Banner
Identification
Name Rifampin
Accession Number DB01045 (APRD00207, EXPT02777)
Type small molecule
Groups approved
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
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
RFP
Rifampicin
Rifampin
Salts Not Available
Brand names
Name Company
Archidyn
Rifadin
Rifadine
Rifagen
Rifaldin
Rifaprodin
Rifoldin
Rifoldine
Riforal
Rimactan
Rimactane
Rimactin
Rimazid
Rofact
Tubocin
First Prev Next Last
Brand mixtures
Brand Name Ingredients
Rifamate Rifampin + Isoniazid
Rifater Isoniazid + Pyrazinaamide + Rifampin
Categories
  • Enzyme Inhibitors
  • Antituberculosis Agents
  • Nucleic Acid Synthesis Inhibitors
  • Leprostatic Agents
  • Antibiotics
  • Antibiotics, Antitubercular
CAS number 13292-46-1
Weight Average: 822.9402
Monoisotopic: 822.40512334
Chemical Formula C43H58N4O12
InChI Key InChIKey=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
Plain Text
IUPAC Name
(7S,11S,12R,13S,14R,15R,16R,17S,18S)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-[(E)-N-(4-methylpiperazin-1-yl)carboximidoyl]-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1^{4,7}.0^{5,28}]triaconta-1,3,5(28),9,19,21,25(29),26-octaen-13-yl acetate
SMILES
CO[C@H]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/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)C(O)=C2C(O)=C3C
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections.
Pharmacodynamics Rifampin 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 action Rifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
Absorption Well absorbed from gastrointestinal tract.
Volume of distribution Not Available
Protein binding 89%
Metabolism Primarily hepatic, rapidly deacetylated.
Route of elimination Less than 30% of the dose is excreted in the urine as rifampin or metabolites.
Half life 3.35 (+/- 0.66) hours
Clearance
  • 0.19 +/- 0.06 L/hr/kg [300 mg IV]
  • 0.14 +/- 0.03 L/hr/kg [600 mg IV]
Toxicity LD50=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness
Affected organisms
  • Mycobacteria
  • Various gram-negative and gram-positive eubacteria
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
  • Lannett holdings inc
  • Sandoz inc
  • Versapharm inc
  • Actavis totowa llc
  • Akorn strides llc
  • Bedford laboratories div ben venue laboratories inc
Packagers
Dosage forms
Form Route Strength
Capsule Oral
Prices
Unit description Cost Unit
Rifadin iv 600 mg vial 140.9 USD vial
Rifampin iv 600 mg vial 136.3 USD vial
Rifampin crystals 6.72 USD g
Rifampin powder 3.98 USD g
Rifadin 300 mg capsule 3.09 USD capsule
Rifadin 150 mg capsule 2.57 USD capsule
Rifampin 300 mg capsule 2.37 USD capsule
Rimactane 300 mg capsule 2.35 USD capsule
Rifampin 150 mg capsule 2.27 USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents Not Available
Properties
State solid
Experimental Properties
Property Value Source
melting point 183 °C Not Available
water solubility 1400 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 2.7 Not Available
pKa 1.7 SANGSTER (2004)
Predicted Properties
Property Value Source
water solubility 4.13e-02 g/l ALOGPS
logP 3.85 ALOGPS
logP 2.77 ChemAxon
logS -4.3 ALOGPS
pKa (strongest acidic) 6.9 ChemAxon
pKa (strongest basic) 7.53 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 14 ChemAxon
hydrogen donor count 6 ChemAxon
polar surface area 220.15 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 225.58 ChemAxon
polarizability 86.46 ChemAxon
References
Synthesis Reference Not Available
General Reference
  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. Epub 2008 Mar 18. Pubmed
External Links
Resource Link
KEGG Drug D00211 Link_out
KEGG Compound C06688 Link_out
ChEBI 28077 Link_out
ChEMBL 28077 Link_out
Therapeutic Targets Database DNC000965 Link_out
PharmGKB PA451250 Link_out
IUPHAR 2765 Link_out
Guide to Pharmacology 2765 Link_out
Drug Product Database 393444 Link_out
RxList http://www.rxlist.com/cgi/generic2/rifampin.htm Link_out
Drugs.com http://www.drugs.com/cdi/rifampin.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Rifampin Link_out
ATC Codes
  • J04AB02
AHFS Codes
  • 08:16.04
PDB Entries
FDA label show (43.3 KB)
MSDS show (86.7 KB)
Interactions
Drug Interactions
Drug Interaction
Acenocoumarol Rifampin may decrease the anticoagulant effect of acenocoumarol by increasing its metabolism.
Acetohexamide Rifampin may decrease the effect of sulfonylurea, acetohexamide.
Alfentanil Rifampin reduces levels and efficacy of alfentanil
Aminophylline Rifampin decreases the effect of theophylline
