Identification

Name
Everolimus
Accession Number
DB01590
Type
Small Molecule
Groups
Approved
Description

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

Structure
Thumb
Synonyms
  • 40-O-(2-hydroxyethyl)-rapamycin
External IDs
RAD 666 / RAD-001 / RAD-666 / RAD001 / SDZ RAD / SDZ-RAD
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AfinitorTablet2.5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet5 mgOralNovartis2010-03-15Not applicableCanada
AfinitorTablet5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet10 mg/1OralNovartis2009-03-31Not applicableUs
AfinitorTablet10 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet2.5 mgOralNovartis2011-08-05Not applicableCanada
AfinitorTablet5 mgOralNovartis Europharm Limited2009-08-03Not applicableEu
AfinitorTablet7.5 mg/1OralNovartis2011-07-29Not applicableUs
AfinitorTablet5 mg/1OralNovartis2009-03-31Not applicableUs
International/Other Brands
Votubia (Novartis)
Categories
UNII
9HW64Q8G6G
CAS number
159351-69-6
Weight
Average: 958.24
Monoisotopic: 957.581356357
Chemical Formula
C53H83NO14
InChI Key
HKVAMNSJSFKALM-GKUWKFKPSA-N
InChI
InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1
IUPAC Name
(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0⁴,⁹]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
SMILES
[H][C@@]1(C[C@@H](C)[C@]2([H])CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](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

Indication

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

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

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

TargetActionsOrganism
ASerine/threonine-protein kinase mTOR
inhibitor
Human
Absorption

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

Volume of distribution

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

Protein binding

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

Metabolism

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

Route of elimination

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

Half life

~30 hours.

Clearance

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

Toxicity

IC50 of 0.63 nM.

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

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe serum concentration of (R)-warfarin can be increased when it is combined with Everolimus.
(S)-WarfarinThe serum concentration of (S)-Warfarin can be increased when it is combined with Everolimus.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Everolimus is combined with 2-Methoxyethanol.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Everolimus.
3-isobutyl-1-methyl-7H-xanthineThe metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Everolimus.
4-hydroxycoumarinThe serum concentration of 4-hydroxycoumarin can be increased when it is combined with Everolimus.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Everolimus.
7-DeazaguanineThe metabolism of 7-Deazaguanine can be decreased when combined with Everolimus.
7,9-DimethylguanineThe metabolism of 7,9-Dimethylguanine can be decreased when combined with Everolimus.
8-azaguanineThe metabolism of 8-azaguanine can be decreased when combined with Everolimus.
Food Interactions
Not Available

