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Identification
NameRifapentine
Accession NumberDB01201  (APRD01217)
TypeSmall Molecule
GroupsApproved
Description

Rifapentine is an antibiotic drug used in the treatment of tuberculosis. It inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme.

Structure
Thumb
Synonyms
3-(((4-Cyclopentyl-1-piperazinyl)imino)methyl)rifamycin
Cyclopentylrifampicin
Priftin (tn)
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Priftintablet, film coated150 mg/1oralSanofi Aventis U.S. Llc1998-06-22Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIXJM390A33U
CAS number61379-65-5
WeightAverage: 877.0307
Monoisotopic: 876.452073532
Chemical FormulaC47H64N4O12
InChI KeyInChIKey=WDZCUPBHRAEYDL-GZAUEHORSA-N
InChI
InChI=1S/C47H64N4O12/c1-24-13-12-14-25(2)46(59)49-37-32(23-48-51-20-18-50(19-21-51)31-15-10-11-16-31)41(56)34-35(42(37)57)40(55)29(6)44-36(34)45(58)47(8,63-44)61-22-17-33(60-9)26(3)43(62-30(7)52)28(5)39(54)27(4)38(24)53/h12-14,17,22-24,26-28,31,33,38-39,43,53-57H,10-11,15-16,18-21H2,1-9H3,(H,49,59)/b13-12+,22-17+,25-14-,48-23+/t24-,26+,27+,28+,33-,38-,39+,43+,47-/m0/s1
IUPAC Name
(7S,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-26-[(1E)-[(4-cyclopentylpiperazin-1-yl)imino]methyl]-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1⁴,⁷.0⁵,²⁸]triaconta-1(28),2,4,9,19,21,25(29),26-octaen-13-yl acetate
SMILES
CO[[email protected]]1\C=C\O[C@@]2(C)OC3=C(C2=O)C2=C(C(O)=C3C)C(O)=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(\C=N\N1CCN(CC1)C1CCCC1)=C2O
Taxonomy
ClassificationNot classified
Pharmacology
IndicationFor the treatment of pulmonary tuberculosis.
PharmacodynamicsRifapentine 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 actionRifapentine has shown higher bacteriostatic and bactericidal activities especially against intracellular bacteria growing in human monocyte-derived macrophages. Rifapentine inhibits DNA-dependent RNA polymerase in susceptible strains of M. tuberculosis. Rifapentine acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
Related Articles
AbsorptionRapidly and well absorbed from the gastrointestinal tract.
Volume of distribution
  • 70.2 ± 9.1 L
Protein binding97.7% (bound to plasma proteins)
Metabolism

