Everolimus 500microgram tablets
Tablet
Oral
Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor.
Active ingredients:
Everolimus
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Official documents, adverse reaction reporting, and safety monitoring
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Official medicine documents
Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Everolimus
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
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Suspected adverse reactions reported for Everolimus
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
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WHO defined daily dose (DDD)
1.5 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
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Sirolimus 500microgram tablets
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Sirolimus 2mg tablets
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2mg
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Sirolimus 1mg/ml oral solution sugar free
Oral solution
1mg
Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Clinical guidelines and formulary information
British National Formulary
Everolimus
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(13)
Everolimus for preventing organ rejection in liver transplantation (TA348)
TA348
Technology appraisal
Updated Jul 2015Lenvatinib with everolimus for previously treated advanced renal cell carcinoma (TA498)
TA498
Technology appraisal
Updated Jan 2018Everolimus for advanced renal cell carcinoma after previous treatment (TA432)
TA432
Technology appraisal
Updated Feb 2017Everolimus with exemestane for treating advanced breast cancer after endocrine therapy (TA421)
TA421
Technology appraisal
Updated Dec 2016Everolimus and sunitinib for treating unresectable or metastatic neuroendocrine tumours in people with progressive disease (TA449)
TA449
Technology appraisal
Updated Jun 2017Nivolumab for previously treated advanced renal cell carcinoma (TA417)
TA417
Technology appraisal
Updated Nov 2016Ribociclib with fulvestrant for treating hormone receptor-positive, HER2-negative advanced breast cancer after endocrine therapy (TA687)
TA687
Technology appraisal
Updated Mar 2021Cabozantinib for previously treated advanced renal cell carcinoma (TA463)
TA463
Technology appraisal
Updated Aug 2017Lutetium (177Lu) oxodotreotide for treating unresectable or metastatic neuroendocrine tumours (TA539)
TA539
Technology appraisal
Updated Aug 2018Abemaciclib with fulvestrant for treating hormone receptor-positive, HER2-negative advanced breast cancer after endocrine therapy (TA725)
TA725
Technology appraisal
Updated Sept 2021Alpelisib with fulvestrant for treating hormone receptor-positive, HER2-negative, PIK3CA-mutated advanced breast cancer (TA816)
TA816
Technology appraisal
Updated Aug 2022Elacestrant for treating oestrogen receptor-positive HER2-negative advanced breast cancer with an ESR1 mutation after endocrine treatment (TA1036)
TA1036
Technology appraisal
Updated Feb 2025Capivasertib with fulvestrant for treating hormone receptor-positive HER2-negative advanced breast cancer after endocrine treatment (TA1063)
TA1063
Technology appraisal
Updated May 2025Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
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These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
30 hours
Mechanism
Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 bindin…
Food interactions
5 warnings
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
1 to 2 hours
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.…
Half-life
30 hours
~30 hours.
Protein binding
74%
~ 74% in both healthy patients and those with moderate hepatic impairment.
Volume of distribution
17%
The blood-to-plasma ratio of everolimus is 17% to 73%.
Metabolism
Everolimus is a substrate of CYP3A4 and PgP (phosphoglycolate phosphatase).…
Elimination
80%
After a single dose of radiolabeled everolimus was given to transplant patients receiving cyclosporine, the majority (80%) of radioactivity was…
Clearance
3 mg
Following a 3 mg radiolabeled dose of everolimus, 80% of the radioactivity was recovered from the feces, while 5% was excreted in the urine.
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
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.
Properties:
View FDA drug labelsolid
Avg. mass: 958.24 Da
DrugBank 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.
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.
Also known as(77)
40-O-(2-hydroxyethyl)-rapamycin
42-O-(2-Hydroxyethyl)rapamycin
Everolimus
évérolimus
2.7.11.1
FK506-binding protein 12-rapamycin complex-associated protein 1
FKBP12-rapamycin complex-associated protein
FRAP
Dosage forms(48)
Tablet (Oral)
Tablet (Oral) — 10 mg/1
Tablet (Oral) — 10.000 mg
Tablet (Oral) — 7.5 mg
Tablet (Oral) — 10 mg
Tablet, soluble (Oral) — 2 mg
Tablet, soluble (Oral) — 3 mg
Tablet, soluble (Oral) — 5 mg
Molecular properties(19)
Drug interactions(1391)
Known interactions with other medications. Always consult a healthcare professional.