References

Synthesis Reference

EMA Report

General References
  1. Kuhn B, Jacobsen W, Christians U, Benet LZ, Kollman PA: Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem. 2001 Jun 7;44(12):2027-34. [PubMed:11384247]
  2. Krueger DA, Care MM, Holland K, Agricola K, Tudor C, Mangeshkar P, Wilson KA, Byars A, Sahmoud T, Franz DN: Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis. N Engl J Med. 2010 Nov 4;363(19):1801-11. doi: 10.1056/NEJMoa1001671. [PubMed:21047224]
  3. den Burger JC, Wilhelm AJ, Chahbouni A, Vos RM, Sinjewel A, Swart EL: Analysis of cyclosporin A, tacrolimus, sirolimus, and everolimus in dried blood spot samples using liquid chromatography tandem mass spectrometry. Anal Bioanal Chem. 2012 Oct;404(6-7):1803-11. doi: 10.1007/s00216-012-6317-8. Epub 2012 Aug 17. [PubMed:22899246]
  4. Pawaskar DK, Straubinger RM, Fetterly GJ, Hylander BH, Repasky EA, Ma WW, Jusko WJ: Synergistic interactions between sorafenib and everolimus in pancreatic cancer xenografts in mice. Cancer Chemother Pharmacol. 2013 May;71(5):1231-40. doi: 10.1007/s00280-013-2117-x. Epub 2013 Mar 3. [PubMed:23455452]
External Links
KEGG Drug
D02714
PubChem Compound
6442177
PubChem Substance
46505248
ChemSpider
21106307
ChEBI
68478
ChEMBL
CHEMBL1908360
Therapeutic Targets Database
DAP001223
PharmGKB
PA164746311
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Everolimus
ATC Codes
L01XE10 — EverolimusL04AA18 — Everolimus
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (548 KB)
MSDS
Download (220 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingOtherMeningiomas / Neurofibromatosis Type 2 / Vestibular Schwannomas1
0RecruitingSupportive CareHead and Neck Carcinoma / Salivary gland dysfunction / Xerostomia1
0RecruitingTreatmentDelayed Graft Function1
1Active Not RecruitingOtherNasopharyngeal Carcinoma, Lymphomas, Any EBV+ Solid Tumour1
1Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
1Active Not RecruitingTreatmentAdvanced Cancers / Advanced Malignant Neoplasm / Metastatic Malignant Neoplasm / Recurrent Malignant Neoplasm / Refractory Malignant Neoplasm1
1Active Not RecruitingTreatmentAdvanced Cancers / Tumors, Solid1
1Active Not RecruitingTreatmentBreast Adenocarcinoma / Estrogen Receptor Negative / HER2/Neu Negative / Progesterone Receptor-negative / Stage IV Breast Cancer / Triple-Negative Breast Carcinoma1
1Active Not RecruitingTreatmentCancer, Advanced1
1Active Not RecruitingTreatmentCancer, Advanced / Tumors, Solid2
1Active Not RecruitingTreatmentCancer, Breast1
1Active Not RecruitingTreatmentChronic Lymphocytic Leukemia (CLL) - Refractory / Multiple Myeloma (MM) / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma1
1Active Not RecruitingTreatmentEsophageal Cancers1
1Active Not RecruitingTreatmentEsophageal Cancers / Neoplasms, Esophageal1
1Active Not RecruitingTreatmentFallopian Tube Cancer / Peritoneal Cavity Cancer / Recurrent Ovarian Epithelial Cancer1
1Active Not RecruitingTreatmentFumarate Hydratase (FH)-Deficient Tumors / Lung Cancer Non-Small Cell Cancer (NSCLC) / Mesothelioma / Renal Cell Adenocarcinoma / Succinate Dehydrogenase (SDH)-Deficient Gastrointestinal Stromal Tumors (GIST) / Succinate Dehydrogenase (SDH)-Deficient Non-gastrointestinal Stromal Tumors / Triple-Negative Breast Cancer (TNBC) / Tumors Harboring Amplifications in the cMyc Gene / Tumors Harboring Isocitrate Dehydrogenase-1 (IDH1) and IDH2 Mutations / Tumors, Solid1
1Active Not RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndrome1
1Active Not RecruitingTreatmentLeukemias1
1Active Not RecruitingTreatmentNeoplasms1
1Active Not RecruitingTreatmentNeoplasms / Neoplasms, Breast / Neoplasms, Kidney / Pancreatic Neuroendocine Neoplasms1
1Active Not RecruitingTreatmentNeuroendocrine Tumors2
1Active Not RecruitingTreatmentProstate Cancer2
1CompletedNot AvailableHepatic Insufficiency1
1CompletedNot AvailableTumors, Solid1
1CompletedTreatmentAdenoidcystic Carcinoma / Neuroendocrine Tumors / Solid Organ Malignancies1
1CompletedTreatmentAdvanced Cancer of the Esophagogastric Junction / Advanced Gastric Cancer1
1CompletedTreatmentAdvanced Gastric Cancer1
1CompletedTreatmentAdvanced Solid Tumors1
1CompletedTreatmentAdvanced Solid Tumors / Metastatic Breast Cancer (MBC) / Metastatic Renal Cell Carcinoma1
1CompletedTreatmentBladder Cancers / Renal Pelvis Cancer / Ureteral Cancer1
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentCancer, Breast2
1CompletedTreatmentCancers / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentCarcinoid Tumors / Neuroendocrine Tumors / Progressive Neuroendocrine Tumors of pancreatic origin2
1CompletedTreatmentCarcinoma, Colorectal / Colorectal Cancers / Colorectal Tumors / Neoplasms, Colorectal1