Amiodarone Rifampin decreases the effect of amiodarone
Amitriptyline The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, amitriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if rifampin is initiated, discontinued or dose changed.
Amoxapine The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, amoxapine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amoxapine if rifampin is initiated, discontinued or dose changed.
Amprenavir In presence of rifampin anticipate decrease of amprenavir efficiency
Anisindione Rifampin may decrease the anticoagulant effect of anisindione.
Aprepitant The CYP3A4 inducer, rifampin, may decrease the effect of aprepitant.
Artemether Oral administration of rifampin, a strong CYP3A4 inducer, with Coartem Tablets resulted in significant decreases in exposure to artemether, dihydroartemisinin (DHA, metabolite of artemether) and lumefantrine by 89%, 85% and 68%, respectively, when compared to exposure values after Coartem Tablets alone. Concomitant use of strong inducers of CYP3A4 such as rifampin, carbamazepine, phenytoin and St. John’s wort is contraindicated with Coartem Tablets.
Atazanavir Rifampin reduces levels and efficacy of atazanavir
Atorvastatin Rifampin may decrease the effect of atorvastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of atorvastatin if rifampin is initiated, discontinued or dose changed.
Atovaquone Rifampin may decrease the effect of atovaquone.
Bendamustine CYP1A2 metabolism may result in increased levels of active metabolites, decreases levels of bendamustine.
Betamethasone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, betamethasone.
Bisoprolol Rifampin may decrease the serum concentration of bisprolol by increasing its metabolism.
Bromazepam Rifampin may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifampin is initiated, discontinued or dose changed.
Bupropion Rifampin reduces bupropion levels
Buspirone Rifampin decreases the effect of buspirone
Cabazitaxel Concomitant therapy with a strong CYP3A inducer may decrease concentrations of cabazitaxel. Avoid concomitant therapy.
Caspofungin Decreased levels/effects of caspofungin
Celecoxib Rifampin, a strong CYP2C9 inducer, may decrease the serum levels of celecoxib by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects if rifampin is initiated, discontinued or dose changed.
Cerivastatin Rifampin may decrease the effect of cerivastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of cerivastatin if rifampin is initiated, discontinued or dose changed.
Chloramphenicol Rifampin decreases the effect of chloramphenicol
Chlorpropamide Rifampin may decrease the effect of sulfonylurea, chlorpropamide.
Clarithromycin The rifamycin, rifampin, may decrease the effect of the macrolide, clarithromycin.
Clomipramine The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, clomipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of clomipramine if rifampin is initiated, discontinued or dose changed.
Clozapine Rifampin decreases the effect of clozapine
Cortisone acetate The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, cortisone acetate.
Cyclosporine The rifamycin decreases the effect of cyclosporine
Dabigatran etexilate P-Glycoprotein inducers such as rifampin may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
Dapsone Decreased levels of dapsone
Dasatinib Rifampin may decrease the serum level and efficacy of dasatinib.
Delavirdine Rifampin decreases the effect of delavirdine
Desipramine The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, desipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if rifampin is initiated, discontinued or dose changed.
Dexamethasone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, dexamethasone.
Diazepam Rifampin may decrease the effect of the benzodiazepine, diazepam.
Diclofenac Rifampin, a CYP2C9 inducer, may increase the metabolism of diclofenac.
Dicumarol Rifampin may decrease the anticoagulant effect of dicumarol.
Diltiazem Rifampin decreases levels of diltiazem
Disopyramide Rifampin decreases the effect of disopyramide
Doxepin The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, doxepin, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of doxepin if rifampin is initiated, discontinued or dose changed.
Doxycycline The rifamycin decreases the effect of doxycycline
Dyphylline Rifampin decreases the effect of theophylline
Enalapril Rifampin, a strong CYP3A4 inducer, may increase the metabolism of enalapril. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of enalapril if rifampin is initiated, discontinued or dose changed.