The risk or severity of adverse effects can be increased when Denosumab is combined with Everolimus.
Peginterferon alfa-2a
Unknown severity
The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Everolimus.
Interferon alfa-n1
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Everolimus.
Interferon alfa-n3
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Everolimus.
Peginterferon alfa-2b
Unknown severity
The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Everolimus.
Interferon gamma-1b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Everolimus.
Interferon alfa-2a
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Everolimus.
Gemtuzumab ozogamicin
Unknown severity
The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Everolimus.
Pegaspargase
Unknown severity
The risk or severity of adverse effects can be increased when Pegaspargase is combined with Everolimus.
Interferon beta-1b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Everolimus.
Interferon alfacon-1
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Everolimus.
The risk or severity of adverse effects can be increased when Rituximab is combined with Everolimus.
Basiliximab
Unknown severity
The risk or severity of adverse effects can be increased when Basiliximab is combined with Everolimus.
The risk or severity of adverse effects can be increased when Muromonab is combined with Everolimus.
Ibritumomab tiuxetan
Unknown severity
The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Everolimus.
Tositumomab
Unknown severity
The risk or severity of adverse effects can be increased when Tositumomab is combined with Everolimus.
Alemtuzumab
Unknown severity
The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Everolimus.
The risk or severity of adverse effects can be increased when Alefacept is combined with Everolimus.
Efalizumab
Unknown severity
The risk or severity of adverse effects can be increased when Efalizumab is combined with Everolimus.
Antithymocyte immunoglobulin (rabbit)
Unknown severity
The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Everolimus.
Interferon alfa-2b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Everolimus.
Daclizumab
Unknown severity
The risk or severity of adverse effects can be increased when Daclizumab is combined with Everolimus.
Phenylalanine
Unknown severity
The risk or severity of adverse effects can be increased when Phenylalanine is combined with Everolimus.
Cladribine
Moderate
Everolimus may increase the immunosuppressive activities of Cladribine.
Carmustine
Unknown severity
The risk or severity of adverse effects can be increased when Carmustine is combined with Everolimus.
The risk or severity of adverse effects can be increased when Bleomycin is combined with Everolimus.
Chlorambucil
Unknown severity
The risk or severity of adverse effects can be increased when Chlorambucil is combined with Everolimus.
Raltitrexed
Unknown severity
The risk or severity of adverse effects can be increased when Raltitrexed is combined with Everolimus.
The risk or severity of adverse effects can be increased when Mitomycin is combined with Everolimus.
Floxuridine
Unknown severity
The risk or severity of adverse effects can be increased when Floxuridine is combined with Everolimus.
Tioguanine
Unknown severity
The risk or severity of adverse effects can be increased when Tioguanine is combined with Everolimus.
Dexrazoxane
Unknown severity
The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Everolimus.
Streptozocin
Unknown severity
The risk or severity of adverse effects can be increased when Streptozocin is combined with Everolimus.
Trifluridine
Unknown severity
The risk or severity of adverse effects can be increased when Trifluridine is combined with Everolimus.
Epirubicin
Unknown severity
The risk or severity of adverse effects can be increased when Epirubicin is combined with Everolimus.
Lenalidomide
Unknown severity
The risk or severity of adverse effects can be increased when Lenalidomide is combined with Everolimus.
Altretamine
Unknown severity
The risk or severity of adverse effects can be increased when Altretamine is combined with Everolimus.
The risk or severity of adverse effects can be increased when Cisplatin is combined with Everolimus.
Oxaliplatin
Unknown severity
The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Everolimus.
Fluorouracil
Unknown severity
The risk or severity of adverse effects can be increased when Fluorouracil is combined with Everolimus.
Propylthiouracil
Unknown severity
The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Everolimus.
Pentostatin
Unknown severity
The risk or severity of adverse effects can be increased when Pentostatin is combined with Everolimus.
The risk or severity of adverse effects can be increased when Linezolid is combined with Everolimus.
Clofarabine
Unknown severity
The risk or severity of adverse effects can be increased when Clofarabine is combined with Everolimus.