1CompletedTreatmentCentral nervous system neoplasms malignant NEC / Recurrent or Refractory Solid Tumors1
1CompletedTreatmentCholangiocarcinoma of the Gallbladder / Localized Gallbladder Cancer / Unresectable Gallbladder Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Indolent Non-Hodgkin's Lymphomas / Mantle Cell Lymphoma (MCL)1
1CompletedTreatmentEndometrial Cancers1
1CompletedTreatmentGastrin-Producing Neuroendocrine Tumor / Lung Carcinoid Tumor / Metastatic Digestive System Neuroendocrine Tumor G1 / Pancreatic Glucagonoma / Pancreatic Insulinoma / Pancreatic Polypeptide Tumor / Paraganglioma / Recurrent Digestive System Neuroendocrine Tumor G1 / Recurrent Merkel Cell Carcinoma / Recurrent Pancreatic Neuroendocrine Carcinoma / Regional Digestive System Neuroendocrine Tumor G1 / Somatostatin-Producing Neuroendocrine Tumor / Stage III Merkel Cell Carcinoma / Stage IV Merkel Cell Carcinoma / Thyroid Gland Medullary Carcinoma1
1CompletedTreatmentGastrinoma / Glucagonoma / Insulinoma / Metastatic Gastrointestinal Carcinoid Tumor / Metastatic Pheochromocytoma / Non-Small Cell Lung Cancer Recurrent / Pancreatic Polypeptide Tumor / Recurrent Gastrointestinal Carcinoid Tumor / Recurrent Islet Cell Carcinoma / Recurrent Melanoma / Recurrent Neuroendocrine Carcinoma of the Skin / Recurrent Pheochromocytoma / Renal Cell Cancer, Recurrent / Somatostatinoma / Stage III Neuroendocrine Carcinoma of the Skin / Stage IV Melanoma / Stage IV Non-Small Cell Lung Cancer / Stage IV Renal Cell Cancer / Thyroid Gland Medullary Carcinoma / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentGlioblastomas / Gliosarcoma1
1CompletedTreatmentHead & Neck Cancer1
1CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1CompletedTreatmentLocally Advanced Cervical Cancer1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)4
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Relapsed and/or Refractory Solid Tumors / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1CompletedTreatmentLung Cancers1
1CompletedTreatmentLung Cancers / Tumors, Solid1
1CompletedTreatmentLung Neuroendocrine Neoplasm1
1CompletedTreatmentMalignant Lymphomas1
1CompletedTreatmentMalignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm1
1CompletedTreatmentMalignant Lymphomas / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentMetastatic Breast Cancer (MBC)1
1CompletedTreatmentMetastatic Clear Cell Renal Cancer1
1CompletedTreatmentMetastatic Colorectal Cancers1
1CompletedTreatmentMetastatic Renal Cell Carcinoma1
1CompletedTreatmentMultiple Myeloma (MM)1
1CompletedTreatmentNeoplasm Metastases1
1CompletedTreatmentNeoplasms Metastasis / Neoplasms, Breast1
1CompletedTreatmentNeoplasms, Brain / Rhabdomyosarcomas / Soft Tissue Sarcoma (STS) / Tumors1
1CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)2
1CompletedTreatmentProstate Cancer1
1CompletedTreatmentProstate Cancer Patients With Detectable PSA Following Prostatectomy1
1CompletedTreatmentRecurrent Adenoid Cystic Carcinoma of the Oral Cavity / Recurrent Basal Cell Carcinoma of the Lip / Recurrent Colon Cancer / Recurrent Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity / Recurrent Inverted Papilloma of the Paranasal Sinus and Nasal Cavity / Recurrent Lymphoepithelioma of the Nasopharynx / Recurrent Lymphoepithelioma of the Oropharynx / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity / Recurrent Mucoepidermoid Carcinoma of the Oral Cavity / Recurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Stage IV Adenoid Cystic Carcinoma of the Oral Cavity / Stage IV Basal Cell Carcinoma of the Lip / Stage IV Lymphoepithelioma of the Nasopharynx / Stage IV Lymphoepithelioma of the Oropharynx / Stage IV Mucoepidermoid Carcinoma of the Oral Cavity / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Larynx / Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IV Squamous Cell Carcinoma of the Oropharynx / Stage IV Verrucous Carcinoma of the Larynx / Stage IV Verrucous Carcinoma of the Oral Cavity / Stage IVA Colon Cancer / Stage IVA Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity / Stage IVA Inverted Papilloma of the Paranasal Sinus and Nasal Cavity / Stage IVA Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity / Stage IVA Salivary Gland Cancer / Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVB Colon Cancer / Stage IVB Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity / Stage IVB Inverted Papilloma of the Paranasal Sinus and Nasal Cavity / Stage IVB Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity / Stage IVB Salivary Gland Cancer / Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVC Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity / Stage IVC Inverted Papilloma of the Paranasal Sinus and Nasal Cavity / Stage IVC Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity / Stage IVC Salivary Gland Cancer / Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Tongue Cancer1