Erlotinib Decreased levels/effect of erlotinib
Erythromycin The rifamycin, rifampin, may decrease the effect of the macrolide, erythromycin.
Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
Ethotoin Rifampin decreases the effect of the hydantoin
Etoricoxib Rifampin reduces levels and efficacy of etoricoxib
Fentanyl Rifampin may decrease the serum level and therapeutic effect of fentanyl.
Fluconazole Rifampin may decrease the effect of fluconazole.
Fludrocortisone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, fludrocortisone.
Fluvastatin Rifampin may decrease the effect of fluvastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of fluvastatin if rifampin is initiated, discontinued or dose changed.
Fosamprenavir Rifampin may decrease the effectiveness of fosamprenavir.
Fosphenytoin Rifampin may decrease the effect of fosphenytoin.
Gefitinib Rifampin reduces levels and efficacy of gefitinib
Gliclazide Rifampin may decrease the effect of sulfonylurea, gliclazide.
Glimepiride Rifampin may decrease the effect of sulfonylurea, glimepiride.
Glipizide Rifampin may decrease the effect of sulfonylurea, glipizide.
Glisoxepide Rifampin may decrease the effect of sulfonylurea, glisoxepide.
Glyburide Rifampin may decrease the effect of sulfonylurea, glibenclamide.
Glycodiazine Rifampin may decrease the effect of sulfonylurea, glycodiazine.
Haloperidol The rifamycin decreases the effect of haloperidol
Hydrocortisone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, hydrocortisone.
Imatinib Rifampin decreases levels of imatinib
Imipramine The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, imipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of imipramine if rifampin is initiated, discontinued or dose changed.
Indinavir Rifampin decreases the effect of indinavir
Itraconazole Rifampin may decrease the effect of itraconazole.
Josamycin The rifamycin, rifampin, may decrease the effect of the macrolide, josamycin.
Ketoconazole Rifampin may decrease the effect of ketoconazole.
Lamotrigine Rifampin decreases levels of lamotrigine
Leflunomide Rifampin increases the effect of leflunomide
Losartan Rifampin decreases the effect of losartan
Lovastatin Rifampin may decrease the effect of lovastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of lovastatin if rifampin is initiated, discontinued or dose changed.
Mefloquine Rifampin lowers mefloquine levels
Mephenytoin Rifampin decreases the effect of the hydantoin
Mestranol This product may cause a slight decrease of contraceptive effect
Methadone The rifamycin decreases the effect of methadone
Methylprednisolone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, methylprednisolone.
Metoprolol Rifampin may decrease the serum concentration of metoprolol by increasing its metabolism.
Mexiletine Rifampin decreases the effect of mexiletine
Midazolam Rifampin may increase the metabolism of midazolam. Monitor for changes in the therapeutic and adverse effects of midazolam if rifampin is initiated, discontinued or dose changed.
Morphine Rifampin decreases the effect of morphine/codeine
Mycophenolate mofetil Rifampin may decrease the serum concentration of mycophenolate. Concomitant therapy should be avoided.
Nelfinavir Rifampin decreases the effect of nelfinavir
Nifedipine Rifampin decreases the effect of the calcium channel blocker, nifedipine.
Norethindrone This product may cause a slight decrease of contraceptive effect
Nortriptyline The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, nortriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of nortriptyline if rifampin is initiated, discontinued or dose changed.
Oxtriphylline Rifampin may decrease the effect and toxicity of oxtriphylline.
Paramethasone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, paramethasone.
Pazopanib Concomitant therapy with a CYP3A4 inducer may decrease exposure of pazopanib.
Phenytoin Rifampin may decrease the therapeutic and adverse effects of phenytoin.
Praziquantel Significant decrease in praziquantel level
Prednisolone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisolone.
Prednisone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisone.
Propafenone Rifampin decreases the effect of propafenone
Propranolol Rifampin may decrease the serum concentration of propranolol by increasing its metabolism.
Protriptyline The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, protriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of protriptyline if rifampin is initiated, discontinued or dose changed.
