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Identification
NamePaclitaxel
Accession NumberDB01229  (APRD00259, DB05261, DB05927)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

Paclitaxel is a mitotic inhibitor used in cancer chemotherapy. It was discovered in a US National Cancer Institute program at the Research Triangle Institute in 1967 when Monroe E. Wall and Mansukh C. Wani isolated it from the bark of the Pacific yew tree, Taxus brevifolia and named it taxol. Later it was discovered that endophytic fungi in the bark synthesize paclitaxel.
When it was developed commercially by Bristol-Myers Squibb (BMS), the generic name was changed to paclitaxel and the BMS compound is sold under the trademark Taxol. In this formulation, paclitaxel is dissolved in Kolliphor EL and ethanol, as a delivery agent. A newer formulation, in which paclitaxel is bound to albumin, is sold under the trademark Abraxane. [Wikipedia]

Structure
Thumb
Synonyms
(2AR-(2aalpha,4beta,4abeta,6beta,9alpha(alpha r*,betas*),11alpha,12alpha,12balpha))-beta-(benzoylamino)-alpha-hydroxybenzenepropanoic acid 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca(3,4)benz(1,2-b)oxet-9-yl ester
5beta,20-Epoxy-1,2-alpha,4,7beta,10beta,13alpha-hexahydroxytax-11-en-9-one 4,10-diacetate 2-benzoate 13-ester with (2R,3S)-N-benzoyl-3-phenylisoserine
Paclitaxel
Taxol
Taxol A
External Identifiers
  • ABI-007
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Abraxaneinjection, powder, lyophilized, for suspension100 mg/20mLintravenousAbraxis Bio Science, Llc2005-02-102016-04-05Us
Abraxane for Injectable Suspensionpowder for suspension100 mgintravenousCelgene Inc2006-08-31Not applicableCanada
Aj-paclitaxelsolution6 mgintravenousAgila Jamp Canada IncNot applicableNot applicableCanada
Paclitaxelliquid6 mgintravenousIvax Pharmaceuticals IncorporatedNot applicableNot applicableCanada
Paclitaxelinjection6 mg/mLintravenousWG Critical Care, LLC2013-07-112016-04-05Us
Paclitaxelinjection6 mg/mLintravenousWG Critical Care, LLC2013-07-112016-04-05Us
Paclitaxelinjection6 mg/mLintravenousWG Critical Care, LLC2013-07-112016-04-05Us
Paclitaxel for Injectionsolution6 mgintravenousTeva Canada LimitedNot applicableNot applicableCanada
Paclitaxel for Injectionsolution6 mgintravenousHospira Healthcare Corporation2007-12-17Not applicableCanada
Paclitaxel for Injectionsolution6 mgintravenousBiolyse Pharma Corporation2001-10-31Not applicableCanada
Paclitaxel for Injection USPsolution6 mgintravenousSterimax Inc2011-02-22Not applicableCanada
Paclitaxel Injectionliquid6 mgintravenousDraxis Health Inc.Not applicableNot applicableCanada
Paclitaxel Injectionliquid6 mgintravenousImmunex Corporation1997-10-242005-12-06Canada
Paclitaxel Injection USPsolution6 mgintravenousSandoz Canada Incorporated2015-03-31Not applicableCanada
Paclitaxel Injection USPsolution6 mgintravenousAccord Healthcare Inc2014-07-02Not applicableCanada
Paclitaxel Injection, USPsolution6 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Paxeneliquid6 mgintravenousBaker Norton Pharmaceuticals Inc.Not applicableNot applicableCanada
Taxolsolution6 mgintravenousBristol Myers Squibb Canada1993-12-312012-07-20Canada
Teva-paclitaxel for Injectionliquid6 mgintravenousTeva Canada LimitedNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-paclitaxel Injectablesolution6 mgintravenousApotex Inc2005-02-07Not applicableCanada
Paclitaxelinjection, solution6 mg/mLintravenousActavis Pharma, Inc.2015-01-052016-04-05Us
Paclitaxelinjection100 mg/16.7mLintravenousPfizer Laboratories Div Pfizer Inc.2011-09-302016-04-23Us