Pemetrexed
Unknown severity
The risk or severity of adverse effects can be increased when Pemetrexed is combined with Everolimus.
Sulfasalazine
Unknown severity
The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Everolimus.
Dacarbazine
Unknown severity
The risk or severity of adverse effects can be increased when Dacarbazine is combined with Everolimus.
Penicillamine
Unknown severity
The risk or severity of adverse effects can be increased when Penicillamine is combined with Everolimus.
Mechlorethamine
Unknown severity
The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Everolimus.
Azacitidine
Unknown severity
The risk or severity of adverse effects can be increased when Azacitidine is combined with Everolimus.
Showing 50 of 1391 interactions
Food & lifestyle interactions
Avoid Grapefruit
Avoid grapefruit products. Grapefruit inhibits the metabolism of everolimus through the CYP3A4 pathway and, therefore, may increase serum levels of everolimus.
Advice
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).
Advice
Take at the same time every day.
Advice
Take with a full glass of water.
Advice
Take with or without food. Take consistently with regard to food as food may reduce the AUC and Cmax of everolimus.
Toxicity & overdose
IC50 of 0.63 nM.
How it works
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.
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
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.
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.
Half-life
~30 hours.
Protein binding
~ 74% in both healthy patients and those with moderate hepatic impairment.
Volume of distribution
The blood-to-plasma ratio of everolimus is 17% to 73%.
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.
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.
Drug targets(1)
Proteins and enzymes this drug interacts with in the body
Serine/threonine-protein kinase mTOR
MTOR
inhibitor
Specific functionATP binding
Cellular location
Lysosome membrane
General function & pharmacology
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 .
PMID:12087098 PMID:12150925 PMID:12150926 PMID:12231510 PMID:12718876 PMID:14651849 PMID:15268862 PMID:15467718 PMID:15545625 PMID:15718470 PMID:18497260 PMID:18762023 PMID:18925875 PMID:20516213 PMID:20537536 PMID:21659604 PMID:23429703 PMID:23429704 PMID:25799227 PMID:26018084 PMID:29150432 PMID:29236692 PMID:31112131 PMID:31601708 PMID:32561715 PMID:34519269 PMID:37751742
MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins .
PMID:15268862 PMID:15467718 PMID:17517883 PMID:18372248 PMID:18497260 PMID:18925875 PMID:20516213 PMID:21576368 PMID:21659604 PMID:23429704 PMID:30171069 PMID:29236692 PMID:37751742
Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 and 2) .
PMID:15268862 PMID:15467718 PMID:18497260 PMID:18925875 PMID:20516213 PMID:21576368 PMID:21659604 PMID:23429704 PMID:29424687 PMID:29567957 PMID:35926713
In response to nutrients, growth factors or amino acids, mTORC1 is recruited to the lysosome membrane and promotes protein, lipid and nucleotide synthesis by phosphorylating key regulators of mRNA translation and ribosome synthesis .
PMID:12087098 PMID:12150925 PMID:12150926 PMID:12231510 PMID:12718876 PMID:14651849 PMID:15268862 PMID:15467718 PMID:15545625 PMID:15718470 PMID:18497260 PMID:18762023 PMID:18925875 PMID:20516213 PMID:20537536 PMID:21659604 PMID:23429703 PMID:23429704 PMID:25799227 PMID:26018084 PMID:29150432 PMID:29236692 PMID:31112131 PMID:34519269
This includes phosphorylation of EIF4EBP1 and release of its inhibition toward the elongation initiation factor 4E (eiF4E) .
PMID:24403073 PMID:29236692
Moreover, phosphorylates and activates RPS6KB1 and RPS6KB2 that promote protein synthesis by modulating the activity of their downstream targets including ribosomal protein S6, eukaryotic translation initiation factor EIF4B, and the inhibitor of translation initiation PDCD4 .
PMID:12087098 PMID:12150925 PMID:18925875 PMID:29150432 PMID:29236692
Stimulates the pyrimidine biosynthesis pathway, both by acute regulation through RPS6KB1-mediated phosphorylation of the biosynthetic enzyme CAD, and delayed regulation, through transcriptional enhancement of the pentose phosphate pathway which produces 5-phosphoribosyl-1-pyrophosphate (PRPP), an allosteric activator of CAD at a later step in synthesis, this function is dependent on the mTORC1 complex .