1CompletedTreatmentRefractory Malignancy1
1CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
1CompletedTreatmentRenal Cancers / Tumors, Solid1
1CompletedTreatmentRenal Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentRenal Cell Adenocarcinoma2
1CompletedTreatmentSarcomas / Tumors, Solid1
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific3
1RecruitingTreatmentAdvanced Cancers1
1RecruitingTreatmentAnaplastic Astrocytoma (AA) / Bithalamic High Grade Glioma / Brain Stem Gliomas / Diffuse Intrinsic Pontine Glioma (DIPG) / Glioblastomas / High Grade Glioma (HGG) / Malignant Glioma of Brain1
1RecruitingTreatmentCancer of the Ovary / Cancer, Breast1
1RecruitingTreatmentCancer, Breast / Tumors, Solid1
1RecruitingTreatmentCentral Nervous System Embryonal Tumor, Not Otherwise Specified / Malignant Gliomas / Recurrent Atypical Teratoid/Rhabdoid Tumor / Recurrent Childhood Ependymoma / Recurrent Diffuse Intrinsic Pontine Glioma / Recurrent Medulloblastoma / Refractory Diffuse Intrinsic Pontine Glioma1
1RecruitingTreatmentColorectal Cancer, Non-small Cell Lung Carcinoma (Adenocarcinoma), Triple Negative Breast Cancer / Colorectal Cancer, Non-small Cell Lung Carcinoma (Adenocarcinoma), Triple Negative Breast Cancer, Renal Cell Carcinoma / Colorectal Cancers / Non-small Cell Lung Carcinoma (Adenocarcinoma) / Triple Negative Breast Cancer (TNBC)1
1RecruitingTreatmentEverolimus / Neuroendocrine Tumors1
1RecruitingTreatmentHead and Neck Carcinoma / Lung Cancers1
1RecruitingTreatmentLeukaemia, Lymphoblastic / Lymphoma, Lymphoblastic1
1RecruitingTreatmentMalignant Neoplasm of Breast / Malignant Neoplasms of Digestive Organs / Malignant Neoplasms of Female Genital Organs / Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites / Malignant Neoplasms of Independent (Primary) Multiple Sites / Malignant Neoplasms of Lip Oral Cavity and Pharynx / Malignant Neoplasms of Mesothelial and Soft Tissue / Malignant Neoplasms of Respiratory and Intrathoracic Organs / Malignant Neoplasms of Thyroid and Other Endocrine Glands / Malignant Neoplasms of Urinary Tract / Neoplasms of Uncertain or Unknown Behavior1
1RecruitingTreatmentNeoplasms, Breast1
1RecruitingTreatmentRecurrent Adult Hodgkin's Lymphoma / Recurrent Childhood Hodgkin Lymphoma / Recurrent Hodgkin Lymphoma / Refractory Hodgkin Lymphoma1
1RecruitingTreatmentRenal Cell Carcinoma Recurrent1
1RecruitingTreatmentTransplantation, Liver1
1RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
1TerminatedNot AvailableCancers1
1TerminatedTreatment714leukemia / Malignant Lymphomas1
1TerminatedTreatmentCancer, Breast2
1TerminatedTreatmentCancers1
1TerminatedTreatmentGraft Versus Host Disease (GVHD)1
1TerminatedTreatmentHead and Neck Carcinoma2
1TerminatedTreatmentHepatocellular,Carcinoma1
1TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1TerminatedTreatmentLung Cancers / Metastatic Cancers1
1TerminatedTreatmentLung Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1TerminatedTreatmentMultiple Myeloma in Relapse1
1TerminatedTreatmentNeoplasm Metastases / Neuroendocrine Tumors / Non-Small Cell Lung Carcinoma (NSCLC) / Renal Cell Adenocarcinoma1
1TerminatedTreatmentNeoplasms1
1TerminatedTreatmentRenal Cell Adenocarcinoma2
1Unknown StatusTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1Unknown StatusTreatmentLeukemias1
1Unknown StatusTreatmentLocally Advanced Disease / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1Unknown StatusTreatmentMetastatic or Locally Advanced Solid Tumors1
1WithdrawnTreatmentCervical Cancers1
1WithdrawnTreatmentLiver Cancer1
1WithdrawnTreatmentRecurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Salivary Gland Squamous Cell Carcinoma / Tongue Cancer1
1, 2Active Not RecruitingTreatmentAdenocarcinomas / Neoplasms, Pancreatic1
1, 2Active Not RecruitingTreatmentAdult Nasal Type Extranodal NK/T-Cell Lymphoma / Anaplastic Large Cell Lymphoma / Angioimmunoblastic T-Cell Lymphoma / B-cell Adult Acute Lymphoblastic Leukemia / Chronic Lymphocytic Leukemia (CLL) - Refractory / Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Hepatosplenic T-Cell Lymphoma / Nodal marginal zone B-cell lymphomas / Post-Transplant Lymphoproliferative Disorder / Primary Central Nervous System Non-Hodgkin Lymphoma / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Adult T-Cell Leukemia/Lymphoma / Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Mycosis Fungoides/Sezary Syndrome / Recurrent Small Lymphocytic Lymphoma / Refractory Multiple Myeloma / Splenic Marginal Zone Lymphoma / T-cell Adult Acute Lymphoblastic Leukemia / Waldenström's Macroglobulinemia (WM)1