Paclitaxelinjection, solution6 mg/mLintravenousSagent Pharmaceuticals2011-09-272016-04-05Us
Paclitaxelinjection30 mg/5mLintravenousMylan Institutional LLC2011-09-302016-04-05Us
Paclitaxelinjection, solution, concentrate6 mg/mLintravenousTeva Parenteral Medicines, Inc.2009-09-162016-04-05Us
Paclitaxelinjection100 mg/16.7mLintravenousMylan Institutional LLC2011-09-302016-04-05Us
Paclitaxelinjection, solution, concentrate6 mg/mLintravenousTeva Parenteral Medicines, Inc.2008-10-232016-04-05Us
Paclitaxelinjection300 mg/50mLintravenousMylan Institutional LLC2011-09-302016-04-05Us
Paclitaxelinjection, solution, concentrate6 mg/mLintravenousTeva Parenteral Medicines, Inc.2008-09-242016-04-05Us
Paclitaxelinjection, solution6 mg/mLintravenousSandoz Inc2008-01-022016-04-05Us
Paclitaxelinjection, solution, concentrate6 mg/mLintravenousTeva Parenteral Medicines, Inc.2009-11-032016-04-05Us
Paclitaxelinjection, solution6 mg/mLintravenousFresenius Kabi USA, LLC2009-03-202016-04-05Us
Paclitaxelinjection30 mg/5mLintravenousPfizer Laboratories Div Pfizer Inc.2011-09-302016-04-23Us
Paclitaxelinjection, solution6 mg/mLintravenousHospira Worldwide, Inc.2002-05-082016-04-05Us
Paclitaxelinjection300 mg/50mLintravenousPfizer Laboratories Div Pfizer Inc.2011-09-302016-04-23Us
Over the Counter ProductsNot Available
International Brands
NameCompany
OnxolNot Available
PaxceedNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIP88XT4IS4D
CAS number33069-62-4
WeightAverage: 853.9061
Monoisotopic: 853.330955345
Chemical FormulaC47H51NO14
InChI KeyInChIKey=RCINICONZNJXQF-MZXODVADSA-N
InChI
InChI=1S/C47H51NO14/c1-25-31(60-43(56)36(52)35(28-16-10-7-11-17-28)48-41(54)29-18-12-8-13-19-29)23-47(57)40(61-42(55)30-20-14-9-15-21-30)38-45(6,32(51)22-33-46(38,24-58-33)62-27(3)50)39(53)37(59-26(2)49)34(25)44(47,4)5/h7-21,31-33,35-38,40,51-52,57H,22-24H2,1-6H3,(H,48,54)/t31-,32-,33+,35-,36+,37+,38-,40-,45+,46-,47+/m0/s1
IUPAC Name
(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-1,9-dihydroxy-15-{[(2R,3S)-2-hydroxy-3-phenyl-3-(phenylformamido)propanoyl]oxy}-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0³,¹⁰.0⁴,⁷]heptadec-13-en-2-yl benzoate
SMILES
[H][C@]12[[email protected]](OC(=O)C3=CC=CC=C3)[C@]3(O)C[[email protected]](OC(=O)[[email protected]](O)[C@@H](NC(=O)C4=CC=CC=C4)C4=CC=CC=C4)C(C)=C([C@@H](OC(C)=O)C(=O)[C@]1(C)[C@@H](O)C[[email protected]]1OC[C@@]21OC(C)=O)C3(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as taxanes and derivatives. These are diterpenoids with a structure based either on the taxane skeleton, or a derivative thereof. In term of phytochemistry, several derivatives of the taxane skeleton exist
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassPrenol lipids
Sub ClassDiterpenoids
Direct ParentTaxanes and derivatives
Alternative Parents
Substituents
  • Taxane diterpenoid
  • N-benzylbenzamide
  • Beta amino acid or derivatives
  • Phenylpropylamine
  • Benzoate ester
  • Benzylether
  • Benzoic acid or derivatives
  • Benzamide
  • Benzoyl
  • Alpha-acyloxy ketone
  • Fatty acid ester
  • Fatty acyl
  • Benzenoid
  • Monosaccharide
  • Dicarboxylic acid or derivatives
  • Monocyclic benzene moiety
  • Acetate salt
  • Tertiary alcohol
  • Cyclic alcohol
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Oxetane
  • Ketone
  • Carboxylic acid ester
  • Carboxamide group
  • Oxacycle
  • Organoheterocyclic compound
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed in the treatment of Kaposi's sarcoma and cancer of the lung, ovarian, and breast. Abraxane® is specfically indicated for the treatment of metastatic breast cancer and locally advanced or metastatic non-small cell lung cancer.