PMID:23429703 PMID:23429704
Regulates ribosome synthesis by activating RNA polymerase III-dependent transcription through phosphorylation and inhibition of MAF1 an RNA polymerase III-repressor .
PMID:20516213
Activates dormant ribosomes by mediating phosphorylation of SERBP1, leading to SERBP1 inactivation and reactivation of translation .
PMID:36691768
In parallel to protein synthesis, also regulates lipid synthesis through SREBF1/SREBP1 and LPIN1 .
PMID:23426360
To maintain energy homeostasis mTORC1 may also regulate mitochondrial biogenesis through regulation of PPARGC1A (By similarity). In the same time, mTORC1 inhibits catabolic pathways: negatively regulates autophagy through phosphorylation of ULK1 .
PMID:32561715
Under nutrient sufficiency, phosphorylates ULK1 at 'Ser-758', disrupting the interaction with AMPK and preventing activation of ULK1 .
PMID:32561715
Also prevents autophagy through phosphorylation of the autophagy inhibitor DAP .
PMID:20537536
Also prevents autophagy by phosphorylating RUBCNL/Pacer under nutrient-rich conditions .
PMID:30704899
Prevents autophagy by mediating phosphorylation of AMBRA1, thereby inhibiting AMBRA1 ability to mediate ubiquitination of ULK1 and interaction between AMBRA1 and PPP2CA .
PMID:23524951 PMID:25438055
mTORC1 exerts a feedback control on upstream growth factor signaling that includes phosphorylation and activation of GRB10 a INSR-dependent signaling suppressor .
PMID:21659604
Among other potential targets mTORC1 may phosphorylate CLIP1 and regulate microtubules .
PMID:12231510
The mTORC1 complex is inhibited in response to starvation and amino acid depletion .
PMID:12150925 PMID:12150926 PMID:24403073 PMID:31695197
The non-canonical mTORC1 complex, which acts independently of RHEB, specifically mediates phosphorylation of MiT/TFE factors MITF, TFEB and TFE3 in the presence of nutrients, promoting their cytosolic retention and inactivation .
PMID:22343943 PMID:22576015 PMID:22692423 PMID:24448649 PMID:32612235 PMID:36608670 PMID:36697823
Upon starvation or lysosomal stress, inhibition of mTORC1 induces dephosphorylation and nuclear translocation of TFEB and TFE3, promoting their transcription factor activity .
PMID:22343943 PMID:22576015 PMID:22692423 PMID:24448649 PMID:32612235 PMID:36608670
The mTORC1 complex regulates pyroptosis in macrophages by promoting GSDMD oligomerization .
PMID:34289345
MTOR phosphorylates RPTOR which in turn inhibits mTORC1 (By similarity). As part of the mTORC2 complex, MTOR transduces signals from growth factors to pathways involved in proliferation, cytoskeletal organization, lipogenesis and anabolic output .
PMID:15268862 PMID:15467718 PMID:24670654 PMID:29424687 PMID:29567957 PMID:35926713
In response to growth factors, mTORC2 phosphorylates and activates AGC protein kinase family members, including AKT (AKT1, AKT2 and AKT3), PKC (PRKCA, PRKCB and PRKCE) and SGK1 .
PMID:15268862 PMID:15467718 PMID:21376236 PMID:24670654 PMID:29424687 PMID:29567957 PMID:35926713
In contrast to mTORC1, mTORC2 is nutrient-insensitive .
PMID:15467718
mTORC2 plays a critical role in AKT1 activation by mediating phosphorylation of different sites depending on the context, such as 'Thr-450', 'Ser-473', 'Ser-477' or 'Thr-479', facilitating the phosphorylation of the activation loop of AKT1 on 'Thr-308' by PDPK1/PDK1 which is a prerequisite for full activation .
PMID:15718470 PMID:21376236 PMID:24670654 PMID:29424687 PMID:29567957
mTORC2 also regulates the phosphorylation of SGK1 at 'Ser-422' .
