
LeflunomideThe serum concentration of the active metabolites of Leflunomide can be increased when Leflunomide is used in combination with Rifampicin.
LercanidipineThe serum concentration of Lercanidipine can be decreased when it is combined with Rifampicin.
LevothyroxineThe serum concentration of Levothyroxine can be decreased when it is combined with Rifampicin.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Rifampicin.
LiothyronineThe serum concentration of Liothyronine can be decreased when it is combined with Rifampicin.
LiotrixThe serum concentration of Liotrix can be decreased when it is combined with Rifampicin.
LopinavirThe risk or severity of adverse effects can be increased when Rifampicin is combined with Lopinavir.
LosartanThe serum concentration of Losartan can be decreased when it is combined with Rifampicin.
LumacaftorThe serum concentration of Rifampicin can be decreased when it is combined with Lumacaftor.
LumefantrineThe serum concentration of Lumefantrine can be decreased when it is combined with Rifampicin.
LurasidoneThe serum concentration of Lurasidone can be decreased when it is combined with Rifampicin.
MacitentanThe serum concentration of MACITENTAN can be decreased when it is combined with Rifampicin.
Magnesium SulfateThe serum concentration of Magnesium Sulfate can be decreased when it is combined with Rifampicin.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Rifampicin.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Rifampicin.
MethohexitalThe metabolism of Methohexital can be increased when combined with Rifampicin.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Rifampicin.
MifepristoneThe serum concentration of Mifepristone can be decreased when it is combined with Rifampicin.
MirabegronThe serum concentration of Mirabegron can be decreased when it is combined with Rifampicin.
MorphineThe serum concentration of Morphine can be decreased when it is combined with Rifampicin.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Rifampicin.
NaloxegolThe serum concentration of Naloxegol can be decreased when it is combined with Rifampicin.
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Rifampicin.
NetupitantThe serum concentration of Netupitant can be decreased when it is combined with Rifampicin.
NevirapineThe serum concentration of Nevirapine can be decreased when it is combined with Rifampicin.
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Rifampicin.
NicotineThe metabolism of Nicotine can be increased when combined with Rifampicin.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Rifampicin.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Rifampicin.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Rifampicin.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Rifampicin.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Rifampicin.
NitrazepamThe serum concentration of Nitrazepam can be decreased when it is combined with Rifampicin.
NitrendipineThe serum concentration of Nitrendipine can be decreased when it is combined with Rifampicin.
NorethisteroneThe serum concentration of Norethindrone can be decreased when it is combined with Rifampicin.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Rifampicin.
OmeprazoleThe serum concentration of Omeprazole can be decreased when it is combined with Rifampicin.
OxycodoneThe serum concentration of Oxycodone can be decreased when it is combined with Rifampicin.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Rifampicin.
PaliperidoneThe serum concentration of Paliperidone can be decreased when it is combined with Rifampicin.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Rifampicin.
PantoprazoleThe metabolism of Pantoprazole can be increased when combined with Rifampicin.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Rifampicin.
PentobarbitalThe metabolism of Pentobarbital can be increased when combined with Rifampicin.
PerampanelThe serum concentration of Perampanel can be decreased when it is combined with Rifampicin.
PerhexilineThe serum concentration of Perhexiline can be decreased when it is combined with Rifampicin.
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Rifampicin.
Picosulfuric acidThe therapeutic efficacy of Sodium picosulfate can be decreased when used in combination with Rifampicin.
PioglitazoneThe metabolism of Pioglitazone can be increased when combined with Rifampicin.
PirfenidoneThe serum concentration of Pirfenidone can be decreased when it is combined with Rifampicin.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rifampicin.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Rifampicin.
PrasugrelRifampicin may decrease the antiplatelet activities of Prasugrel.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Rifampicin.
PraziquantelThe serum concentration of Praziquantel can be decreased when it is combined with Rifampicin.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Rifampicin.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Rifampicin.
PrenylamineThe serum concentration of Prenylamine can be decreased when it is combined with Rifampicin.