PharmacodynamicsPaclitaxel is a taxoid antineoplastic agent indicated as first-line and subsequent therapy for the treatment of advanced carcinoma of the ovary, and other various cancers including breast cancer. Paclitaxel is a novel antimicrotubule agent that promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. In addition, paclitaxel induces abnormal arrays or "bundles" of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis.
Mechanism of actionPaclitaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, paclitaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, paclitaxel binds to the β subunit of tubulin. Tubulin is the "building block" of mictotubules, and the binding of paclitaxel locks these building blocks in place. The resulting microtubule/paclitaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that paclitaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis stopping protein called Bcl-2 (B-cell leukemia 2) and thus arresting its function.
Related Articles
AbsorptionWhen a 24 hour infusion of 135 mg/m^2 is given to ovarian cancer patients, the maximum plasma concentration (Cmax) is 195 ng/mL, while the AUC is 6300 ng•h/mL.
Volume of distribution
  • 227 to 688 L/m^2 [apparent volume of distribution at steady-state, 24 hour infusion]
Protein binding89%-98% bound to plasma protein. The presence of cimetidine, ranitidine, dexamethasone, or diphenhydramine did not affect protein binding of paclitaxel.
Metabolism

Hepatic. In vitro studies with human liver microsomes and tissue slices showed that paclitaxel was metabolized primarily to 6a-hydrox-ypaclitaxel by the cytochrome P450 isozyme CYP2C8; and to two minor metabolites, 3’-p-hydroxypaclitaxel and 6a, 3’-p-dihydroxypaclitaxel, by CYP3A4.

SubstrateEnzymesProduct
Paclitaxel
Not Available
3'-p-hydroxypaclitaxelDetails
Paclitaxel
Not Available
6a-hydrox-ypaclitaxelDetails
Paclitaxel
Not Available
6a, 3'-p-dihydroxypaclitaxelDetails
Route of eliminationIn 5 patients administered a 225 or 250 mg/m2 dose of radiolabeled paclitaxel as a 3-hour infusion, a mean of 71% of the radioactivity was excreted in the feces in 120 hours, and 14% was recovered in the urine.
Half lifeWhen a 24 hour infusion of 135 mg/m^2 is given to ovarian cancer patients, the elimination half=life is 52.7 hours.
