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Identification
NameEverolimus
Accession NumberDB01590
TypeSmall Molecule
GroupsApproved
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.

Structure
Thumb
Synonyms
Afinitor
Certican
RAD001
SDZ-RAD
VOTUBIA
Zortress
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Afinitortablet7.5 mg/1oralNovartis Pharmaceuticals Corporation2011-07-292016-04-23Us
Afinitortablet2.5 mg/1oralNovartis Pharmaceuticals Corporation2010-07-092016-04-23Us
Afinitortablet2.5 mgoralNovartis Pharmaceuticals Canada Inc2011-08-05Not applicableCanada
Afinitortablet10 mg/1oralNovartis Pharmaceuticals Corporation2009-03-312016-04-23Us
Afinitortablet10 mgoralNovartis Pharmaceuticals Canada Inc2010-01-19Not applicableCanada
Afinitortablet5 mg/1oralNovartis Pharmaceuticals Corporation2009-03-312016-04-23Us
Afinitortablet5 mgoralNovartis Pharmaceuticals Canada Inc2010-03-15Not applicableCanada
Afinitortablet7.5 mgoralNovartis Pharmaceuticals Canada Inc2016-04-05Not applicableCanada
Afinitor Disperztablet, for suspension3 mg/1oralNovartis Pharmaceuticals Corporation2012-08-292016-04-23Us
Afinitor Disperztablet for suspension5 mgoralNovartis Pharmaceuticals Canada Inc2014-11-28Not applicableCanada
Afinitor Disperztablet, for suspension2 mg/1oralNovartis Pharmaceuticals Corporation2012-08-292016-04-23Us
Afinitor Disperztablet for suspension3 mgoralNovartis Pharmaceuticals Canada Inc2014-11-28Not applicableCanada
Afinitor Disperztablet for suspension2 mgoralNovartis Pharmaceuticals Canada Inc2014-11-28Not applicableCanada
Afinitor Disperztablet, for suspension5 mg/1oralNovartis Pharmaceuticals Corporation2012-08-292016-04-23Us
Certicantablet0.50 mgoralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
Certicantablet0.25 mgoralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
Certicantablet0.75 mgoralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
Zortresstablet.5 mg/1oralNovartis Pharmaceuticals Corporation2010-04-222016-04-23Us
Zortresstablet.25 mg/1oralNovartis Pharmaceuticals Corporation2010-04-222016-04-23Us
Zortresstablet.75 mg/1oralNovartis Pharmaceuticals Corporation2010-04-222016-04-23Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
VOTUBIANovartis
Brand mixturesNot Available
SaltsNot Available
Categories
UNII9HW64Q8G6G
CAS number159351-69-6
WeightAverage: 958.2244
Monoisotopic: 957.581356369
Chemical FormulaC53H83NO14
InChI KeyInChIKey=HKVAMNSJSFKALM-CYUZEOOHSA-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-/m0/s1
IUPAC Name
(1S,9R,15R,16E,18R,19R,21S,23R,24E,26E,28E,30S,32R,35S)-1,18-dihydroxy-12-[(2S)-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
CO[C@@H]1C[[email protected]](C[[email protected]](C)C2CC(=O)[[email protected]](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@@H](C)C[C@@H](C)\C=C\C=C\C=C(C)\[[email protected]](C[[email protected]]3CC[[email protected]](C)[C@](O)(O3)C(=O)C(=O)N3CCCC[C@@H]3C(=O)O2)OC)CC[[email protected]]1OCCO
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassMacrolide lactams
Sub ClassNot Available
Direct ParentMacrolide lactams
Alternative Parents
Substituents
  • Macrolide lactam
  • Macrolide
  • Alpha-amino acid ester
  • Piperidine
  • Oxane
  • Tertiary carboxylic acid amide
  • Cyclic ketone
  • Tertiary amine
  • Secondary alcohol
  • Lactone
  • Lactam
  • Ketone
  • Hemiacetal
  • Carboxylic acid ester
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationEverolimus 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.
PharmacodynamicsNot Available
Mechanism of actionEverolimus 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.
Related Articles
AbsorptionIn 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 eliminationAfter 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.

