Identification

Name
Everolimus
Accession Number
DB01590
Description

Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 958.24
Monoisotopic: 957.581356357
Chemical Formula
C53H83NO14
Synonyms
  • 40-O-(2-hydroxyethyl)-rapamycin
  • 42-O-(2-Hydroxyethyl)rapamycin
  • Everolimus
  • évérolimus
External IDs
  • RAD 666
  • RAD-001
  • RAD-666
  • RAD001
  • SDZ RAD
  • SDZ-RAD

Pharmacology

Indication

Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole. Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease. Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Indicated in pediatric and adult patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics
Not Available
Mechanism of action

Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake.

TargetActionsOrganism
ASerine/threonine-protein kinase mTOR
inhibitor
Humans
Absorption

In patients with advanced solid tumors, peak everolimus concentrations are reached 1 to 2 hours after administration of oral doses ranging from 5 mg to 70 mg. Following single doses, Cmax is dose-proportional between 5 mg and 10 mg. At doses of 20 mg and higher, the increase in Cmax is less than dose-proportional, however AUC shows dose-proportionality over the 5 mg to 70 mg dose range. Steady-state was achieved within 2 weeks following once-daily dosing. Dose Proportionality in Patients with SEGA (subependymal giant-cell astrocytomas) and TSC (tuberous sclerosis complex): In patients with SEGA and TSC, everolimus Cmin was approximately dose-proportional within the dose range from 1.35 mg/m2 to 14.4 mg/m2.

Volume of distribution

The blood-to-plasma ratio of everolimus is 17% to 73%.

Protein binding

~ 74% in both healthy patients and those with moderate hepatic impairment.

Metabolism

Everolimus is a substrate of CYP3A4 and PgP (phosphoglycolate phosphatase). Three monohydroxylated metabolites, two hydrolytic ring-opened products, and a phosphatidylcholine conjugate of everolimus were the 6 primary metabolites detected in human blood. In vitro, everolimus competitively inhibited the metabolism of CYP3A4 and was a mixed inhibitor of the CYP2D6 substrate dextromethorphan.

Route of elimination

After a single dose of radiolabeled everolimus was given to transplant patients receiving cyclosporine, the majority (80%) of radioactivity was recovered from the feces and only a minor amount (5%) was excreted in urine.

Half-life

~30 hours.

Clearance

Following a 3 mg radiolabeled dose of everolimus, 80% of the radioactivity was recovered from the feces, while 5% was excreted in the urine.

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

IC50 of 0.63 nM.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Everolimus can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Everolimus can be increased when combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Everolimus.
AcalabrutinibThe metabolism of Everolimus can be decreased when combined with Acalabrutinib.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Everolimus.
AcebutololThe metabolism of Acebutolol can be decreased when combined with Everolimus.
AcenocoumarolThe serum concentration of Everolimus can be increased when it is combined with Acenocoumarol.
AcetaminophenThe metabolism of Everolimus can be increased when combined with Acetaminophen.
AcetazolamideThe metabolism of Everolimus can be decreased when combined with Acetazolamide.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Everolimus.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid grapefruit products. Grapefruit inhibits the metabolism of everolimus through the CYP3A4 pathway and, therefore, may increase serum levels of everolimus.
  • Avoid St. John's Wort. Coadministration of St. John's Wort with everolimus may reduce serum levels of everolimus by inducing CYP3A4 and P-glycoprotein (PGP).
  • Take at the same time every day.
  • Take with a full glass of water.
  • Take with or without food. Take consistently with regard to food as food may reduce the AUC and Cmax of everolimus.