PrimidoneThe metabolism of Primidone can be increased when combined with Rifampicin.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Rifampicin.
PropofolRifampicin may increase the hypotensive activities of Propofol.
PyrazinamidePyrazinamide may increase the hepatotoxic activities of Rifampicin.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Rifampicin.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Rifampicin.
QuinineThe serum concentration of Quinine can be decreased when it is combined with Rifampicin.
RaltegravirThe serum concentration of Raltegravir can be decreased when it is combined with Rifampicin.
RamelteonThe metabolism of Ramelteon can be increased when combined with Rifampicin.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Rifampicin.
RegorafenibThe serum concentration of Regorafenib can be decreased when it is combined with Rifampicin.
RepaglinideThe serum concentration of Repaglinide can be decreased when it is combined with Rifampicin.
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Rifampicin.
RisedronateThe serum concentration of Risedronate can be decreased when it is combined with Rifampicin.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Rifampicin.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Rifampicin.
RoflumilastThe serum concentration of Roflumilast can be decreased when it is combined with Rifampicin.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Rifampicin.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Rifampicin.
RosiglitazoneThe metabolism of Rosiglitazone can be increased when combined with Rifampicin.
SaquinavirThe risk or severity of adverse effects can be increased when Rifampicin is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifampicin.
SecobarbitalThe metabolism of Secobarbital can be increased when combined with Rifampicin.
SildenafilThe metabolism of Sildenafil can be increased when combined with Rifampicin.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Rifampicin.
SirolimusThe metabolism of Sirolimus can be increased when combined with Rifampicin.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Rifampicin.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Rifampicin.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Rifampicin.
SunitinibThe serum concentration of Sunitinib can be decreased when it is combined with Rifampicin.
SuvorexantThe serum concentration of Suvorexant can be decreased when it is combined with Rifampicin.
TacrolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Rifampicin.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Rifampicin.
TamoxifenThe metabolism of Tamoxifen can be increased when combined with Rifampicin.
TasimelteonThe serum concentration of Tasimelteon can be decreased when it is combined with Rifampicin.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Rifampicin.
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Rifampicin.
TerbinafineThe serum concentration of Terbinafine can be decreased when it is combined with Rifampicin.
TeriflunomideThe serum concentration of Rifampicin can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Rifampicin can be decreased when it is combined with Tesmilifene.
Thyroid, porcineThe serum concentration of Thyroid extract can be decreased when it is combined with Rifampicin.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Rifampicin resulting in a loss in efficacy.
TipranavirThe serum concentration of Tipranavir can be decreased when it is combined with Rifampicin.
TofacitinibThe serum concentration of Tofacitinib can be decreased when it is combined with Rifampicin.
TolazamideThe serum concentration of Tolazamide can be decreased when it is combined with Rifampicin.
TolbutamideThe serum concentration of Tolbutamide can be decreased when it is combined with Rifampicin.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Rifampicin.
TorasemideThe metabolism of Torasemide can be increased when combined with Rifampicin.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Rifampicin.
TrabectedinThe serum concentration of Trabectedin can be decreased when it is combined with Rifampicin.
TreprostinilThe serum concentration of Treprostinil can be decreased when it is combined with Rifampicin.
TroglitazoneThe metabolism of Troglitazone can be increased when combined with Rifampicin.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Rifampicin.
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Rifampicin.
VandetanibThe serum concentration of Vandetanib can be decreased when it is combined with Rifampicin.
VemurafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Rifampicin.
VerapamilThe serum concentration of Verapamil can be decreased when it is combined with Rifampicin.
VilazodoneThe serum concentration of Vilazodone can be decreased when it is combined with Rifampicin.
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Rifampicin.
VorapaxarThe serum concentration of Vorapaxar can be decreased when it is combined with Rifampicin.
VoriconazoleThe serum concentration of Rifampicin can be increased when it is combined with Voriconazole.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Rifampicin.