ToxicityIC50 of 0.63 nM.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg/1
Tabletoral10 mg
Tabletoral2.5 mg/1
Tabletoral2.5 mg
Tabletoral5 mg/1
Tabletoral5 mg
Tabletoral7.5 mg/1
Tabletoral7.5 mg
Tablet for suspensionoral2 mg
Tablet for suspensionoral3 mg
Tablet for suspensionoral5 mg
Tablet, for suspensionoral2 mg/1
Tablet, for suspensionoral3 mg/1
Tablet, for suspensionoral5 mg/1
Tabletoral0.25 mg
Tabletoral0.50 mg
Tabletoral0.75 mg
Tabletoral.25 mg/1
Tabletoral.5 mg/1
Tabletoral.75 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)
CA2145383 No2004-11-162013-09-24Canada
CA2225960 No2004-05-112016-07-12Canada
US5665772 Yes2000-03-092020-03-09Us
US6004973 Yes1997-01-122017-01-12Us
US6239124 Yes1998-02-112018-02-11Us
US6440990 No1993-09-242013-09-24Us
US6455518 Yes1998-01-292018-01-29Us
US7297703 Yes2000-06-062020-06-06Us
US7741338 No1999-12-062019-12-06Us
US8410131 Yes2006-05-012026-05-01Us
US8436010 Yes2002-08-222022-08-22Us
US8617598 Yes2003-03-272023-03-27Us
US8778962 Yes2002-08-182022-08-18Us
US9006224 No2008-07-012028-07-01Us
Properties
StateSolid
Experimental PropertiesNot 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
Polarizability105.73 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (87.7 KB)
SpectraNot Available
References
Synthesis Reference
  1. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/001038/WC500022817.pdf
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 ]
External Links
ATC CodesL01XE10L04AA18
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (548 KB)
MSDSDownload (220 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Everolimus can be increased when it is combined with Abiraterone.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Everolimus.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Everolimus.
AmiodaroneThe serum concentration of Everolimus can be increased when it is combined with Amiodarone.
AprepitantThe serum concentration of Everolimus can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Everolimus can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Everolimus can be increased when it is combined with Atorvastatin.
AzithromycinThe serum concentration of Everolimus can be increased when it is combined with Azithromycin.
BenazeprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Benazepril.
BexaroteneThe serum concentration of Everolimus can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Everolimus can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Everolimus can be decreased when it is combined with Bosentan.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Everolimus.
CaptoprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Captopril.
CarbamazepineThe serum concentration of Everolimus can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Everolimus can be increased when it is combined with Carvedilol.
CeritinibThe serum concentration of Everolimus can be increased when it is combined with Ceritinib.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Everolimus.
CilazaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Cilazapril.
ClarithromycinThe serum concentration of Everolimus can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Everolimus is combined with Clozapine.
CobicistatThe serum concentration of Everolimus can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Everolimus can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Everolimus can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Everolimus can be increased when it is combined with Cyclosporine.
DabrafenibThe serum concentration of Everolimus can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Everolimus can be increased when it is combined with Daclatasvir.
DarunavirThe serum concentration of Everolimus can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Everolimus can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Everolimus can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Everolimus can be increased when it is combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Everolimus.
DiltiazemThe serum concentration of Everolimus can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Everolimus can be increased when it is combined with Dipyridamole.
DronedaroneThe serum concentration of Everolimus can be increased when it is combined with Dronedarone.
EfavirenzThe serum concentration of Everolimus can be decreased when it is combined with Efavirenz.
EliglustatThe serum concentration of Everolimus can be increased when it is combined with Eliglustat.
EnalaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Enalapril.
EnalaprilatThe risk or severity of adverse effects can be increased when Everolimus is combined with Enalaprilat.
EnzalutamideThe serum concentration of Everolimus can be decreased when it is combined with Enzalutamide.
ErythromycinThe serum concentration of Everolimus can be increased when it is combined with Erythromycin.
FlibanserinThe serum concentration of Everolimus can be increased when it is combined with Flibanserin.
FluconazoleThe serum concentration of Everolimus can be increased when it is combined with Fluconazole.
FosamprenavirThe serum concentration of Everolimus can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Everolimus can be increased when it is combined with Fosaprepitant.
FosinoprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Fosinopril.
FosphenytoinThe serum concentration of Everolimus can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Everolimus can be increased when it is combined with Fusidic Acid.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Everolimus.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Everolimus.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Everolimus.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Everolimus.
IbrutinibThe serum concentration of Everolimus can be increased when it is combined with Ibrutinib.