Clearance
  • 21.7 L/h/m2 [Dose 135 mg/m2, infusion duration 24 h]
  • 23.8 L/h/m2 [Dose 175 mg/m2, infusion duration 24 h]
  • 7 L/h/m2 [Dose 135 mg/m2, infusion duration 3 h]
  • 12.2 L/h/m2 [Dose 175 mg/m2, infusion duration 3 h]
ToxicityRat (ipr) LD50=32530 µg/kg. Symptoms of overdose include bone marrow suppression, peripheral neurotoxicity, and mucositis. Overdoses in pediatric patients may be associated with acute ethanol toxicity.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Paclitaxel Action PathwayDrug actionSMP00434
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.914
Blood Brain Barrier-0.9748
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.8345
P-glycoprotein inhibitor IInhibitor0.5509
P-glycoprotein inhibitor IINon-inhibitor0.7309
Renal organic cation transporterNon-inhibitor0.9349
CYP450 2C9 substrateNon-substrate0.837
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7278
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8937
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9158
BiodegradationNot ready biodegradable0.9491
Rat acute toxicity2.4391 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9978
hERG inhibition (predictor II)Non-inhibitor0.7982
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for suspensionintravenous100 mg/20mL
Powder for suspensionintravenous100 mg
Injectionintravenous100 mg/16.7mL
Injectionintravenous30 mg/5mL
Injectionintravenous300 mg/50mL
Injectionintravenous6 mg/mL
Injection, solutionintravenous6 mg/mL
Injection, solution, concentrateintravenous6 mg/mL
Solutionintravenous6 mg
Liquidintravenous6 mg
Prices
Unit descriptionCostUnit
Abraxane 100 mg vial1119.6USD vial
Taxol 30 mg/5 ml vial35.06USD ml
Onxol 30 mg/5 ml vial34.54USD ml
Onxol 300 mg/50 ml vial34.54USD ml
Paclitaxel 300 mg/50 ml vial5.31USD ml
Paclitaxel 100 mg/16.7 ml vial4.45USD ml
Paclitaxel 30 mg/5 ml vial3.54USD ml
Paclitaxel 150 mg/25 ml vial3.36USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2086874 No1998-09-012013-01-07Canada
CA2155947 No2007-08-212014-02-22Canada
US5439686 No1993-02-222013-02-22Us
US5498421 No1993-03-122013-03-12Us
US7758891 No2006-02-212026-02-21Us
US7820788 No2004-10-272024-10-27Us
US7923536 No2003-12-092023-12-09Us
US8034375 No2006-08-132026-08-13Us
US8138229 No2003-12-092023-12-09Us
US8268348 No2006-02-212026-02-21Us
US8314156 No2003-12-092023-12-09Us
US8853260 No2000-10-102020-10-10Us
US9101543 No2006-02-212026-02-21Us
USRE41884 No1996-08-142016-08-14Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point216-217 °CFDA label
water solubilityInsolubleFDA label
logP3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00556 mg/mLALOGPS
logP3.2ALOGPS
logP3.54ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)10.36ChemAxon
pKa (Strongest Basic)-1ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area221.29 Å2ChemAxon
Rotatable Bond Count14ChemAxon
Refractivity218.29 m3·mol-1ChemAxon
Polarizability87.17 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Hendricus B. A. de Bont, Ruben G. G. Leenders, Johan W. Scheeren, Hidde J. Haisma, Dick de Vos, “Paclitaxel prodrugs, method for preparation as well as their use in selective chemotherapy.” U.S. Patent US5760072, issued September, 1989.

US5760072
General References
  1. Wall ME, Wani MC: Camptothecin and taxol: discovery to clinic--thirteenth Bruce F. Cain Memorial Award Lecture. Cancer Res. 1995 Feb 15;55(4):753-60. [PubMed:7850785 ]
  2. Wani MC, Taylor HL, Wall ME, Coggon P, McPhail AT: Plant antitumor agents. VI. The isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia. J Am Chem Soc. 1971 May 5;93(9):2325-7. [PubMed:5553076 ]
  3. Fuchs DA, Johnson RK: Cytologic evidence that taxol, an antineoplastic agent from Taxus brevifolia, acts as a mitotic spindle poison. Cancer Treat Rep. 1978 Aug;62(8):1219-22. [PubMed:688258 ]
  4. Saville MW, Lietzau J, Pluda JM, Feuerstein I, Odom J, Wilson WH, Humphrey RW, Feigal E, Steinberg SM, Broder S, et al.: Treatment of HIV-associated Kaposi's sarcoma with paclitaxel. Lancet. 1995 Jul 1;346(8966):26-8. [PubMed:7603142 ]
  5. Authors unspecified: ABI 007. Drugs R D. 2004;5(3):155-9. [PubMed:15139776 ]
  6. Gaitanis A, Staal S: Liposomal doxorubicin and nab-paclitaxel: nanoparticle cancer chemotherapy in current clinical use. Methods Mol Biol. 2010;624:385-92. doi: 10.1007/978-1-60761-609-2_26. [PubMed:20217610 ]
External Links
ATC CodesL01CD01
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (220 KB)
MSDSDownload (74 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Paclitaxel can be increased when it is combined with Abiraterone.