ZaleplonThe serum concentration of Zaleplon can be decreased when it is combined with Rifampicin.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Rifampicin.
ZolpidemThe serum concentration of Zolpidem can be decreased when it is combined with Rifampicin.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be decreased when it is combined with Rifampicin.
Food Interactions
  • Avoid alcohol.
  • Take on empty stomach: 1 hour before or 2 hours after meals.
  • Take with a full glass of water.

Targets

Kind
Protein
Organism
Escherichia coli (strain K12)
Pharmacological action
yes
Actions
inhibitor
General Function:
Ribonucleoside binding
Specific Function:
DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates.
Gene Name:
rpoB
Uniprot ID:
P0A8V2
Molecular Weight:
150631.165 Da
References
  1. Villain-Guillot P, Bastide L, Gualtieri M, Leonetti JP: Progress in targeting bacterial transcription. Drug Discov Today. 2007 Mar;12(5-6):200-8. Epub 2007 Feb 5. [PubMed:17331884 ]
  2. White RJ, Lancini GC, Silvestri LG: Mechanism of action of rifampin on Mycobacterium smegmatis. J Bacteriol. 1971 Nov;108(2):737-41. [PubMed:4942761 ]
  3. Tupin A, Gualtieri M, Roquet-Baneres F, Morichaud Z, Brodolin K, Leonetti JP: Resistance to rifampicin: at the crossroads between ecological, genomic and medical concerns. Int J Antimicrob Agents. 2010 Jun;35(6):519-23. doi: 10.1016/j.ijantimicag.2009.12.017. Epub 2010 Feb 24. [PubMed:20185278 ]
  4. Campbell EA, Korzheva N, Mustaev A, Murakami K, Nair S, Goldfarb A, Darst SA: Structural mechanism for rifampicin inhibition of bacterial rna polymerase. Cell. 2001 Mar 23;104(6):901-12. [PubMed:11290327 ]
  5. Wehrli W: Rifampin: mechanisms of action and resistance. Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11. [PubMed:6356275 ]
Kind
Protein
Organism
Escherichia coli (strain K12)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna-directed rna polymerase activity
Specific Function:
DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates.
Gene Name:
rpoC
Uniprot ID:
P0A8T7
Molecular Weight:
155158.84 Da
References
  1. Villain-Guillot P, Bastide L, Gualtieri M, Leonetti JP: Progress in targeting bacterial transcription. Drug Discov Today. 2007 Mar;12(5-6):200-8. Epub 2007 Feb 5. [PubMed:17331884 ]
  2. White RJ, Lancini GC, Silvestri LG: Mechanism of action of rifampin on Mycobacterium smegmatis. J Bacteriol. 1971 Nov;108(2):737-41. [PubMed:4942761 ]
  3. Tupin A, Gualtieri M, Roquet-Baneres F, Morichaud Z, Brodolin K, Leonetti JP: Resistance to rifampicin: at the crossroads between ecological, genomic and medical concerns. Int J Antimicrob Agents. 2010 Jun;35(6):519-23. doi: 10.1016/j.ijantimicag.2009.12.017. Epub 2010 Feb 24. [PubMed:20185278 ]
  4. Campbell EA, Korzheva N, Mustaev A, Murakami K, Nair S, Goldfarb A, Darst SA: Structural mechanism for rifampicin inhibition of bacterial rna polymerase. Cell. 2001 Mar 23;104(6):901-12. [PubMed:11290327 ]
  5. Wehrli W: Rifampin: mechanisms of action and resistance. Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11. [PubMed:6356275 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and is...
Gene Name:
NR1I2
Uniprot ID:
O75469
Molecular Weight:
49761.245 Da
References
  1. Chen J, Raymond K: Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor. Ann Clin Microbiol Antimicrob. 2006 Feb 15;5:3. [PubMed:16480505 ]
  2. Cheng J, Ma X, Krausz KW, Idle JR, Gonzalez FJ: Rifampicin-activated human pregnane X receptor and CYP3A4 induction enhance acetaminophen-induced toxicity. Drug Metab Dispos. 2009 Aug;37(8):1611-21. doi: 10.1124/dmd.109.027565. Epub 2009 May 21. [PubMed:19460945 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, 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. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sterol 14-demethylase activity
Specific Function:
Catalyzes C14-demethylation of lanosterol; it transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.
