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Identification
NameEverolimus
Accession NumberDB01590
TypeSmall Molecule
GroupsApproved
DescriptionEverolimus 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
40-O-(2-hydroxyethyl)-rapamycin
External Identifiers
  • RAD 666
  • RAD-001
  • RAD-666
  • RAD001
  • SDZ RAD
  • SDZ-RAD
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AfinitorTablet10 mg/1OralNovartis Pharmaceuticals Corporation2009-03-31Not applicableUs
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet2.5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet10 mgOralNovartis Pharmaceuticals Canada Inc2010-01-19Not applicableCanada
AfinitorTablet2.5 mg/1OralNovartis Pharmaceuticals Corporation2010-07-09Not applicableUs
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet7.5 mgOralNovartis Pharmaceuticals Canada Inc2016-04-05Not applicableCanada
AfinitorTablet2.5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet2.5 mgOralNovartis Pharmaceuticals Canada Inc2011-08-05Not applicableCanada
AfinitorTablet7.5 mg/1OralNovartis Pharmaceuticals Corporation2011-07-29Not applicableUs
AfinitorTablet5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet5 mg/1OralNovartis Pharmaceuticals Corporation2009-03-31Not applicableUs
AfinitorTablet5 mgOralNovartis Pharmaceuticals Canada Inc2010-03-15Not applicableCanada
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
Afinitor DisperzTablet, for suspension3 mgOralNovartis Pharmaceuticals Canada Inc2014-11-28Not applicableCanada
Afinitor DisperzTablet, for suspension2 mg/1OralNovartis Pharmaceuticals Corporation2012-08-29Not applicableUs
Afinitor DisperzTablet, for suspension5 mgOralNovartis Pharmaceuticals Canada Inc2014-11-28Not applicableCanada
Afinitor DisperzTablet, for suspension3 mg/1OralNovartis Pharmaceuticals Corporation2012-08-29Not applicableUs
Afinitor DisperzTablet, for suspension5 mg/1OralNovartis Pharmaceuticals Corporation2012-08-29Not applicableUs
Afinitor DisperzTablet, for suspension2 mgOralNovartis Pharmaceuticals Canada Inc2014-11-28Not applicableCanada
CerticanTablet0.75 mgOralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
CerticanTablet0.25 mgOralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
CerticanTablet0.50 mgOralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
VotubiaTablet2.5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension2 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet10 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet2.5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension2 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet10 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension3 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet10 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet2.5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet5 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension3 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
VotubiaTablet, for suspension2 mgOralNovartis Europharm Ltd2011-09-02Not applicableEu
ZortressTablet.75 mg/1OralNovartis Pharmaceuticals Corporation2010-04-22Not applicableUs
ZortressTablet.25 mg/1OralNovartis Pharmaceuticals Corporation2010-04-22Not applicableUs
ZortressTablet.5 mg/1OralNovartis Pharmaceuticals Corporation2010-04-22Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
VotubiaNovartis
Brand mixturesNot Available
SaltsNot Available
Categories
UNII9HW64Q8G6G
CAS number159351-69-6
WeightAverage: 958.24
Monoisotopic: 957.581356357
Chemical FormulaC53H83NO14
InChI KeyHKVAMNSJSFKALM-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
[H][C@@]1(C[C@@H](C)[C@]2([H])CC(=O)[[email protected]](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[[email protected]](C)C[[email protected]](C)\C=C\C=C\C=C(C)\[[email protected]](C[C@]3([H])CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O2)OC)CC[C@@H](OCCO)[C@@H](C1)OC
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.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Serine/threonine-protein kinase mTORProteinyes
inhibitor
HumanP42345 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Everolimus.Approved, Investigational
AcetaminophenThe serum concentration of Everolimus can be increased when it is combined with Acetaminophen.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Everolimus.Withdrawn
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Everolimus.Approved
AfatinibThe serum concentration of Everolimus can be increased when it is combined with Afatinib.Approved
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Everolimus.Experimental
AlbendazoleThe serum concentration of Everolimus can be increased when it is combined with Albendazole.Approved, Vet Approved
AlectinibThe serum concentration of Everolimus can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Everolimus can be increased when it is combined with Alfentanil.Approved, Illicit
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Everolimus.Approved
ALT-110The risk or severity of adverse effects can be increased when Everolimus is combined with ALT-110.Investigational
AmantadineThe serum concentration of Everolimus can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Everolimus can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of Everolimus can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Everolimus can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Everolimus can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Everolimus can be increased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Everolimus can be increased when it is combined with Amsacrine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Everolimus.Investigational
AprepitantThe serum concentration of Everolimus can be increased when it is combined with Aprepitant.Approved, Investigational
AstemizoleThe serum concentration of Everolimus can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Everolimus can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Everolimus can be increased when it is combined with Atenolol.Approved
AtomoxetineThe serum concentration of Everolimus can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Everolimus can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Everolimus can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Everolimus can be increased when it is combined with Azithromycin.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Everolimus.Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Everolimus.Investigational
BenazeprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Benazepril.Approved, Investigational
BenzocaineThe serum concentration of Everolimus can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Everolimus can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Everolimus.Approved, Investigational
BexaroteneThe serum concentration of Everolimus can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Everolimus can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of Everolimus can be increased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Everolimus can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Everolimus can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Everolimus can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Everolimus can be increased when it is combined with Bromocriptine.Approved, Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Everolimus.Withdrawn
BuprenorphineThe serum concentration of Everolimus can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Everolimus can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Everolimus can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Everolimus can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Everolimus can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Everolimus can be increased when it is combined with Candesartan.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Everolimus is combined with Candoxatril.Experimental