AprepitantThe serum concentration of Paclitaxel can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Paclitaxel.
AtazanavirThe serum concentration of Paclitaxel can be increased when it is combined with Atazanavir.
BexaroteneThe serum concentration of Bexarotene can be increased when it is combined with Paclitaxel.
BosentanThe serum concentration of Paclitaxel can be decreased when it is combined with Bosentan.
CarboplatinCarboplatin may increase the myelosuppressive activities of Paclitaxel.
CisplatinCisplatin may increase the myelosuppressive activities of Paclitaxel.
ClozapineThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Clozapine.
ConivaptanThe serum concentration of Paclitaxel can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Paclitaxel can be decreased when it is combined with Dabrafenib.
DasatinibThe serum concentration of Paclitaxel can be increased when it is combined with Dasatinib.
DaunorubicinThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Daunorubicin.
DeferasiroxThe serum concentration of Paclitaxel can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Paclitaxel.
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Paclitaxel.
EpirubicinThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Epirubicin.
FluconazoleThe metabolism of Paclitaxel can be decreased when combined with Fluconazole.
FosaprepitantThe serum concentration of Paclitaxel can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Paclitaxel can be increased when it is combined with Fusidic Acid.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Paclitaxel.
IdarubicinThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Idarubicin.
IdelalisibThe serum concentration of Paclitaxel can be increased when it is combined with Idelalisib.
IvacaftorThe serum concentration of Paclitaxel can be increased when it is combined with Ivacaftor.
LeflunomideThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Leflunomide.
LuliconazoleThe serum concentration of Paclitaxel can be increased when it is combined with Luliconazole.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Paclitaxel.
MifepristoneThe serum concentration of Paclitaxel can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Paclitaxel can be decreased when it is combined with Mitotane.
MitoxantroneThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Mitoxantrone.
NatalizumabThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Natalizumab.
NelfinavirThe metabolism of Paclitaxel can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Paclitaxel can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Paclitaxel.
OxaliplatinOxaliplatin may increase the myelosuppressive activities of Paclitaxel.
PalbociclibThe serum concentration of Paclitaxel can be increased when it is combined with Palbociclib.
PhenytoinThe metabolism of Paclitaxel can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Paclitaxel.
RanolazineThe serum concentration of Paclitaxel can be increased when it is combined with Ranolazine.
RitonavirThe metabolism of Paclitaxel can be decreased when combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Paclitaxel.
RosiglitazoneThe metabolism of Paclitaxel can be decreased when combined with Rosiglitazone.
SaquinavirThe serum concentration of Paclitaxel can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Paclitaxel.
SiltuximabThe serum concentration of Paclitaxel can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Paclitaxel can be increased when it is combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Paclitaxel.
SorafenibThe risk or severity of adverse effects can be increased when Sorafenib is combined with Paclitaxel.
St. John's WortThe serum concentration of Paclitaxel can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Paclitaxel can be increased when it is combined with Stiripentol.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Paclitaxel.
TesmilifeneThe serum concentration of Paclitaxel can be decreased when it is combined with Tesmilifene.
TocilizumabThe serum concentration of Paclitaxel can be decreased when it is combined with Tocilizumab.
TofacitinibPaclitaxel may increase the immunosuppressive activities of Tofacitinib.