Gene Name:
CYP51A1
Uniprot ID:
Q16850
Molecular Weight:
56805.26 Da
References
  1. Ekins S, Mankowski DC, Hoover DJ, Lawton MP, Treadway JL, Harwood HJ Jr: Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. Drug Metab Dispos. 2007 Mar;35(3):493-500. Epub 2006 Dec 28. [PubMed:17194716 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Baneres-Roquet F, Gualtieri M, Villain-Guillot P, Pugniere M, Leonetti JP: Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions. Antimicrob Agents Chemother. 2009 Apr;53(4):1528-31. doi: 10.1128/AAC.00971-08. Epub 2009 Jan 21. [PubMed:19164148 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [PubMed:22541068 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. [PubMed:17639026 ]
  2. 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
inducer
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 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
substrateinhibitorinducer
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. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. [PubMed:17639026 ]
  2. 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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Ellis E, Wagner M, Lammert F, Nemeth A, Gumhold J, Strassburg CP, Kylander C, Katsika D, Trauner M, Einarsson C, Marschall HU: Successful treatment of severe unconjugated hyperbilirubinemia via induction of UGT1A1 by rifampicin. J Hepatol. 2006 Jan;44(1):243-5. Epub 2005 Oct 27. [PubMed:16288819 ]
  2. Jemnitz K, Lengyel G, Vereczkey L: In vitro induction of bilirubin conjugation in primary rat hepatocyte culture. Biochem Biophys Res Commun. 2002 Feb 15;291(1):29-33. [PubMed:11829457 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. [PubMed:17639026 ]
  3. 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
inducer
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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. [PubMed:17639026 ]
  2. 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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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
substrateinhibitorinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 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
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 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
inducer
General Function:
Monooxygenase activity
Specific Function:
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name:
CYP3A43
Uniprot ID:
Q9HB55
Molecular Weight:
57669.21 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
inducer
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Leukotriene-b4 20-monooxygenase activity
Specific Function:
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 20-hydroxyeicosatetraenoic acid (20-HETE).
Gene Name:
CYP4A11
Uniprot ID:
Q02928
Molecular Weight:
59347.31 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. Geick A, Eichelbaum M, Burk O: Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001 May 4;276(18):14581-7. Epub 2001 Jan 31. [PubMed:11297522 ]
  2. Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764 ]
  3. Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, Kroemer HK: The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest. 1999 Jul;104(2):147-53. [PubMed:10411543 ]
  4. Fardel O, Lecureur V, Loyer P, Guillouzo A: Rifampicin enhances anti-cancer drug accumulation and activity in multidrug-resistant cells. Biochem Pharmacol. 1995 May 11;49(9):1255-60. [PubMed:7763306 ]
  5. Collett A, Tanianis-Hughes J, Hallifax D, Warhurst G: Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26. [PubMed:15180340 ]
  6. Kuypers DR, Verleden G, Naesens M, Vanrenterghem Y: Drug interaction between mycophenolate mofetil and rifampin: possible induction of uridine diphosphate-glucuronosyltransferase. Clin Pharmacol Ther. 2005 Jul;78(1):81-8. [PubMed:16003296 ]
  7. Gurley BJ, Barone GW, Williams DK, Carrier J, Breen P, Yates CR, Song PF, Hubbard MA, Tong Y, Cheboyina S: Effect of milk thistle (Silybum marianum) and black cohosh (Cimicifuga racemosa) supplementation on digoxin pharmacokinetics in humans. Drug Metab Dispos. 2006 Jan;34(1):69-74. Epub 2005 Oct 12. [PubMed:16221754 ]