CaptoprilThe serum concentration of Everolimus can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Everolimus can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Everolimus can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Everolimus can be increased when it is combined with Caspofungin.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Everolimus.Experimental
CDX-110The risk or severity of adverse effects can be increased when Everolimus is combined with CDX-110.Investigational
CeritinibThe serum concentration of Everolimus can be increased when it is combined with Ceritinib.Approved
ChloroquineThe serum concentration of Everolimus can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Everolimus can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Everolimus can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Everolimus can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Everolimus can be increased when it is combined with Cholesterol.Experimental
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Everolimus.Experimental
CilazaprilThe serum concentration of Everolimus can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Everolimus can be increased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Everolimus can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Everolimus can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Everolimus can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Everolimus can be increased when it is combined with Clemastine.Approved
ClofazimineThe serum concentration of Everolimus can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Everolimus can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe serum concentration of Everolimus can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Everolimus is combined with Clozapine.Approved
CobicistatThe serum concentration of Everolimus can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Everolimus can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Everolimus can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Everolimus can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe serum concentration of Everolimus can be increased when it is combined with Crizotinib.Approved
CyclophosphamideThe serum concentration of Everolimus can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Everolimus can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Everolimus can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Everolimus can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Everolimus can be increased when it is combined with Dactinomycin.Approved
DarunavirThe serum concentration of Everolimus can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Everolimus can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Everolimus can be increased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Everolimus can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Everolimus can be increased when it is combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Everolimus.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Everolimus.Investigational
DesipramineThe serum concentration of Everolimus can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Everolimus.Approved
DesloratadineThe serum concentration of Everolimus can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Everolimus can be increased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Everolimus can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Everolimus can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Everolimus.Approved
DigoxinThe serum concentration of Everolimus can be increased when it is combined with Digoxin.Approved
DihydroergotamineThe serum concentration of Everolimus can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Everolimus can be increased when it is combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Everolimus can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Everolimus.Approved, Investigational
DoxazosinThe serum concentration of Everolimus can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Everolimus can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Everolimus can be increased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe serum concentration of Everolimus can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Everolimus can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Everolimus can be increased when it is combined with Dronedarone.Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Everolimus.Approved
EfavirenzThe serum concentration of Everolimus can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Everolimus can be increased when it is combined with Elbasvir.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Everolimus.Approved
EnalaprilThe serum concentration of Everolimus can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Everolimus is combined with Enalaprilat.Approved
EnzalutamideThe serum concentration of Everolimus can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Everolimus can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Everolimus can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Everolimus can be increased when it is combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Everolimus can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Everolimus can be increased when it is combined with Estramustine.Approved
EtoposideThe serum concentration of Everolimus can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Everolimus can be increased when it is combined with Etravirine.Approved
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Everolimus.Approved, Investigational
FelodipineThe serum concentration of Everolimus can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Everolimus can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Everolimus can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Everolimus can be increased when it is combined with Fidaxomicin.Approved
FingolimodEverolimus may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe serum concentration of Everolimus can be increased when it is combined with Fluconazole.Approved
FluoxetineThe serum concentration of Everolimus can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Everolimus can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Everolimus can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Everolimus can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe serum concentration of Everolimus can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Everolimus can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Everolimus can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Fosinopril.Approved
FosphenytoinThe serum concentration of Everolimus can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Everolimus can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Everolimus is combined with G17DT.Investigational
GefitinibThe serum concentration of Everolimus can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Everolimus can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Everolimus is combined with GI-5005.Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Everolimus.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Everolimus.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Everolimus.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Everolimus.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Everolimus.Approved
GlyburideThe serum concentration of Everolimus can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Everolimus can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Everolimus can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Everolimus can be increased when it is combined with Grepafloxacin.Withdrawn
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Everolimus.Investigational
HaloperidolThe serum concentration of Everolimus can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Everolimus can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Everolimus can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Everolimus can be increased when it is combined with Imatinib.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Imidapril.Investigational