TrastuzumabThe serum concentration of Paclitaxel can be decreased when it is combined with Trastuzumab.
TrimethoprimThe metabolism of Paclitaxel can be decreased when combined with Trimethoprim.
VerapamilThe serum concentration of Paclitaxel can be increased when it is combined with Verapamil.
VinorelbinePaclitaxel may increase the neurotoxic activities of Vinorelbine.
Food Interactions
  • Avoid echinacea.
  • Avoid grapefruit and grapefruit juice due to potential increase of paclitaxel.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ubiquitin protein ligase binding
Specific Function:
Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating f...
Gene Name:
BCL2
Uniprot ID:
P10415
Molecular Weight:
26265.66 Da
References
  1. Gan Y, Wientjes MG, Au JL: Expression of basic fibroblast growth factor correlates with resistance to paclitaxel in human patient tumors. Pharm Res. 2006 Jun;23(6):1324-31. Epub 2006 Jun 8. [PubMed:16741658 ]
  2. Thomadaki H, Talieri M, Scorilas A: Treatment of MCF-7 cells with taxol and etoposide induces distinct alterations in the expression of apoptosis-related genes BCL2, BCL2L12, BAX, CASPASE-9 and FAS. Biol Chem. 2006 Aug;387(8):1081-6. [PubMed:16895478 ]
  3. Yoshino T, Shiina H, Urakami S, Kikuno N, Yoneda T, Shigeno K, Igawa M: Bcl-2 expression as a predictive marker of hormone-refractory prostate cancer treated with taxane-based chemotherapy. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6116-24. [PubMed:17062688 ]
  4. Matsuyoshi S, Shimada K, Nakamura M, Ishida E, Konishi N: Bcl-2 phosphorylation has pathological significance in human breast cancer. Pathobiology. 2006;73(4):205-12. [PubMed:17119350 ]
  5. Zhang X, Wang Q, Ling MT, Wong YC, Leung SC, Wang X: Anti-apoptotic role of TWIST and its association with Akt pathway in mediating taxol resistance in nasopharyngeal carcinoma cells. Int J Cancer. 2007 May 1;120(9):1891-8. [PubMed:17230521 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Structural constituent of cytoskeleton
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
Gene Name:
TUBB1
Uniprot ID:
Q9H4B7
Molecular Weight:
50326.56 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. Cheung CH, Chen HH, Kuo CC, Chang CY, Coumar MS, Hsieh HP, Chang JY: Survivin counteracts the therapeutic effect of microtubule de-stabilizers by stabilizing tubulin polymers. Mol Cancer. 2009 Jul 3;8:43. doi: 10.1186/1476-4598-8-43. [PubMed:19575780 ]
  4. Horwitz SB: Mechanism of action of taxol. Trends Pharmacol Sci. 1992 Apr;13(4):134-6. [PubMed:1350385 ]
  5. Kovacs P, Csaba G, Pallinger E, Czaker R: Effects of taxol treatment on the microtubular system and mitochondria of Tetrahymena. Cell Biol Int. 2007 Jul;31(7):724-32. Epub 2007 Jan 14. [PubMed:17314054 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Harmsen S, Meijerman I, Beijnen JH, Schellens JH: Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor. Cancer Chemother Pharmacol. 2009 Jun;64(1):35-43. doi: 10.1007/s00280-008-0842-3. Epub 2008 Oct 7. [PubMed:18839173 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Structural molecule activity
Specific Function:
Non-neuronal microtubule-associated protein. Promotes microtubule assembly.
Gene Name:
MAP4
Uniprot ID:
P27816
Molecular Weight:
121003.805 Da
References
  1. McGrogan BT, Gilmartin B, Carney DN, McCann A: Taxanes, microtubules and chemoresistant breast cancer. Biochim Biophys Acta. 2008 Apr;1785(2):96-132. Epub 2007 Nov 12. [PubMed:18068131 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Structural molecule activity
Specific Function:
The exact function of MAP2 is unknown but MAPs may stabilize the microtubules against depolymerization. They also seem to have a stiffening effect on microtubules.