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEU flag
AfinitorTablet2.5 mgOralNovartis Europharm Limited2009-08-03Not applicableEU flag
AfinitorTablet2.5 mg/1OralNovartis Pharmaceuticals Corporation2010-07-09Not applicableUS flag
AfinitorTablet5 mgOralNovartis2010-03-15Not applicableCanada flag
AfinitorTablet5 mgOralNovartis Europharm Limited2009-08-03Not applicableEU flag
AfinitorTablet2.5 mgOralNovartis2011-08-05Not applicableCanada flag
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEU flag
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEU flag
AfinitorTablet10 mg/1OralNovartis Pharmaceuticals Corporation2009-03-31Not applicableUS flag
AfinitorTablet7.5 mgOralNovartis2016-04-052018-07-09Canada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EverolimusTablet.25 mg/1OralHikma Pharmaceuticals USA Inc.2020-03-10Not applicableUS flag
EverolimusTablet2.5 mg/1OralHikma Pharmaceuticals USA Inc.2020-06-08Not applicableUS flag
EverolimusTablet7.5 mg/1OralTeva Pharmaceuticals USA, Inc.2020-06-10Not applicableUS flag
EverolimusTablet2.5 mg/1OralPar Pharmaceutical, Inc.2019-12-10Not applicableUS flag
EverolimusTablet7.5 mg/1OralHikma Pharmaceuticals USA Inc.2020-06-08Not applicableUS flag
EverolimusTablet5 mg/1OralMylan Pharmaceuticals Inc.2020-09-10Not applicableUS flag
EverolimusTablet7.5 mg/1OralPar Pharmaceutical, Inc.2019-12-10Not applicableUS flag
EverolimusTablet.75 mg/1OralHikma Pharmaceuticals USA Inc.2020-03-10Not applicableUS flag
EverolimusTablet5 mg/1OralTeva Pharmaceuticals USA, Inc.2020-06-10Not applicableUS flag
EverolimusTablet5 mg/1OralHikma Pharmaceuticals USA Inc.2020-06-08Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
L01XE10 — EverolimusL04AA18 — Everolimus
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as macrolide lactams. These are cyclic polyketides containing both a cyclic amide and a cyclic ester group.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Macrolide lactams
Sub Class
Not Available
Direct Parent
Macrolide lactams
Alternative Parents
Alpha amino acid esters / Macrolides and analogues / Piperidines / Oxanes / Tertiary carboxylic acid amides / Secondary alcohols / Carboxylic acid esters / Cyclic ketones / Hemiacetals / Lactams
show 10 more
Substituents
Alcohol / Aliphatic heteropolycyclic compound / Alpha-amino acid ester / Alpha-amino acid or derivatives / Azacycle / Carbonyl group / Carboxamide group / Carboxylic acid derivative / Carboxylic acid ester / Cyclic ketone
show 23 more
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
cyclic ketone, secondary alcohol, ether, primary alcohol, lactam, macrocyclic lactone, cyclic acetal (CHEBI:68478)

Chemical Identifiers

UNII
9HW64Q8G6G
CAS number
159351-69-6
InChI Key
HKVAMNSJSFKALM-GKUWKFKPSA-N
InChI
InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1
IUPAC Name
(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0⁴,⁹]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
SMILES