  8. Chen J, Raymond K: Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor. Ann Clin Microbiol Antimicrob. 2006 Feb 15;5:3. [PubMed:16480505 ]
  9. Lamba J, Strom S, Venkataramanan R, Thummel KE, Lin YS, Liu W, Cheng C, Lamba V, Watkins PB, Schuetz E: MDR1 genotype is associated with hepatic cytochrome P450 3A4 basal and induction phenotype. Clin Pharmacol Ther. 2006 Apr;79(4):325-38. Epub 2006 Feb 20. [PubMed:16580901 ]
  10. Huang R, Murry DJ, Kolwankar D, Hall SD, Foster DR: Vincristine transcriptional regulation of efflux drug transporters in carcinoma cell lines. Biochem Pharmacol. 2006 Jun 14;71(12):1695-704. Epub 2006 Apr 18. [PubMed:16620787 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [PubMed:11134001 ]
  2. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
  3. Cui Y, Konig J, Keppler D: Vectorial transport by double-transfected cells expressing the human uptake transporter SLC21A8 and the apical export pump ABCC2. Mol Pharmacol. 2001 Nov;60(5):934-43. [PubMed:11641421 ]
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. Courtois A, Payen L, Vernhet L, de Vries EG, Guillouzo A, Fardel O: Inhibition of multidrug resistance-associated protein (MRP) activity by rifampicin in human multidrug-resistant lung tumor cells. Cancer Lett. 1999 May 3;139(1):97-104. [PubMed:10408915 ]
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 taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
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. 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 ]
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. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
  2. Fattinger K, Cattori V, Hagenbuch B, Meier PJ, Stieger B: Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2. Hepatology. 2000 Jul;32(1):82-6. [PubMed:10869292 ]
  3. 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 ]
  4. van Montfoort JE, Stieger B, Meijer DK, Weinmann HJ, Meier PJ, Fattinger KE: Hepatic uptake of the magnetic resonance imaging contrast agent gadoxetate by the organic anion transporting polypeptide Oatp1. J Pharmacol Exp Ther. 1999 Jul;290(1):153-7. [PubMed:10381771 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulfate, allopurinol, 5-fluorouracil, paclitaxel, L-ascorbic acid, salicylate, ethotrexate, and alpha-ketoglutarate.
Gene Name:
SLC22A7
Uniprot ID:
Q9Y694
Molecular Weight:
60025.025 Da
References
  1. Sekine T, Cha SH, Tsuda M, Apiwattanakul N, Nakajima N, Kanai Y, Endou H: Identification of multispecific organic anion transporter 2 expressed predominantly in the liver. FEBS Lett. 1998 Jun 12;429(2):179-82. [PubMed:9650585 ]
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. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [PubMed:11134001 ]
  2. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. [PubMed:12085361 ]
  3. 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 ]
  4. Sharma P, Holmes VE, Elsby R, Lambert C, Surry D: Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions. Xenobiotica. 2010 Jan;40(1):24-37. doi: 10.3109/00498250903351013. [PubMed:19919292 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name:
ABCC5
Uniprot ID:
O15440
Molecular Weight:
160658.8 Da
References
  1. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Kauffmann HM, Pfannschmidt S, Zoller H, Benz A, Vorderstemann B, Webster JI, Schrenk D: Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression. Toxicology. 2002 Feb 28;171(2-3):137-46. [PubMed:11836020 ]
  2. Fromm MF, Kauffmann HM, Fritz P, Burk O, Kroemer HK, Warzok RW, Eichelbaum M, Siegmund W, Schrenk D: The effect of rifampin treatment on intestinal expression of human MRP transporters. Am J Pathol. 2000 Nov;157(5):1575-80. [PubMed:11073816 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Teng S, Jekerle V, Piquette-Miller M: Induction of ABCC3 (MRP3) by pregnane X receptor activators. Drug Metab Dispos. 2003 Nov;31(11):1296-9. [PubMed:14570758 ]
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Drug created on June 13, 2005 07:24 / Updated on January 17, 2014 14:51