Gene Name:
MAP2
Uniprot ID:
P11137
Molecular Weight:
199524.51 Da
References
  1. McGrogan BT, Gilmartin B, Carney DN, McCann A: Taxanes, microtubules and chemoresistant breast cancer. Biochim Biophys Acta. 2008 Apr;1785(2):96-132. Epub 2007 Nov 12. [PubMed:18068131 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Structural constituent of cytoskeleton
Specific Function:
Promotes microtubule assembly and stability, and might be involved in the establishment and maintenance of neuronal polarity. The C-terminus binds axonal microtubules while the N-terminus binds neural plasma membrane components, suggesting that tau functions as a linker protein between both. Axonal polarity is predetermined by TAU/MAPT localization (in the neuronal cell) in the domain of the ce...
Gene Name:
MAPT
Uniprot ID:
P10636
Molecular Weight:
78927.025 Da
References
  1. McGrogan BT, Gilmartin B, Carney DN, McCann A: Taxanes, microtubules and chemoresistant breast cancer. Biochim Biophys Acta. 2008 Apr;1785(2):96-132. Epub 2007 Nov 12. [PubMed:18068131 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 ]
  2. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. [PubMed:23536207 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
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, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 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
substrateinhibitor
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. 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 ]
  2. Lecureur V, Sun D, Hargrove P, Schuetz EG, Kim RB, Lan LB, Schuetz JD: Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. Mol Pharmacol. 2000 Jan;57(1):24-35. [PubMed:10617675 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674 ]
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  3. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
  4. Jang SH, Wientjes MG, Au JL: Kinetics of P-glycoprotein-mediated efflux of paclitaxel. J Pharmacol Exp Ther. 2001 Sep;298(3):1236-42. [PubMed:11504826 ]
  5. Li D, Jang SH, Kim J, Wientjes MG, Au JL: Enhanced drug-induced apoptosis associated with P-glycoprotein overexpression is specific to antimicrotubule agents. Pharm Res. 2003 Jan;20(1):45-50. [PubMed:12608535 ]
  6. Troutman MD, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res. 2003 Aug;20(8):1210-24. [PubMed:12948019 ]
  7. Kim S, Kim SS, Bang YJ, Kim SJ, Lee BJ: In vitro activities of native and designed peptide antibiotics against drug sensitive and resistant tumor cell lines. Peptides. 2003 Jul;24(7):945-53. [PubMed:14499271 ]
  8. Walle UK, Walle T: Taxol transport by human intestinal epithelial Caco-2 cells. Drug Metab Dispos. 1998 Apr;26(4):343-6. [PubMed:9531522 ]
  9. Lecureur V, Sun D, Hargrove P, Schuetz EG, Kim RB, Lan LB, Schuetz JD: Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. Mol Pharmacol. 2000 Jan;57(1):24-35. [PubMed:10617675 ]
  10. 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 ]
  11. Kuo CC, Hsieh HP, Pan WY, Chen CP, Liou JP, Lee SJ, Chang YL, Chen LT, Chen CT, Chang JY: BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo. Cancer Res. 2004 Jul 1;64(13):4621-8. [PubMed:15231674 ]
  12. Li YC, Fung KP, Kwok TT, Lee CY, Suen YK, Kong SK: Mitochondria-targeting drug oligomycin blocked P-glycoprotein activity and triggered apoptosis in doxorubicin-resistant HepG2 cells. Chemotherapy. 2004 Jun;50(2):55-62. [PubMed:15211078 ]