Hepatic

Route of eliminationFollowing a single 600 mg oral dose of radiolabeled rifapentine to healthy volunteers (n=4), 87% of the total 14C rifapentine was recovered in the urine (17%) and feces (70%).
Half lifeNot Available
Clearance
  • Apparent Oral cl=2.51 +/- 0.14 L/h [Male tuberculosis patients who received 600 mg rifapentine in combination with isoniazid, pyrazinamide and ethambutol]
  • Apparent Oral cl=1.69 +/- 0.41 L/h [Female tuberculosis patients who received 600 mg rifapentine in combination with isoniazid, pyrazinamide and ethambutol]
ToxicityNot Available
Affected organisms
  • Mycobacterium tuberculosis
  • Mycobacterium
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.6848
Blood Brain Barrier-0.9659
Caco-2 permeable-0.6609
P-glycoprotein substrateSubstrate0.8997
P-glycoprotein inhibitor IInhibitor0.7632
P-glycoprotein inhibitor IINon-inhibitor0.5252
Renal organic cation transporterNon-inhibitor0.8267
CYP450 2C9 substrateNon-substrate0.8555
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7246
CYP450 1A2 substrateNon-inhibitor0.8865
CYP450 2C9 inhibitorNon-inhibitor0.8436
CYP450 2D6 inhibitorNon-inhibitor0.9073
CYP450 2C19 inhibitorNon-inhibitor0.8449
CYP450 3A4 inhibitorNon-inhibitor0.7042
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8274
Ames testNon AMES toxic0.598
CarcinogenicityNon-carcinogens0.8187
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3722 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9221
hERG inhibition (predictor II)Inhibitor0.6821
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedoral150 mg/1
Prices
Unit descriptionCostUnit
Priftin 150 mg tablet3.96USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0213 mg/mLALOGPS
logP4.83ALOGPS
logP3.56ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)7.01ChemAxon
pKa (Strongest Basic)7.98ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count14ChemAxon
Hydrogen Donor Count6ChemAxon
Polar Surface Area220.15 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity242 m3·mol-1ChemAxon
Polarizability93.14 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesJ04AB05
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (1.74 MB)
MSDSDownload (58.3 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Abiraterone can be decreased when it is combined with Rifapentine.
AlfentanilThe serum concentration of Alfentanil can be decreased when it is combined with Rifapentine.
AmlodipineThe serum concentration of Amlodipine can be decreased when it is combined with Rifapentine.
AmrinoneThe serum concentration of Amrinone can be decreased when it is combined with Rifapentine.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Rifapentine.
ApremilastThe serum concentration of Apremilast can be decreased when it is combined with Rifapentine.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Rifapentine.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Rifapentine resulting in a loss in efficacy.
AtovaquoneThe serum concentration of Atovaquone can be decreased when it is combined with Rifapentine.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Rifapentine.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Rifapentine.
BepridilThe serum concentration of Bepridil can be decreased when it is combined with Rifapentine.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Rifapentine.
BortezomibThe serum concentration of Bortezomib can be decreased when it is combined with Rifapentine.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Rifapentine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Rifapentine.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Rifapentine.
BuspironeThe serum concentration of Buspirone can be decreased when it is combined with Rifapentine.
ButabarbitalThe metabolism of Butabarbital can be increased when combined with Rifapentine.
ButethalThe metabolism of Butethal can be increased when combined with Rifapentine.
CabozantinibThe serum concentration of Cabozantinib can be decreased when it is combined with Rifapentine.
CannabidiolThe serum concentration of Cannabidiol can be decreased when it is combined with Rifapentine.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Rifapentine.
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Rifapentine.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Rifapentine.
ClopidogrelThe risk or severity of adverse effects can be increased when Rifapentine is combined with Clopidogrel.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Rifapentine.
CobicistatThe serum concentration of Cobicistat can be decreased when it is combined with Rifapentine.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Rifapentine.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Rifapentine.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Rifapentine.
DapsoneThe metabolism of Dapsone can be increased when combined with Rifapentine.
DarunavirThe serum concentration of Darunavir can be decreased when it is combined with Rifapentine.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Rifapentine.
DelavirdineThe metabolism of Delavirdine can be increased when combined with Rifapentine.
DexamethasoneThe serum concentration of Dexamethasone can be decreased when it is combined with Rifapentine.
DiclofenacThe serum concentration of Diclofenac can be decreased when it is combined with Rifapentine.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Rifapentine.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Rifapentine.
DronabinolThe serum concentration of Dronabinol can be decreased when it is combined with Rifapentine.
DronedaroneThe serum concentration of Dronedarone can be decreased when it is combined with Rifapentine.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Rifapentine.
ElvitegravirThe serum concentration of Elvitegravir can be decreased when it is combined with Rifapentine.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Rifapentine.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Rifapentine.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Rifapentine.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Rifapentine.
EverolimusThe serum concentration of Everolimus can be decreased when it is combined with Rifapentine.
ExemestaneThe serum concentration of Exemestane can be decreased when it is combined with Rifapentine.
FelodipineThe serum concentration of Felodipine can be decreased when it is combined with Rifapentine.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Rifapentine.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Rifapentine.
FludrocortisoneThe serum concentration of Fludrocortisone can be decreased when it is combined with Rifapentine.
FlunarizineThe serum concentration of Flunarizine can be decreased when it is combined with Rifapentine.
FlunisolideThe metabolism of Flunisolide can be increased when combined with Rifapentine.
GabapentinThe serum concentration of Gabapentin can be decreased when it is combined with Rifapentine.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Rifapentine.
GuanfacineThe serum concentration of Guanfacine can be decreased when it is combined with Rifapentine.
HeptabarbitalThe metabolism of Heptabarbital can be increased when combined with Rifapentine.
HexobarbitalThe metabolism of Hexobarbital can be increased when combined with Rifapentine.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Rifapentine.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Rifapentine.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Rifapentine.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Rifapentine.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be increased when Ifosfamide is used in combination with Rifapentine.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Rifapentine.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Rifapentine 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 Rifapentine resulting in a loss in efficacy.
IsoniazidRifapentine may increase the hepatotoxic activities of Isoniazid.
IsradipineThe serum concentration of Isradipine can be decreased when it is combined with Rifapentine.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Rifapentine.
IvabradineThe serum concentration of Ivabradine can be decreased when it is combined with Rifapentine.
IvacaftorThe serum concentration of Ivacaftor can be decreased when it is combined with Rifapentine.