References

Synthesis Reference

EMA Report

General References
  1. Kuhn B, Jacobsen W, Christians U, Benet LZ, Kollman PA: Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem. 2001 Jun 7;44(12):2027-34. [PubMed:11384247]
  2. Krueger DA, Care MM, Holland K, Agricola K, Tudor C, Mangeshkar P, Wilson KA, Byars A, Sahmoud T, Franz DN: Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis. N Engl J Med. 2010 Nov 4;363(19):1801-11. doi: 10.1056/NEJMoa1001671. [PubMed:21047224]
  3. den Burger JC, Wilhelm AJ, Chahbouni A, Vos RM, Sinjewel A, Swart EL: Analysis of cyclosporin A, tacrolimus, sirolimus, and everolimus in dried blood spot samples using liquid chromatography tandem mass spectrometry. Anal Bioanal Chem. 2012 Oct;404(6-7):1803-11. doi: 10.1007/s00216-012-6317-8. Epub 2012 Aug 17. [PubMed:22899246]
  4. Pawaskar DK, Straubinger RM, Fetterly GJ, Hylander BH, Repasky EA, Ma WW, Jusko WJ: Synergistic interactions between sorafenib and everolimus in pancreatic cancer xenografts in mice. Cancer Chemother Pharmacol. 2013 May;71(5):1231-40. doi: 10.1007/s00280-013-2117-x. Epub 2013 Mar 3. [PubMed:23455452]
KEGG Drug
D02714
PubChem Compound
6442177
PubChem Substance
46505248
ChemSpider
21106307
BindingDB
50088378
RxNav
141704
ChEBI
68478
ChEMBL
CHEMBL1908360
ZINC
ZINC000169677008
Therapeutic Targets Database
DAP001223
PharmGKB
PA164746311
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Everolimus
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (548 KB)
MSDS
Download (220 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingOtherGrowth and Development1
4Active Not RecruitingTreatmentHepatocellular Carcinoma1
4Active Not RecruitingTreatmentProgressive Neuroendocrine Tumors of pancreatic origin1
4Active Not RecruitingTreatmentTransplant, Kidney1
4CompletedBasic ScienceHuman Immunodeficiency Virus (HIV) Infections / Transplant, Kidney / Transplantation, Liver1
4CompletedDiagnosticCardiac Transplant1
4CompletedDiagnosticNeoplasms, Breast1
4CompletedOtherHER2/Neu-negative Carcinoma of Breast / Hormone Receptor Positive Malignant Neoplasm of Breast / Recurrent Breast Cancer1
4CompletedOtherRenal Failure1
4CompletedOtherTransplant, Kidney1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Chunghwa Chemical Synthesis and Biotech Co. Ltd.
  • Novartis AG
  • Quality Care
Dosage Forms
FormRouteStrength
Tablet0.5 mg
Tablet1 mg
TabletOral10 mg/1
TabletOral10 mg
TabletOral2.5 mg
TabletOral5 mg
TabletOral7.5 mg
Tablet10 mg
Tablet2.5 mg
Tablet
Tablet5 mg
Tablet, for suspensionOral2 mg/1
Tablet, for suspensionOral3 mg/1
Tablet, for suspensionOral5 mg/1
Tablet0.1 mg
Tablet250 mcg
Tablet500 mcg
Tablet750 mcg
TabletOral
TabletOral0.1 MG
Tablet, orally disintegratingOral0.1 mg
Tablet, orally disintegratingOral250 mcg
TabletOral0.25 mg
TabletOral1 mg
Tablet, for suspensionOral0.1 mg
Tablet, for suspensionOral0.25 mg
Tablet0.25 mg
Tablet0.75 mg
TabletOral0.75 mg
TabletOral0.5 mg
Tablet7.5 mg
TabletOral.25 mg/1
TabletOral.5 mg/1
TabletOral.75 mg/1
TabletOral2.5 mg/1
TabletOral5 mg/1
TabletOral7.5 mg/1
Tablet, for suspensionOral1 MG
Tablet, for suspensionOral2 mg
Tablet, for suspensionOral3 mg
Tablet, for suspensionOral5 mg
Tablet2 mg
Tablet3 mg
TabletOral0.25 mg/1
TabletOral0.5 mg/1
TabletOral0.75 mg/1
TabletOral1 mg/1
Prices
Unit descriptionCostUnit
Afinitor 10 mg tablet247.58USD tablet
Afinitor 5 mg tablet234.75USD tablet
Vesicare 10 mg tablet6.98USD tablet
Vesicare 5 mg tablet6.98USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6440990No2002-08-272013-09-24US flag
CA2145383No2004-11-162013-09-24Canada flag
CA2225960No2004-05-112016-07-12Canada flag
US8410131Yes2013-04-022026-05-01US flag
US8436010Yes2013-05-072022-08-22US flag
US5665772Yes1997-09-092020-03-09US flag
US6004973Yes1999-12-212017-01-12US flag
US6239124Yes2001-05-292018-02-11US flag
US6455518Yes2002-09-242018-01-29US flag
US8778962Yes2014-07-152022-08-18US flag
US9006224No2015-04-142028-07-01US flag
US7741338No2010-06-222019-12-06US flag
US7297703Yes2007-11-202020-06-06US flag
US8617598Yes2013-12-312023-03-27US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00163 mg/mLALOGPS