ImipramineThe serum concentration of Everolimus can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Everolimus can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Everolimus can be increased when it is combined with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Everolimus is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Everolimus is combined with INGN 225.Investigational
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Everolimus.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Everolimus.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Everolimus.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Everolimus.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Everolimus.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Everolimus.Approved
IsavuconazoniumThe serum concentration of Everolimus can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsradipineThe serum concentration of Everolimus can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Everolimus can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Everolimus can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Everolimus can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Everolimus can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Everolimus can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Everolimus can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Everolimus can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Everolimus is combined with Leflunomide.Approved, Investigational
LevofloxacinThe serum concentration of Everolimus can be increased when it is combined with Levofloxacin.Approved, Investigational
LidocaineThe serum concentration of Everolimus can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Everolimus.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Everolimus.Approved
LisinoprilThe serum concentration of Everolimus can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Everolimus can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Everolimus can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of Everolimus can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Everolimus can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Everolimus can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Everolimus can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Everolimus can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Everolimus can be decreased when it is combined with Lumacaftor.Approved
MaprotilineThe serum concentration of Everolimus can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Everolimus can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Everolimus can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Everolimus can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Everolimus can be increased when it is combined with Meprobamate.Approved, Illicit
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Everolimus.Withdrawn
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Everolimus.Approved
MethadoneThe serum concentration of Everolimus can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Everolimus can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Everolimus can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Everolimus can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Everolimus can be increased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Everolimus can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Everolimus.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Everolimus.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Everolimus.Approved, Investigational
MitomycinThe serum concentration of Everolimus can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Everolimus can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Everolimus can be increased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Everolimus can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Moexipril.Approved
MorphineThe serum concentration of Everolimus can be increased when it is combined with Morphine.Approved, Investigational
NafcillinThe serum concentration of Everolimus can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Everolimus can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Everolimus can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Everolimus is combined with Natalizumab.Approved, Investigational
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Everolimus.Approved, Investigational
NefazodoneThe serum concentration of Everolimus can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Everolimus can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Everolimus can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Everolimus can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Everolimus can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Everolimus can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Everolimus can be increased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Everolimus can be increased when it is combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Everolimus can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Everolimus can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Everolimus can be increased when it is combined with Nitrendipine.Approved
OlaparibThe serum concentration of Everolimus can be increased when it is combined with Olaparib.Approved
OmapatrilatThe risk or severity of adverse effects can be increased when Everolimus is combined with Omapatrilat.Investigational
OmeprazoleThe serum concentration of Everolimus can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Everolimus can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Everolimus.Approved
P-NitrophenolThe serum concentration of Everolimus can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Everolimus can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Everolimus can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Everolimus can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Everolimus can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Everolimus can be increased when it is combined with Paroxetine.Approved, Investigational
PentobarbitalThe serum concentration of Everolimus can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Everolimus can be increased when it is combined with Perindopril.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Everolimus.Approved, Withdrawn
PhenobarbitalThe serum concentration of Everolimus can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Everolimus can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Everolimus.Approved, Investigational
PimozideThe serum concentration of Everolimus can be increased when it is combined with Pimozide.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Everolimus.Approved, Investigational
PonatinibThe serum concentration of Everolimus can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Everolimus can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Everolimus.Approved, Investigational
PravastatinThe serum concentration of Everolimus can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Everolimus can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Everolimus can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of Everolimus can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Everolimus can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Everolimus can be increased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Everolimus can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Everolimus can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Everolimus can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Everolimus can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Everolimus can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Everolimus can be increased when it is combined with Quinacrine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Quinapril.Approved, Investigational
QuinidineThe serum concentration of Everolimus can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Everolimus can be increased when it is combined with Quinine.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Everolimus is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Everolimus.Approved
RamiprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Ramipril.Approved
RanitidineThe serum concentration of Everolimus can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Everolimus can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Everolimus can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Everolimus can be increased when it is combined with Regorafenib.Approved
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Everolimus.Approved, Investigational
RescinnamineThe risk or severity of adverse effects can be increased when Everolimus is combined with Rescinnamine.Approved
ReserpineThe serum concentration of Everolimus can be increased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of Everolimus can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Everolimus can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Everolimus can be decreased when it is combined with Rifapentine.Approved
RilpivirineThe serum concentration of Everolimus can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of Everolimus can be increased when it is combined with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Everolimus.Approved
RolapitantThe serum concentration of Everolimus can be increased when it is combined with Rolapitant.Approved
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Everolimus.Approved, Investigational
SaquinavirThe serum concentration of Everolimus can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Everolimus.Approved
ScopolamineThe serum concentration of Everolimus can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Everolimus can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Everolimus can be increased when it is combined with Sertraline.Approved
SildenafilThe serum concentration of Everolimus can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Everolimus can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Everolimus can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Everolimus can be increased when it is combined with Simvastatin.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Everolimus.Approved
SirolimusThe serum concentration of Everolimus can be increased when it is combined with Sirolimus.Approved, Investigational
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Everolimus.Approved, Investigational
SorafenibThe serum concentration of Everolimus can be increased when it is combined with Sorafenib.Approved, Investigational
SpiraprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Spirapril.Approved
SpironolactoneThe serum concentration of Everolimus can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Everolimus is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Everolimus can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Everolimus can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Everolimus can be increased when it is combined with Stiripentol.Approved
SulfinpyrazoneThe serum concentration of Everolimus can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe serum concentration of Everolimus can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Everolimus.Approved, Investigational
SumatriptanThe serum concentration of Everolimus can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Everolimus can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Everolimus can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Everolimus.Approved, Investigational
TacrolimusThe serum concentration of Everolimus can be increased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Everolimus can be increased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Everolimus can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of Everolimus can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Everolimus can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Everolimus can be increased when it is combined with Telmisartan.Approved, Investigational
TemocaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Temocapril.Experimental, Investigational
TemsirolimusThe serum concentration of Everolimus can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Everolimus can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Everolimus can be increased when it is combined with Terfenadine.Withdrawn
TestosteroneThe serum concentration of Everolimus can be increased when it is combined with Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Everolimus is combined with TG4010.Investigational
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Everolimus.Investigational
TicagrelorThe serum concentration of Everolimus can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe serum concentration of Everolimus can be increased when it is combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Everolimus can be decreased when it is combined with Tocilizumab.Approved
TofacitinibEverolimus may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Everolimus.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Everolimus.Approved
TolvaptanThe serum concentration of Everolimus can be increased when it is combined with Tolvaptan.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Everolimus is combined with Trandolapril.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Everolimus.Approved, Investigational
TrifluoperazineThe serum concentration of Everolimus can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Everolimus can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Everolimus can be increased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Everolimus can be increased when it is combined with Trimipramine.Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Everolimus.Withdrawn
TroleandomycinThe serum concentration of Everolimus can be increased when it is combined with Troleandomycin.Approved
VenlafaxineThe serum concentration of Everolimus can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Everolimus can be increased when it is combined with Verapamil.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Everolimus.Approved, Investigational
VinblastineThe serum concentration of Everolimus can be increased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Everolimus can be increased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Everolimus can be increased when it is combined with Vinorelbine.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Everolimus.Approved, Investigational
VoriconazoleThe serum concentration of Everolimus can be increased when it is combined with Voriconazole.Approved, Investigational
ZimelidineThe serum concentration of Everolimus can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe serum concentration of Everolimus can be increased when it is combined with Ziprasidone.Approved
Food InteractionsNot 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)
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
TabletOral2.5 mg/1
TabletOral5 mg
TabletOral5 mg/1
TabletOral7.5 mg/1
TabletOral7.5 mg
Tablet, for suspensionOral2 mg/1
Tablet, for suspensionOral2 mg
Tablet, for suspensionOral3 mg
Tablet, for suspensionOral3 mg/1
Tablet, for suspensionOral5 mg/1
Tablet, for suspensionOral5 mg
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
Polarizability106.61 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (87.7 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
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
  • Alpha-amino acid ester
  • Macrolide
  • Alpha-amino acid or derivatives
  • Piperidine
  • Oxane
  • Tertiary carboxylic acid amide
  • Carboxamide group
  • Carboxylic acid ester
  • Hemiacetal
  • Ketone
  • Lactam
  • Cyclic ketone
  • Secondary alcohol
  • Lactone
  • Carboxylic acid derivative
  • Dialkyl ether
  • Ether
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Organic nitrogen compound
  • Hydrocarbon derivative
  • Organic oxygen compound
  • Carbonyl group
  • Organic oxide
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors

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 December 08, 2016 03:55