PMID:18925875
mTORC2 may regulate the actin cytoskeleton, through phosphorylation of PRKCA, PXN and activation of the Rho-type guanine nucleotide exchange factors RHOA and RAC1A or RAC1B .
PMID:15268862
The mTORC2 complex also phosphorylates various proteins involved in insulin signaling, such as FBXW8 and IGF2BP1 (By similarity).
May also regulate insulin signaling by acting as a tyrosine protein kinase that catalyzes phosphorylation of IGF1R and INSR; additional evidence are however required to confirm this result in vivo .
PMID:26584640
Regulates osteoclastogenesis by adjusting the expression of CEBPB isoforms (By similarity). Plays an important regulatory role in the circadian clock function; regulates period length and rhythm amplitude of the suprachiasmatic nucleus (SCN) and liver clocks (By similarity)
PMID:12087098 PMID:12150925 PMID:12150926 PMID:12231510 PMID:12718876 PMID:14651849 PMID:15268862 PMID:15467718 PMID:15545625 PMID:15718470 PMID:18497260 PMID:18762023 PMID:18925875 PMID:20516213 PMID:20537536 PMID:21659604 PMID:23429703 PMID:23429704 PMID:25799227 PMID:26018084 PMID:29150432 PMID:29236692 PMID:31112131 PMID:31601708 PMID:32561715 PMID:34519269 PMID:37751742
MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins .
PMID:15268862 PMID:15467718 PMID:17517883 PMID:18372248 PMID:18497260 PMID:18925875 PMID:20516213 PMID:21576368 PMID:21659604 PMID:23429704 PMID:30171069 PMID:29236692 PMID:37751742
Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 and 2) .
PMID:15268862 PMID:15467718 PMID:18497260 PMID:18925875 PMID:20516213 PMID:21576368 PMID:21659604 PMID:23429704 PMID:29424687 PMID:29567957 PMID:35926713
In response to nutrients, growth factors or amino acids, mTORC1 is recruited to the lysosome membrane and promotes protein, lipid and nucleotide synthesis by phosphorylating key regulators of mRNA translation and ribosome synthesis .
PMID:12087098 PMID:12150925 PMID:12150926 PMID:12231510 PMID:12718876 PMID:14651849 PMID:15268862 PMID:15467718 PMID:15545625 PMID:15718470 PMID:18497260 PMID:18762023 PMID:18925875 PMID:20516213 PMID:20537536 PMID:21659604 PMID:23429703 PMID:23429704 PMID:25799227 PMID:26018084 PMID:29150432 PMID:29236692 PMID:31112131 PMID:34519269
This includes phosphorylation of EIF4EBP1 and release of its inhibition toward the elongation initiation factor 4E (eiF4E) .
PMID:24403073 PMID:29236692
Moreover, phosphorylates and activates RPS6KB1 and RPS6KB2 that promote protein synthesis by modulating the activity of their downstream targets including ribosomal protein S6, eukaryotic translation initiation factor EIF4B, and the inhibitor of translation initiation PDCD4 .
PMID:12087098 PMID:12150925 PMID:18925875 PMID:29150432 PMID:29236692
Stimulates the pyrimidine biosynthesis pathway, both by acute regulation through RPS6KB1-mediated phosphorylation of the biosynthetic enzyme CAD, and delayed regulation, through transcriptional enhancement of the pentose phosphate pathway which produces 5-phosphoribosyl-1-pyrophosphate (PRPP), an allosteric activator of CAD at a later step in synthesis, this function is dependent on the mTORC1 complex .
PMID:23429703 PMID:23429704
Regulates ribosome synthesis by activating RNA polymerase III-dependent transcription through phosphorylation and inhibition of MAF1 an RNA polymerase III-repressor .
PMID:20516213
Activates dormant ribosomes by mediating phosphorylation of SERBP1, leading to SERBP1 inactivation and reactivation of translation .
PMID:36691768
In parallel to protein synthesis, also regulates lipid synthesis through SREBF1/SREBP1 and LPIN1 .
PMID:23426360
To maintain energy homeostasis mTORC1 may also regulate mitochondrial biogenesis through regulation of PPARGC1A (By similarity). In the same time, mTORC1 inhibits catabolic pathways: negatively regulates autophagy through phosphorylation of ULK1 .