1, 2Active Not RecruitingTreatmentAdult Nasal Type Extranodal NK/T-Cell Lymphoma / Anaplastic Large Cell Lymphoma / Angioimmunoblastic T-Cell Lymphoma / Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Hepatosplenic T-Cell Lymphoma / Nodal marginal zone B-cell lymphomas / Peripheral T-Cell Lymphoma (PTCL) / Post-Transplant Lymphoproliferative Disorder / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent Adult T-Cell Leukemia/Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Mycosis Fungoides/Sezary Syndrome / Splenic Marginal Zone Lymphoma / Waldenström's Macroglobulinemia (WM)1
1, 2Active Not RecruitingTreatmentBrain and Central Nervous System Tumors2
1, 2Active Not RecruitingTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentCentral Nervous System Metastases / Her2-Positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
1, 2Active Not RecruitingTreatmentHistological Evidence of Metastatic Clear Cell Renal Cell Carcinoma / Metastatic Clear Cell Renal Cell Carcinoma / Of Discontinuing Sunitinib, Sorafenib or Pazopanib. Previous / That Has Been Previously Treated With 1-3 Prior Regimens. Phase 1 Only, Any Number of Prior Regimens / Therapy With Bevacizumab, IL2, or Interferon Are Permitted / With Evidence of Progressive Disease on or Within 6 Months1
1, 2Active Not RecruitingTreatmentMalignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm1
1, 2Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
1, 2Active Not RecruitingTreatmentMetastatic Renal Cell Carcinoma1
1, 2Active Not RecruitingTreatmentProgressive Neuroendocrine Tumors of pancreatic origin1
1, 2Active Not RecruitingTreatmentWaldenström's Macroglobulinemia (WM)1
1, 2CompletedTreatmentAcinar Cell Adenocarcinoma of the Pancreas / Duct Cell Adenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage IV Pancreatic Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2CompletedTreatmentAcute Lymphocytic Leukemia (ALL) / Leukemias1
1, 2CompletedTreatmentAdenocarcinoma of the Esophagus / Adenocarcinomas of the Gastroesophageal Junction / Advanced Gastric Cancer / Diffuse Adenocarcinoma of the Stomach / Intestinal Adenocarcinoma of the Stomach / Mixed Adenocarcinoma of the Stomach / Recurrent Esophageal Cancer / Recurrent Gastric Cancer / Stage IV Esophageal Cancer1
1, 2CompletedTreatmentAdult Synovial Sarcoma / Recurrent Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
1, 2CompletedTreatmentAdvanced or Metastatic Pancreatic Adenocarcinoma1
1, 2CompletedTreatmentAgnogenic Myeloid Metaplasia / Leukemias / Mantle Cell Lymphoma (MCL)1
1, 2CompletedTreatmentAnaplastic Large Cell Lymphoma, ALK-Negative / Angioimmunoblastic T Cell Lymphoma / Cutaneous T Cell Lymphomas (CTCL) / Peripheral T Cell Lymphoma Unspecified1
1, 2CompletedTreatmentAngiolipoma / Tuberous Sclerosis1
1, 2CompletedTreatmentBladder Cancers1
1, 2CompletedTreatmentBrain and Central Nervous System Tumors1
1, 2CompletedTreatmentBrain and Central Nervous System Tumors / Prostate Cancer1
1, 2CompletedTreatmentCD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma1
1, 2CompletedTreatmentCancer, Breast2
1, 2CompletedTreatmentCancer, Breast / Neoplasms Metastasis1
1, 2CompletedTreatmentCancers of the Head and Neck / Neoplasms, Head and Neck1
1, 2CompletedTreatmentCarcinoma, Colorectal / Colorectal Cancers / Colorectal Tumors / Neoplasms, Colorectal1
1, 2CompletedTreatmentColorectal Cancers1
1, 2CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
1, 2CompletedTreatmentEpilepsies / Tuberous Sclerosis Complex (TSC)1
1, 2CompletedTreatmentGastrointestinal Cancers1
1, 2CompletedTreatmentGastrointestinal Stromal Tumors1
1, 2CompletedTreatmentHead and Neck Carcinoma1
1, 2CompletedTreatmentHepatocellular,Carcinoma1
1, 2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2CompletedTreatmentLeukemia, Lymphocytic1
1, 2CompletedTreatmentLeukemias1
1, 2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2CompletedTreatmentLung Cancers1
1, 2CompletedTreatmentLymphangioleiomyomatosis / Tuberous Sclerosis1
1, 2CompletedTreatmentMalignant Lymphomas1
1, 2CompletedTreatmentMetastatic Gastric Cancers1
1, 2CompletedTreatmentMetastatic Renal Cell Cancer1
1, 2CompletedTreatmentMetastatic, Androgen Independent Prostate Cancer / Prostate Cancer1
1, 2CompletedTreatmentPancreatic Cancer Metastatic1
1, 2CompletedTreatmentProstate Cancer1
1, 2CompletedTreatmentRenal Cancers1
1, 2CompletedTreatmentRenal Cell Adenocarcinoma1
1, 2CompletedTreatmentSubependymal Giant Cell Astrocytoma / Tuberous Sclerosis1