logP5.01ALOGPS
logP7.4ChemAxon
logS-5.8ALOGPS
pKa (Strongest Acidic)9.96ChemAxon
pKa (Strongest Basic)-2.7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count13ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area204.66 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity261.71 m3·mol-1ChemAxon
Polarizability106.61 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.8288
Blood Brain Barrier-0.9541
Caco-2 permeable-0.6604
P-glycoprotein substrateSubstrate0.8117
P-glycoprotein inhibitor IInhibitor0.7789
P-glycoprotein inhibitor IIInhibitor0.7294
Renal organic cation transporterNon-inhibitor0.796
CYP450 2C9 substrateNon-substrate0.8793
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9078
CYP450 2C9 inhibitorNon-inhibitor0.9106
CYP450 2D6 inhibitorNon-inhibitor0.9388
CYP450 2C19 inhibitorNon-inhibitor0.9346
CYP450 3A4 inhibitorNon-inhibitor0.8168
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9734
Ames testNon AMES toxic0.6227
CarcinogenicityNon-carcinogens0.9362
BiodegradationNot ready biodegradable0.9257
Rat acute toxicity2.7442 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9776
hERG inhibition (predictor II)Non-inhibitor0.712
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (87.7 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Tfiiic-class transcription factor binding
Specific Function
Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly...
Gene Name
MTOR
Uniprot ID
P42345
Uniprot Name
Serine/threonine-protein kinase mTOR
Molecular Weight
288889.05 Da
References
  1. Ettenger R, Hoyer PF, Grimm P, Webb N, Loirat C, Mahan JD, Mentser M, Niaudet P, Offner G, Vandamme-Lombaerts R, Hexham JM: Multicenter trial of everolimus in pediatric renal transplant recipients: results at three year. Pediatr Transplant. 2008 Jun;12(4):456-63. doi: 10.1111/j.1399-3046.2007.00832.x. [PubMed:18466433]
  2. Rostaing L, Kamar N: mTOR inhibitor/proliferation signal inhibitors: entering or leaving the field? J Nephrol. 2010 Mar-Apr;23(2):133-42. [PubMed:20155724]
  3. George S, Bukowski RM: Role of everolimus in the treatment of renal cell carcinoma. Ther Clin Risk Manag. 2009 Oct;5(5):699-706. Epub 2009 Sep 15. [PubMed:19774211]
  4. Teachey DT, Grupp SA, Brown VI: Mammalian target of rapamycin inhibitors and their potential role in therapy in leukaemia and other haematological malignancies. Br J Haematol. 2009 Jun;145(5):569-80. doi: 10.1111/j.1365-2141.2009.07657.x. Epub 2009 Mar 16. [PubMed:19344392]
  5. Albert S, Serova M, Dreyer C, Sablin MP, Faivre S, Raymond E: New inhibitors of the mammalian target of rapamycin signaling pathway for cancer. Expert Opin Investig Drugs. 2010 Aug;19(8):919-30. doi: 10.1517/13543784.2010.499121. [PubMed:20569080]
  6. Coppin C: Everolimus: the first approved product for patients with advanced renal cell cancer after sunitinib and/or sorafenib. Biologics. 2010 May 25;4:91-101. [PubMed:20531964]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Everolimus FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Picard N, Levoir L, Lamoureux F, Yee SW, Giacomini KM, Marquet P: Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters. Xenobiotica. 2011 Sep;41(9):752-7. doi: 10.3109/00498254.2011.573882. Epub 2011 Apr 27. [PubMed:21524191]
  2. Votubia, INN:EVEROLIMUS - European Medicines Agency - europa.eu [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. Picard N, Levoir L, Lamoureux F, Yee SW, Giacomini KM, Marquet P: Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters. Xenobiotica. 2011 Sep;41(9):752-7. doi: 10.3109/00498254.2011.573882. Epub 2011 Apr 27. [PubMed:21524191]
  2. Votubia, INN:EVEROLIMUS - European Medicines Agency - europa.eu [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Picard N, Levoir L, Lamoureux F, Yee SW, Giacomini KM, Marquet P: Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters. Xenobiotica. 2011 Sep;41(9):752-7. doi: 10.3109/00498254.2011.573882. Epub 2011 Apr 27. [PubMed:21524191]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on August 29, 2007 09:37 / Updated on October 27, 2020 11:13

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