PMID:32561715
Under nutrient sufficiency, phosphorylates ULK1 at 'Ser-758', disrupting the interaction with AMPK and preventing activation of ULK1 .
PMID:32561715
Also prevents autophagy through phosphorylation of the autophagy inhibitor DAP .
PMID:20537536
Also prevents autophagy by phosphorylating RUBCNL/Pacer under nutrient-rich conditions .
PMID:30704899
Prevents autophagy by mediating phosphorylation of AMBRA1, thereby inhibiting AMBRA1 ability to mediate ubiquitination of ULK1 and interaction between AMBRA1 and PPP2CA .
PMID:23524951 PMID:25438055
mTORC1 exerts a feedback control on upstream growth factor signaling that includes phosphorylation and activation of GRB10 a INSR-dependent signaling suppressor .
PMID:21659604
Among other potential targets mTORC1 may phosphorylate CLIP1 and regulate microtubules .
PMID:12231510
The mTORC1 complex is inhibited in response to starvation and amino acid depletion .
PMID:12150925 PMID:12150926 PMID:24403073 PMID:31695197
The non-canonical mTORC1 complex, which acts independently of RHEB, specifically mediates phosphorylation of MiT/TFE factors MITF, TFEB and TFE3 in the presence of nutrients, promoting their cytosolic retention and inactivation .
PMID:22343943 PMID:22576015 PMID:22692423 PMID:24448649 PMID:32612235 PMID:36608670 PMID:36697823
Upon starvation or lysosomal stress, inhibition of mTORC1 induces dephosphorylation and nuclear translocation of TFEB and TFE3, promoting their transcription factor activity .
PMID:22343943 PMID:22576015 PMID:22692423 PMID:24448649 PMID:32612235 PMID:36608670
The mTORC1 complex regulates pyroptosis in macrophages by promoting GSDMD oligomerization .
PMID:34289345
MTOR phosphorylates RPTOR which in turn inhibits mTORC1 (By similarity). As part of the mTORC2 complex, MTOR transduces signals from growth factors to pathways involved in proliferation, cytoskeletal organization, lipogenesis and anabolic output .
PMID:15268862 PMID:15467718 PMID:24670654 PMID:29424687 PMID:29567957 PMID:35926713
In response to growth factors, mTORC2 phosphorylates and activates AGC protein kinase family members, including AKT (AKT1, AKT2 and AKT3), PKC (PRKCA, PRKCB and PRKCE) and SGK1 .
PMID:15268862 PMID:15467718 PMID:21376236 PMID:24670654 PMID:29424687 PMID:29567957 PMID:35926713
In contrast to mTORC1, mTORC2 is nutrient-insensitive .
PMID:15467718
mTORC2 plays a critical role in AKT1 activation by mediating phosphorylation of different sites depending on the context, such as 'Thr-450', 'Ser-473', 'Ser-477' or 'Thr-479', facilitating the phosphorylation of the activation loop of AKT1 on 'Thr-308' by PDPK1/PDK1 which is a prerequisite for full activation .
PMID:15718470 PMID:21376236 PMID:24670654 PMID:29424687 PMID:29567957
mTORC2 also regulates the phosphorylation of SGK1 at 'Ser-422' .
PMID:18925875
mTORC2 may regulate the actin cytoskeleton, through phosphorylation of PRKCA, PXN and activation of the Rho-type guanine nucleotide exchange factors RHOA and RAC1A or RAC1B .
PMID:15268862
The mTORC2 complex also phosphorylates various proteins involved in insulin signaling, such as FBXW8 and IGF2BP1 (By similarity).
May also regulate insulin signaling by acting as a tyrosine protein kinase that catalyzes phosphorylation of IGF1R and INSR; additional evidence are however required to confirm this result in vivo .
PMID:26584640
Regulates osteoclastogenesis by adjusting the expression of CEBPB isoforms (By similarity). Plays an important regulatory role in the circadian clock function; regulates period length and rhythm amplitude of the suprachiasmatic nucleus (SCN) and liver clocks (By similarity)
Metabolizing enzymes(2)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP2D6Cytochrome P450 2D6
inhibitor
CYP3A4Cytochrome P450 3A4
substrate
Transporters(4)
Proteins that transport this drug across cell membranes
Solute carrier organic anion transporter family member 1B1
SLCO1B1
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the Na(+)-independent uptake of organic anions .