IdelalisibThe serum concentration of Everolimus can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Everolimus can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Everolimus can be increased when it is combined with Indinavir.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Everolimus.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Everolimus.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Everolimus.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Everolimus.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Everolimus.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Everolimus.
IsavuconazoniumThe serum concentration of Everolimus can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Everolimus can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Everolimus can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Everolimus can be increased when it is combined with Ketoconazole.
LapatinibThe serum concentration of Everolimus can be increased when it is combined with Lapatinib.
LeflunomideThe risk or severity of adverse effects can be increased when Everolimus is combined with Leflunomide.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Everolimus.
LisinoprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Lisinopril.
LomitapideThe serum concentration of Everolimus can be increased when it is combined with Lomitapide.
LuliconazoleThe serum concentration of Everolimus can be increased when it is combined with Luliconazole.
MefloquineThe serum concentration of Everolimus can be increased when it is combined with Mefloquine.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Everolimus.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Everolimus.
MifepristoneThe serum concentration of Everolimus can be increased when it is combined with Mifepristone.
MirabegronThe serum concentration of Everolimus can be increased when it is combined with Mirabegron.
MitotaneThe serum concentration of Everolimus can be decreased when it is combined with Mitotane.
MoexiprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Moexipril.
NatalizumabThe risk or severity of adverse effects can be increased when Everolimus is combined with Natalizumab.
NefazodoneThe serum concentration of Everolimus can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Everolimus can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Everolimus can be increased when it is combined with Nicardipine.
NilotinibThe serum concentration of Everolimus can be increased when it is combined with Nilotinib.
PalbociclibThe serum concentration of Everolimus can be increased when it is combined with Palbociclib.
PerindoprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Perindopril.
PhenobarbitalThe serum concentration of Everolimus can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Everolimus can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Everolimus.
PosaconazoleThe serum concentration of Everolimus can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Everolimus can be decreased when it is combined with Primidone.
ProgesteroneThe serum concentration of Everolimus can be increased when it is combined with Progesterone.
PropranololThe serum concentration of Everolimus can be increased when it is combined with Propranolol.
QuinaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Quinapril.
QuinidineThe serum concentration of Everolimus can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Everolimus can be increased when it is combined with Quinine.
RamiprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Ramipril.
RanolazineThe serum concentration of Everolimus can be increased when it is combined with Ranolazine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Everolimus.
ReserpineThe serum concentration of Everolimus can be increased when it is combined with Reserpine.
RifabutinThe serum concentration of Everolimus can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Everolimus can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Everolimus can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Everolimus can be increased when it is combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Everolimus.
RolapitantThe serum concentration of Everolimus can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of Everolimus can be increased when it is combined with Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Everolimus.
SiltuximabThe serum concentration of Everolimus can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Everolimus can be increased when it is combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Everolimus.
St. John's WortThe serum concentration of Everolimus can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Everolimus can be increased when it is combined with Stiripentol.
SunitinibThe serum concentration of Everolimus can be increased when it is combined with Sunitinib.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Everolimus.
TamoxifenThe serum concentration of Everolimus can be increased when it is combined with Tamoxifen.
TelaprevirThe serum concentration of Everolimus can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Everolimus can be increased when it is combined with Telithromycin.
TesmilifeneThe serum concentration of Everolimus can be decreased when it is combined with Tesmilifene.
TocilizumabThe serum concentration of Everolimus can be decreased when it is combined with Tocilizumab.
TofacitinibEverolimus may increase the immunosuppressive activities of Tofacitinib.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Everolimus.
TrandolaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Trandolapril.
TrastuzumabTrastuzumab may increase the neutropenic activities of Everolimus.
VandetanibThe serum concentration of Everolimus can be increased when it is combined with Vandetanib.
VemurafenibThe serum concentration of Everolimus can be increased when it is combined with Vemurafenib.
VerapamilThe serum concentration of Everolimus can be increased when it is combined with Verapamil.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Everolimus.
VoriconazoleThe serum concentration of Everolimus can be increased when it is combined with Voriconazole.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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 or indirectly regulates the phosphorylation of at least 800 proteins. Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 and 2). Activ...
Gene Name:
MTOR
Uniprot ID:
P42345
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
Human
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 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 ]
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Drug created on August 29, 2007 09:37 / Updated on May 05, 2016 03:15