Quinidine Rifampin decreases the effect of quinidine
Quinidine barbiturate Rifampin decreases the effect of quinidine
Ramelteon Rifampin reduces the levels/effect of ramelteon
Repaglinide Rifampin decreases the effect of repaglinide
Ritonavir Rifampin decreases the effect of ritonavir
Rosiglitazone Rifampin reduces levels and efficacy of rosiglitazone
Saquinavir Rifampin decreases the effect of saquinavir
Saxagliptin Rifampin is a strong inducer of CYP3A4 which decreases exposure of saxagliptin. The exposure of the active metabolite, 5-hydroxy saxagliptin, also increases.
Simvastatin Rifampin may decrease the effect of simvastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of simvastatin if rifampin is initiated, discontinued or dose changed.
Sirolimus The rifamycin decreases the effect of sirolimus
Sunitinib Possible decrease in sunitinib levels
Tacrolimus Rifampin may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Rifampin therapy is initiated, discontinued or altered.
Tadalafil Rifampin may reduce Tadalafil plasma concentrations and efficacy.
Tamoxifen The rifamycin decreases the effect of anti-estrogen
Telithromycin Rifampin may decrease the plasma concentration of Telithromycin. Concomitant therapy should be avoided.
Temsirolimus Rifampin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Terbinafine Rifampin may increase the metabolism and clearance of Terbinafine. Co-administration may result in Terbinafine treatment failure.
Theophylline Rifampin decreases the effect of theophylline
Tipranavir Rifampin may decrease the plasma concentration of Tipranavir. Concomitant use is not recommended.
Tocainide Rifampin lowers tocainide levels/effects
Tolazamide Rifampin may decrease the effect of sulfonylurea, tolazamide.
Tolbutamide Rifampin may decrease the effect of sulfonylurea, tolbutamide.
Tolvaptan Rifampin is a CYP3A4 inducer and will decrease serum concentrations of tolvaptan and ultimately, its clinical effects.
Toremifene The rifamycin decreases the effect of anti-estrogen
Tramadol Rifampin may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
Trazodone The CYP3A4 inducer, Rifampin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Rifampin is initiated, discontinued or dose changed.
Tretinoin The strong CYP2C8 inducer, Rifampin, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rifampin is initiated, discontinued or dose changed.
Triamcinolone The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, triamcinolone.
Triazolam Rifampin may decrease the effect of the benzodiazepine, triazolam.
Trimethoprim Rifampin decreases the effect of trimethoprim
Trimipramine The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, trimipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of trimipramine if rifampin is initiated, discontinued or dose changed.
Ulipristal Concomitant therapy with strong CYP3A4 inducers may decrease plasma concentrations of ulipristal and ultimately its effectiveness. Avoid combination therapy.
Valproic Acid Rifampin may reduce the serum concentration of Valproic acid by increasing Valproic acid metabolism. Valproic acid dose adjustments may be required during concomitant therapy. Monitor Valproic acid serum concentrations, efficacy and toxicity if Rifampin is initiated, discontinued or dose changed.
Verapamil Rifampin, a CYP3A4 inducer, may decrease the serum concentration of Verapamil by increasing its metabolism (particularly in the intestinal mucosa) and decreasing its absorption. Monitor for changes in the therapeutic/adverse effects of Verapamil if Rifampin is initiated, discontinued or dose changed.
Voriconazole Rifampin may decrease the serum concentration of voriconazole likely by increasing its metabolism via CYP3A enzymes. Voriconazole may increase the serum concentration of rifampin likely by inhibiting its metabolism via CYP3A. Concomitant therapy is contraindicated.
Warfarin Rifampin may decrease the anticoagulant effect of warfarin by increasing its metabolism.
Zaleplon Rifampin decreases the effect of zaleplon
Zidovudine Rifampin may decrease the serum concentration of zidovudine by increasing its metabolism. Monitor for changes in the serum concentration and therapeutic and adverse effects of zidovudine if rifampin is initiated, discontinued or dose changed.
Food Interactions
  • Avoid alcohol.
  • Take on empty stomach: 1 hour before or 2 hours after meals.
  • Take with a full glass of water.
Targets