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
Solute carrier organic anion transporter family member 1B3
SLCO1B3
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the Na(+)-independent uptake of organic anions .
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
Solute carrier organic anion transporter family member 1A2
SLCO1A2
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane .
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
ATP-dependent translocase ABCB1
ABCB1
substrate
inhibitor
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Scientific references(4)
Kuhn B., Jacobsen W., Christians U., Benet L.Z., Kollman P.A.
Metabolism of Sirolimus and Its Derivative Everolimus by Cytochrome P450 3A4: Insights from Docking, Molecular Dynamics, and Quantum Chemical Calculations.
Journal of Medicinal Chemistry
200144(12):2027-2034. doi: 10.1021/jm010079y
Krueger D.A., Care M.M., Holland K., Agricola K., Tudor C., Mangeshkar P., Wilson K.A., Byars A., Sahmoud T., Franz D.N.
Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis.
New England Journal of Medicine
2010 Nov 4363(19):1801-11. doi: 10.1056/NEJMoa1001671
den Burger J.C., Wilhelm A.J., Chahbouni A., Vos R.M., Sinjewel A., Swart E.L.
Analysis of cyclosporin A, tacrolimus, sirolimus, and everolimus in dried blood spot samples using liquid chromatography tandem mass spectrometry.
Anal Bioanal Chemistry
2012 Oct404(6-7):1803-11. doi: 10.1007/s00216-012-6317-8. Epub 2012 Aug 17
Pawaskar D.K., Straubinger R.M., Fetterly G.J., Hylander B.H., Repasky E.A., Ma W.W., Jusko W.J.
Synergistic interactions between sorafenib and everolimus in pancreatic cancer xenografts in mice.
Cancer Chemother Pharmacology
2013 May71(5):1231-40. doi: 10.1007/s00280-013-2117-x. Epub 2013 Mar 3
ATC classification(2 codes)
ATC L01EG02
ATC L04AH02
Affected organisms(1)
Humans and other mammals
Commercial products(135)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Everolimus
Additional database identifiers
Drugs Product Database (DPD)
13238
ChemSpider
21106307
BindingDB
50088378
ZINC
ZINC000169677008
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3942
GenAtlas
FRAP1
GeneCards
MTOR
GenBank Gene Database
L34075
Guide to Pharmacology
2109
UniProt Accession
MTOR_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2625
GenAtlas
CYP2D6
GeneCards
CYP2D6
GenBank Gene Database
M20403
GenBank Protein Database
181350
Guide to Pharmacology
1329
UniProt Accession
CP2D6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10959
GenAtlas
SLCO1B1
GeneCards
SLCO1B1
GenBank Gene Database
AF060500
GenBank Protein Database
5051630
Guide to Pharmacology
1220
UniProt Accession
SO1B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10961
GeneCards
SLCO1B3
GenBank Gene Database
AJ251506
GenBank Protein Database
9187497
Guide to Pharmacology
1221
UniProt Accession
SO1B3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10956
GeneCards
SLCO1A2
GenBank Gene Database
U21943
GenBank Protein Database
885978
Guide to Pharmacology
1219
UniProt Accession
SO1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
International reference pricing
4 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $6.98/tablet
To $247.58/tablet
Vesicare 10 mg tablet
$6.98/tablet
Vesicare 5 mg tablet
$6.98/tablet
Afinitor 5 mg tablet
$234.75/tablet
Afinitor 10 mg tablet
$247.58/tablet
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
2 active patents, 12 expired
9006224
United States
Approved 14 Apr 2015 · Expires 1 Jul 2028
2y 3m
Approved 2 Apr 2013 · Expires 1 May 2026
28 days
Approved 31 Dec 2013 · Expires 27 Mar 2023
Expired
Approved 7 May 2013 · Expires 22 Aug 2022
Expired
Approved 15 Jul 2014 · Expires 18 Aug 2022
Expired
The earliest active patent expires May 2026. Generic versions may become available after this date.
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)