IxabepiloneThe serum concentration of Ixabepilone can be decreased when it is combined with Rifapentine.
KetoconazoleThe serum concentration of Rifapentine can be increased when it is combined with Ketoconazole.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Rifapentine.
LapatinibThe serum concentration of Lapatinib can be decreased when it is combined with Rifapentine.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Rifapentine.
LercanidipineThe serum concentration of Lercanidipine can be decreased when it is combined with Rifapentine.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Rifapentine.
LumefantrineThe serum concentration of Lumefantrine can be decreased when it is combined with Rifapentine.
LurasidoneThe serum concentration of Lurasidone can be decreased when it is combined with Rifapentine.
MacitentanThe serum concentration of MACITENTAN can be decreased when it is combined with Rifapentine.
Magnesium SulfateThe serum concentration of Magnesium Sulfate can be decreased when it is combined with Rifapentine.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Rifapentine.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Rifapentine.
MethohexitalThe metabolism of Methohexital can be increased when combined with Rifapentine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Rifapentine.
MifepristoneThe serum concentration of Mifepristone can be decreased when it is combined with Rifapentine.
MorphineThe serum concentration of Morphine can be decreased when it is combined with Rifapentine.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Rifapentine.
NaloxegolThe serum concentration of Naloxegol can be decreased when it is combined with Rifapentine.
NetupitantThe serum concentration of Netupitant can be decreased when it is combined with Rifapentine.
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Rifapentine.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Rifapentine.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Rifapentine.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Rifapentine.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Rifapentine.
NitrendipineThe serum concentration of Nitrendipine can be decreased when it is combined with Rifapentine.
NorethisteroneThe serum concentration of Norethindrone can be decreased when it is combined with Rifapentine.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Rifapentine.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Rifapentine.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Rifapentine.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Rifapentine.
PentobarbitalThe metabolism of Pentobarbital can be increased when combined with Rifapentine.
PerampanelThe serum concentration of Perampanel can be decreased when it is combined with Rifapentine.
PerhexilineThe serum concentration of Perhexiline can be decreased when it is combined with Rifapentine.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rifapentine.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Rifapentine.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Rifapentine.
PraziquantelThe serum concentration of Praziquantel can be decreased when it is combined with Rifapentine.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Rifapentine.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Rifapentine.
PrenylamineThe serum concentration of Prenylamine can be decreased when it is combined with Rifapentine.
PrimidoneThe metabolism of Primidone can be increased when combined with Rifapentine.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Rifapentine.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Rifapentine.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Rifapentine.
RaltegravirThe serum concentration of Raltegravir can be increased when it is combined with Rifapentine.
RamelteonThe metabolism of Ramelteon can be increased when combined with Rifapentine.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Rifapentine.
RegorafenibThe serum concentration of Regorafenib can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Rifapentine.
RisedronateThe serum concentration of Risedronate can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Rifapentine.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Rifapentine.
RoflumilastThe serum concentration of Roflumilast can be decreased when it is combined with Rifapentine.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Rifapentine.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Rifapentine.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifapentine.
SecobarbitalThe metabolism of Secobarbital can be increased when combined with Rifapentine.
SildenafilThe metabolism of Sildenafil can be increased when combined with Rifapentine.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Rifapentine.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Rifapentine.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Rifapentine.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Rifapentine.
SunitinibThe serum concentration of Sunitinib can be decreased when it is combined with Rifapentine.
SuvorexantThe serum concentration of Suvorexant can be decreased when it is combined with Rifapentine.
TacrolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Rifapentine.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Rifapentine.
TamoxifenThe metabolism of Tamoxifen can be increased when combined with Rifapentine.
TasimelteonThe serum concentration of Tasimelteon can be decreased when it is combined with Rifapentine.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Rifapentine.
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Rifapentine.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Rifapentine resulting in a loss in efficacy.
TofacitinibThe serum concentration of Tofacitinib can be decreased when it is combined with Rifapentine.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Rifapentine.
TorasemideThe metabolism of Torasemide can be increased when combined with Rifapentine.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Rifapentine.
TrabectedinThe serum concentration of Trabectedin can be decreased when it is combined with Rifapentine.
TreprostinilThe serum concentration of Treprostinil can be decreased when it is combined with Rifapentine.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Rifapentine.
VandetanibThe serum concentration of Vandetanib can be decreased when it is combined with Rifapentine.
VemurafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Rifapentine.
VerapamilThe serum concentration of Verapamil can be decreased when it is combined with Rifapentine.
VilazodoneThe serum concentration of Vilazodone can be decreased when it is combined with Rifapentine.
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Rifapentine.
VorapaxarThe serum concentration of Vorapaxar can be decreased when it is combined with Rifapentine.
VoriconazoleThe serum concentration of Rifapentine can be increased when it is combined with Voriconazole.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Rifapentine.
ZaleplonThe serum concentration of Zaleplon can be decreased when it is combined with Rifapentine.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Rifapentine.
ZolpidemThe serum concentration of Zolpidem can be decreased when it is combined with Rifapentine.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be decreased when it is combined with Rifapentine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Mycobacterium tuberculosis
Pharmacological action
yes
Actions
inhibitor
General Function:
Transcription
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:
P0A674
Molecular Weight:
146771.0 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Williams DL, Spring L, Collins L, Miller LP, Heifets LB, Gangadharam PR, Gillis TP: Contribution of rpoB mutations to development of rifamycin cross-resistance in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 1998 Jul;42(7):1853-7. [PubMed:9661035 ]
  4. 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 ]

Enzymes

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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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 ]
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Drug created on June 13, 2005 07:24 / Updated on October 04, 2013 10:56