1, 2Not Yet RecruitingTreatmentClassical Hodgkin Lymphoma1
1, 2Not Yet RecruitingTreatmentTransplantation, Liver2
1, 2RecruitingTreatmentAcute Coronary Syndromes (ACS)1
1, 2RecruitingTreatmentAdult Living Donor Kidney Transplant Recipients / Living Kidney Donors / Transplant, Kidney1
1, 2RecruitingTreatmentAnaplastic Gliomas / Glioblastomas / Neoplasms, Brain1
1, 2RecruitingTreatmentCancer, Breast1
1, 2RecruitingTreatmentChildren, Adolescents and Young Adults With Refractory or Recurrent Malignancies1
1, 2RecruitingTreatmentColorectal Adenocarcinoma (CRC) / Gastric Adenocarcinoma / Renal Cell Adenocarcinoma / Transitional Cell Carcinoma1
1, 2RecruitingTreatmentHormone Receptor (HR)-Positive Breast Cancer / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
1, 2RecruitingTreatmentLymphoma, Hodgkins1
1, 2RecruitingTreatmentNeuroendocrine Carcinomas1
1, 2RecruitingTreatmentNeuroendocrine Tumors1
1, 2RecruitingTreatmentPTEN gene mutation / PTEN Hamartoma Tumor Syndrome1
1, 2RecruitingTreatmentPancreatic Adenocarcinoma Metastatic1
1, 2RecruitingTreatmentProgeria1
1, 2RecruitingTreatmentRecurrent and Refractory Solid Tumors1
1, 2SuspendedTreatmentAdvanced Solid Tumors1
1, 2TerminatedTreatmentCancer of the Ovary / Cancers / Malignant Neoplasm of Colon / Neuroendocrine1
1, 2TerminatedTreatmentCancer, Breast1
1, 2TerminatedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Cancer, Recurrent / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
1, 2TerminatedTreatmentHead and Neck Carcinoma2
1, 2TerminatedTreatmentLiver Cancer1
1, 2TerminatedTreatmentLung Cancers1
1, 2TerminatedTreatmentMalignant Neoplasm of Pancreas1
1, 2TerminatedTreatmentMetastatic Breast Cancer (MBC)1
1, 2TerminatedTreatmentNeoplasms1
1, 2Unknown StatusTreatmentAdvanced Malignancies1
1, 2Unknown StatusTreatmentCarcinoid Tumors / Neuroendocrine Tumors1
1, 2Unknown StatusTreatmentEnd-Stage Renal Disease (ESRD) / Renal Failure1
1, 2Unknown StatusTreatmentHematologic Diseases1
1, 2Unknown StatusTreatmentHepatocellular,Carcinoma1
1, 2WithdrawnTreatmentChronic Myeloid Leukemia (CML)1
2Active Not RecruitingPreventionGliomas1
2Active Not RecruitingPreventionRespiratory Tract Infections (RTI)1
2Active Not RecruitingTreatmentAcoustic Schwannoma / Neurofibromatosis Type 21
2Active Not RecruitingTreatmentAdvanced, Persistent, or Recurrent Endometrial Cancer1
2Active Not RecruitingTreatmentBladder Cancers / Metastatic Transitional Cell Carcinoma1
2Active Not RecruitingTreatmentBladder Carcinoma / Transitional Cell Carcinoma1
2Active Not RecruitingTreatmentCD20+, B-cell Lymphomas / Gray Zone Lymphoma / Hodgkins Disease (HD) / Mantle Cell Lymphoma (MCL) / Non-Mantle Cell Low Grade B Cell Lymphomas (SLL/CLL) / Transformed Lymphoma/DLBCL/PMBCL1
2Active Not RecruitingTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2Active Not RecruitingTreatmentCancer, Breast5
2Active Not RecruitingTreatmentCancer, Breast / Triple Negative Breast Cancer (TNBC)1
2Active Not RecruitingTreatmentClear-cell Metastatic Renal Cell Carcinoma1
2Active Not RecruitingTreatmentDifferentiated Thyroid Cancer (DTC)1
2Active Not RecruitingTreatmentEndometrial Cancers2
2Active Not RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2Active Not RecruitingTreatmentFibrolamellar Carcinoma / Fibrolamellar Liver Cancer1
2Active Not RecruitingTreatmentGastrin-Producing Neuroendocrine Tumor / Malignant Pancreatic Gastrinoma / Malignant Pancreatic Glucagonoma / Malignant Pancreatic Insulinoma / Malignant Pancreatic Somatostatinoma / Pancreatic Alpha Cell Adenoma / Pancreatic Beta Cell Adenoma / Pancreatic Delta Cell Adenoma / Pancreatic G-Cell Adenoma / Pancreatic Gastrinoma / Pancreatic Glucagonoma / Pancreatic Insulinoma / Pancreatic Neuroendocrine Tumor G1 / Pancreatic Neuroendocrine Tumor G2 / Pancreatic Polypeptide Tumor / Pancreatic Vipoma / Recurrent Pancreatic Carcinoma / Recurrent Pancreatic Neuroendocrine Carcinoma / Somatostatin-Producing Neuroendocrine Tumor / Stage III Pancreatic Cancer / Stage IV Pancreatic Cancer1
2Active Not RecruitingTreatmentGastrointestinal Neuroendocrine Tumors / Gastrointestinal Tumors / Pancreatic Tumors / Progressive Neuroendocrine Tumors of pancreatic origin1
2Active Not RecruitingTreatmentHead and Neck Carcinoma2
2Active Not RecruitingTreatmentHepatic Metastases / Metastases / Neuroendocrine Tumors1
2Active Not RecruitingTreatmentHormone Receptor Positive Breast Cancer1
2Active Not RecruitingTreatmentMalignant Peripheral Nerve Sheath Tumour (MPNST) / MPNST / Sarcomas1