1. DNA-directed RNA polymerase beta chain

Pharmacological action: yes
Actions: inhibitor

DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates

Organism class: bacterial
UniProt ID: P0A8V2 Link_out
Gene: rpoB
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  2. White RJ, Lancini GC, Silvestri LG: Mechanism of action of rifampin on Mycobacterium smegmatis. J Bacteriol. 1971 Nov;108(2):737-41. Pubmed
  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. Epub 2010 Feb 24. Pubmed
  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
  5. Wehrli W: Rifampin: mechanisms of action and resistance. Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11. Pubmed

2. DNA-directed RNA polymerase subunit beta'

Pharmacological action: yes
Actions: inhibitor

DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates

Organism class: bacterial
UniProt ID: P0A8T7 Link_out
Gene: rpoC Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  2. White RJ, Lancini GC, Silvestri LG: Mechanism of action of rifampin on Mycobacterium smegmatis. J Bacteriol. 1971 Nov;108(2):737-41. Pubmed
  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. Epub 2010 Feb 24. Pubmed
  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
  5. Wehrli W: Rifampin: mechanisms of action and resistance. Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11. Pubmed

3. Orphan nuclear receptor PXR

Pharmacological action: unknown
Actions: agonist

Orphan receptor; its natural ligand is probably pregnane. Binds to a response element in the CYP3A4 and ABCB1/MDR1 genes promoter. Activates its expression in response to a wide variety of endobiotics and xenobiotics

Organism class: human
UniProt ID: O75469 Link_out
Gene: NR1I2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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. Epub 2009 May 21. Pubmed
Enzymes

1. Cytochrome P450 2C9

Actions: substrate, inducer

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, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 1A2

Actions: inducer

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 N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen

UniProt ID: P05177 Link_out
Gene: CYP1A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 2C8

Actions: substrate, inhibitor, inducer

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 responsible for the metabolism the anti- cancer drug paclitaxel (taxol)

UniProt ID: P10632 Link_out
Gene: CYP2C8
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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
  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. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 3A4

Actions: substrate, inducer

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 xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 2B6

Actions: inducer

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

UniProt ID: P20813 Link_out
Gene: CYP2B6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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
  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. Epub 2009 Nov 24. Pubmed

6. UDP-glucuronosyltransferase 1-1

Actions: inducer

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

UniProt ID: P22309 Link_out
Gene: UGT1A1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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

7. Cytochrome P450 2C19

Actions: inducer

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

UniProt ID: P33261 Link_out
Gene: CYP2C19 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 2A6

Actions: substrate, inhibitor, inducer

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

UniProt ID: P11509 Link_out
Gene: CYP2A6
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 2E1

Actions: inducer

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

UniProt ID: P05181 Link_out
Gene: CYP2E1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 3A43

Actions: inducer

Exhibits low testosterone 6-beta-hydroxylase activity

UniProt ID: Q9HB55 Link_out
Gene: CYP3A43 Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

11. Cytochrome P450 3A5

Actions: inducer

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

UniProt ID: P20815 Link_out
Gene: CYP3A5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

12. Cytochrome P450 3A7

Actions: inducer

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

UniProt ID: P24462 Link_out
Gene: CYP3A7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

13. Cytochrome P450 4A11

Actions: inducer

Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity towards prostaglandins A1 and E1

UniProt ID: Q02928 Link_out
Gene: CYP4A11 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed
Transporters

1. Multidrug resistance protein 1

Actions: substrate, inhibitor, inducer

Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells

UniProt ID: P08183 Link_out
Gene: ABCB1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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
  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
  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
  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
  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
  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
  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
  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

2. Solute carrier organic anion transporter family member 1B3

Actions: substrate, inhibitor

Mediates the Na(+)-independent transport of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP)

UniProt ID: Q9NPD5 Link_out
Gene: SLCO1B3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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

3. Multidrug resistance-associated protein 1

Actions: inhibitor

May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Confers resistance to anticancer drugs. Transports LTC4. May protect milk against xenobiotics

UniProt ID: P33527 Link_out
Gene: ABCC1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

4. Solute carrier organic anion transporter family member 2B1

Actions: inhibitor

Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost

UniProt ID: O94956 Link_out
Gene: SLCO2B1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

5. Bile salt export pump

Actions: inhibitor

Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes

UniProt ID: O95342 Link_out
Gene: ABCB11 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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
  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

6. Solute carrier organic anion transporter family member 1A2

Actions: inhibitor

Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity)

UniProt ID: P46721 Link_out
Gene: SLCO1A2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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
  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

7. Solute carrier family 22 member 7

Actions: inhibitor

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

UniProt ID: Q9Y694 Link_out
Gene: SLC22A7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

8. Solute carrier organic anion transporter family member 1B1

Actions: inhibitor

Mediates the Na(+)-independent transport 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. May play an important role in the clearance of bile acids and organic anions from the liver

UniProt ID: Q9Y6L6 Link_out
Gene: SLCO1B1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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
  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. Pubmed

9. Multidrug resistance-associated protein 5

Actions: inducer

Acts as a multispecific organic anion pump which can transport nucleotide analogs

UniProt ID: O15440 Link_out
Gene: ABCC5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

10. Canalicular multispecific organic anion transporter 1

Actions: inducer

Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter

UniProt ID: Q92887 Link_out
Gene: ABCC2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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

11. Canalicular multispecific organic anion transporter 2

Actions: inducer

May act as an inducible transporter in the biliary and intestinal excretion of organic anions

UniProt ID: O15438 Link_out
Gene: ABCC3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19