  13. Kwak JO, Lee SH, Lee GS, Kim MS, Ahn YG, Lee JH, Kim SW, Kim KH, Lee MG: Selective inhibition of MDR1 (ABCB1) by HM30181 increases oral bioavailability and therapeutic efficacy of paclitaxel. Eur J Pharmacol. 2010 Feb 10;627(1-3):92-8. doi: 10.1016/j.ejphar.2009.11.008. Epub 2009 Nov 10. [PubMed:19903471 ]
  14. Woodahl EL, Crouthamel MH, Bui T, Shen DD, Ho RJ: MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. doi: 10.1007/s00280-008-0906-4. Epub 2009 Jan 4. [PubMed:19123050 ]
  15. Tiwari AK, Sodani K, Wang SR, Kuang YH, Ashby CR Jr, Chen X, Chen ZS: Nilotinib (AMN107, Tasigna) reverses multidrug resistance by inhibiting the activity of the ABCB1/Pgp and ABCG2/BCRP/MXR transporters. Biochem Pharmacol. 2009 Jul 15;78(2):153-61. doi: 10.1016/j.bcp.2009.04.002. Epub 2009 Apr 11. [PubMed:19427995 ]
  16. Noguchi K, Kawahara H, Kaji A, Katayama K, Mitsuhashi J, Sugimoto Y: Substrate-dependent bidirectional modulation of P-glycoprotein-mediated drug resistance by erlotinib. Cancer Sci. 2009 Sep;100(9):1701-7. doi: 10.1111/j.1349-7006.2009.01213.x. Epub 2009 May 12. [PubMed:19493273 ]
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. Heijn M, Hooijberg JH, Scheffer GL, Szabo G, Westerhoff HV, Lankelma J: Anthracyclines modulate multidrug resistance protein (MRP) mediated organic anion transport. Biochim Biophys Acta. 1997 May 22;1326(1):12-22. [PubMed:9188796 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
ATP-dependent transporter probably involved in cellular detoxification through lipophilic anion extrusion.
Gene Name:
ABCC10
Uniprot ID:
Q5T3U5
Molecular Weight:
161627.375 Da
References
  1. Chen ZS, Hopper-Borge E, Belinsky MG, Shchaveleva I, Kotova E, Kruh GD: Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). Mol Pharmacol. 2003 Feb;63(2):351-8. [PubMed:12527806 ]
  2. Zhou Y, Hopper-Borge E, Shen T, Huang XC, Shi Z, Kuang YH, Furukawa T, Akiyama S, Peng XX, Ashby CR Jr, Chen X, Kruh GD, Chen ZS: Cepharanthine is a potent reversal agent for MRP7(ABCC10)-mediated multidrug resistance. Biochem Pharmacol. 2009 Mar 15;77(6):993-1001. doi: 10.1016/j.bcp.2008.12.005. Epub 2008 Dec 25. [PubMed:19150344 ]
  3. Hopper-Borge E, Xu X, Shen T, Shi Z, Chen ZS, Kruh GD: Human multidrug resistance protein 7 (ABCC10) is a resistance factor for nucleoside analogues and epothilone B. Cancer Res. 2009 Jan 1;69(1):178-84. doi: 10.1158/0008-5472.CAN-08-1420. [PubMed:19118001 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Smith NF, Acharya MR, Desai N, Figg WD, Sparreboom A: Identification of OATP1B3 as a high-affinity hepatocellular transporter of paclitaxel. Cancer Biol Ther. 2005 Aug;4(8):815-8. [PubMed:16210916 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Fellner S, Bauer B, Miller DS, Schaffrik M, Fankhanel M, Spruss T, Bernhardt G, Graeff C, Farber L, Gschaidmeier H, Buschauer A, Fricker G: Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo. J Clin Invest. 2002 Nov;110(9):1309-18. [PubMed:12417570 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Fellner S, Bauer B, Miller DS, Schaffrik M, Fankhanel M, Spruss T, Bernhardt G, Graeff C, Farber L, Gschaidmeier H, Buschauer A, Fricker G: Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo. J Clin Invest. 2002 Nov;110(9):1309-18. [PubMed:12417570 ]
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Drug created on June 13, 2005 07:24 / Updated on May 04, 2016 02:29