2Active Not RecruitingTreatmentMalignant Ovarian Mixed Epithelial Tumor / Ovarian Endometrioid Adenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Cystadenocarcinoma / Ovarian Serous Surface Papillary Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Ovarian Germ Cell Tumor / Recurrent Primary Peritoneal Carcinoma / Undifferentiated Ovarian Carcinoma1
2Active Not RecruitingTreatmentMelanoma (Skin)1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentMetastatic Renal Cell Cancer / Renal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
2Active Not RecruitingTreatmentMetastatic Renal Cell Carcinoma1
2Active Not RecruitingTreatmentNeoplasms1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingTreatmentMTor Protein / Neoplasms, Breast1
2Active Not RecruitingTreatmentNeuroendocrine Carcinoma of the Lung and Thymus1
2Active Not RecruitingTreatmentProstate Cancer1
2Active Not RecruitingTreatmentRenal Cancers2
2Active Not RecruitingTreatmentRenal Cell Adenocarcinoma2
2Active Not RecruitingTreatmentThymoma and Thymic Carcinoma1
2Active Not RecruitingTreatmentThyroid Cancers2
2Active Not RecruitingTreatmentTransplantation, Kidney1
2Active Not RecruitingTreatmentTuberous Sclerosis1
2CompletedNot AvailableClear Cell Renal Cell Carcinoma / Clear-cell Metastatic Renal Cell Carcinoma1
2CompletedPreventionAdvanced Breast Cancer1
2CompletedPreventionHighly-sensitized Kidney Transplant Recipients1
2CompletedTreatmentAdenocarcinomas / Carcinoma NOS / Hypernephroid / Nephroid Carcinoma / Renal Cell / Renal Cell Adenocarcinoma1
2CompletedTreatmentAdenocarcinomas / Carcinoma NOS / Non Clear Cell Renal Carcinoma / Papillary Cell Renal Carcinoma / Renal Cell1
2CompletedTreatmentAdvanced Adult Hepatocellular Carcinoma1
2CompletedTreatmentAdvanced Gastric Cancer1
2CompletedTreatmentAdvanced Non-clear Cell Renal Cell Carcinoma1
2CompletedTreatmentAstrocytomas / Gliomas / Low-Grade Gliomas1
2CompletedTreatmentAstrocytomas / Low-Grade Gliomas / Oligoastrocytoma, Mixed / Oligodendrogliomas1
2CompletedTreatmentAutism, Early Infantile / Self-injury / Tuberous Sclerosis Complex (TSC)1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Carcinoma1
2CompletedTreatmentCancer, Breast6
2CompletedTreatmentCancers1
2CompletedTreatmentCarcinoids / Carcinoma NOS / Neuroendocrine / Non Functioning / Non Functioning Neuroendocrine Tumors/NET / Non Syndromic Neuroendocrine Tumors/NET1
2CompletedTreatmentCarcinoma of Unknown Primary Origin1
2CompletedTreatmentCarcinoma, Adenoid Cystic1
2CompletedTreatmentCarcinoma, Islet Cell / Neoplasms, Pancreatic / Neuroendocrine Carcinomas / Neuroendocrine Tumors1
2CompletedTreatmentCarcinoma, Islet Cell / Neuroendocrine Carcinomas1
2CompletedTreatmentClear Cell Renal Cell Carcinoma1
2CompletedTreatmentColorectal Adenocarcinoma1
2CompletedTreatmentColorectal Cancers2
2CompletedTreatmentCondition After Allogenic Peripheral Stem Cell Transplantation (SCT)1
2CompletedTreatmentEndometrial Cancers2
2CompletedTreatmentEsophageal Cancers / Malignant Neoplasm of Stomach1
2CompletedTreatmentExtra-Adrenal Paraganglioma / Non-functioning Carcinoid / Pheochromocytomas1
2CompletedTreatmentGerm Cell Cancer / Testicular Cancer1
2CompletedTreatmentGerm Cell Tumors1
2CompletedTreatmentGlioblastoma Multiforme (GBM)1
2CompletedTreatmentHER-2 Positive Breast Cancer1
2CompletedTreatmentHead and Neck Carcinoma2
2CompletedTreatmentHepatocellular,Carcinoma2
2CompletedTreatmentHer2-negative Locally Advanced Breast Cancer / Her2-negative Metastatic Breast Cancer1
2CompletedTreatmentHormone Refractory Prostate Cancer1
2CompletedTreatmentLeukemias / Lymphoproliferative Disorders / Malignant Lymphomas1
2CompletedTreatmentLiver Cancer1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2CompletedTreatmentLymphangioleiomyomatosis1
2CompletedTreatmentLymphoma, Hodgkins1
2CompletedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2CompletedTreatmentMalignant Lymphomas1
2CompletedTreatmentMalignant Neoplasm of Pancreas1
2CompletedTreatmentMalignant Pleural Mesothelioma (MPM)1
2CompletedTreatmentMantle Cell Lymphoma (MCL)1
2CompletedTreatmentMarginal Zone B-Cell Lymphoma1
2CompletedTreatmentMelanoma (Skin)2
2CompletedTreatmentMetastatic Bone Sarcomas / Relapsed Osteosarcoma1
2CompletedTreatmentMetastatic Breast Cancer (MBC)2
2CompletedTreatmentMetastatic Colorectal Cancers1
2CompletedTreatmentMetastatic Gastric Cancers1
2CompletedTreatmentMetastatic Melanoma2
2CompletedTreatmentMetastatic Renal Cell Carcinoma1
2CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm1
2CompletedTreatmentNeoplasms, Breast1
2CompletedTreatmentNeoplasms, Gastrointestinal1
2CompletedTreatmentNeuroendocrine Carcinomas1
2CompletedTreatmentNeurofibromatoses / Neurofibromatosis Type 1 / Plexiform Neurofibroma1
2CompletedTreatmentNeurofibromatosis 11
2CompletedTreatmentNeurofibromatosis 21
2CompletedTreatmentNeurofibromatosis Type II1
2CompletedTreatmentPolycystic Liver Disease (PLD)1
2CompletedTreatmentProgressive Sarcoma1
2CompletedTreatmentProstate Cancer3
2CompletedTreatmentRenal Cancers2
2CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
2CompletedTreatmentRenal Cell Adenocarcinoma5
2CompletedTreatmentSarcoma, Bone / Soft Tissue Sarcoma (STS)1
2CompletedTreatmentSolid Malignancies / Tumors, Solid1
2CompletedTreatmentStomach Neoplasms2
2CompletedTreatmentSystemic Mastocytosis1
2CompletedTreatmentTransitional Cell Carcinoma1
2CompletedTreatmentTransplantation, Kidney2
2CompletedTreatmentTransplantation, Renal1
2CompletedTreatmentTuberous Sclerosis Complex (TSC)1
2CompletedTreatmentTumors, Solid1
2CompletedTreatmentUrothelial Cancer1
2CompletedTreatmentUveal Melanoma1
2CompletedTreatmentUveitis1
2CompletedTreatmentWaldenström's Macroglobulinemia (WM)1
2Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Not Yet RecruitingTreatmentNeoplasms, Breast1
2Not Yet RecruitingTreatmentRenal Cell Adenocarcinoma1
2RecruitingPreventionGraft Versus Host Disease (GVHD)1
2RecruitingTreatmentAdvanced Breast Cancer1
2RecruitingTreatmentBreast Cancer Stage IIB1
2RecruitingTreatmentCancer of the Ovary / Endometrial Cancers1
2RecruitingTreatmentCancer, Breast2
2RecruitingTreatmentCancer, Breast / Estrogen Receptor Negative / HER2/Neu Negative / Invasive Breast Carcinoma / Progesterone Receptor Negative / Triple-Negative Breast Carcinoma1
2RecruitingTreatmentCholangiocarcinoma of the Extrahepatic Bile Duct / Gallbladder Cancer1
2RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG)1
2RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG) / Gliomas1
2RecruitingTreatmentEndometrial Cancers1
2RecruitingTreatmentEndometrial Carcinoma / Malignant Neoplasms of Female Genital Organs1
2RecruitingTreatmentEpilepsies / Focal Cortical Dysplasia / Tuberous Sclerosis Complex (TSC)1
2RecruitingTreatmentEstrogen Receptor Positive Breast Cancer1
2RecruitingTreatmentGliomas1
2RecruitingTreatmentHER2-negative Circulating Tumor Cells / HER2-negative Und Hormone-receptor Positive Metastatic Breast Cancer / Postmenopausal Female Patients1
2RecruitingTreatmentLow Grade Glioma (LGG) / Oligoastrocytoma, Mixed / Oligodendrogliomas / WHO Grade II Astrocytomas1
2RecruitingTreatmentMalignant Solid Neoplasms1
2RecruitingTreatmentMelanoma / Neoplasms Metastasis / TOR Serine-Threonine Kinases1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2RecruitingTreatmentNeoplasms, Brain1
2RecruitingTreatmentNeuroendocrine Carcinoma, Grade 1 [Well-differentiated Neuroendocrine Carcinoma] That Switched to G3 / Neuroendocrine Carcinoma, Grade 2 [Moderately Differentiated Neuroendocrine Carcinoma] That Switched to G3 / Neuroendocrine Carcinoma, Grade 3 / Neuroendocrine Tumor, Grade 3 and Disease Progression as Measured by Response Evaluation Criteria in Solid Tumors (RECIST 1.1.) / Poorly Differentiated Malignant Neuroendocrine Carcinoma / Poorly Differentiated Neuroendocrine Carcinoma1
2RecruitingTreatmentNeuroendocrine Carcinomas3
2RecruitingTreatmentNeuroendocrine Carcinomas / Neuroendocrine Neoplasms / Neuroendocrine Tumors / Neuroendocrine Tumors of the Gastrointestinal Tract and Pancreas1
2RecruitingTreatmentNeuroendocrine Tumors1
2RecruitingTreatmentNon Clear Cell Renal Cell Carcinoma (nccRCC)1
2RecruitingTreatmentOrthotopic Liver Transplant1
2RecruitingTreatmentPediatric Progressive Low-grade Gliomas / Pediatric Recurrent Progressive Low-grade Gliomas1
2RecruitingTreatmentPrimary Aldosteronism1
2RecruitingTreatmentRare Tumor / Refractory Tumors1
2RecruitingTreatmentRecurrent Childhood Ependymoma1
2RecruitingTreatmentRecurrent Meningiomas / Resistant Meningiomas1
2RecruitingTreatmentRefractory Hurthle Cell Thyroid Cancer1
2RecruitingTreatmentRefractory Pediatric AML / Refractory Pediatric Solid Tumors / Relapsed Pediatric AML / Relapsed Pediatric Solid Tumors1
2RecruitingTreatmentRenal Cell Adenocarcinoma1
2RecruitingTreatmentSoft Tissue Sarcoma (STS)1
2RecruitingTreatmentMTOR / TSC1 / TSC2 / Tuberous Sclerosis Complex (TSC)1
2RecruitingTreatmentThyroid Cancers1
2RecruitingTreatmentTuberculosis1
2SuspendedTreatmentChondrosarcomas1
2TerminatedPreventionRenal Cancers1
2TerminatedTreatmentAge-Related Macular Degeneration (ARMD) / Choroidal Neo-Vascular Age-onset Macular Degeneration1
2TerminatedTreatmentBirt-Hogg-Dube Syndrome / Chromophobe Renal Cell Carcinoma / Renal Cancers1
2TerminatedTreatmentBladder Cancers1
2TerminatedTreatmentCancer of the Breast / Cancer, Breast / Neoplasms, Breast1
2TerminatedTreatmentCancer, Breast2
2TerminatedTreatmentCastrate Resistant Prostate Cancer (CRPC) / Chemotherapy Naive Prostate Cancer / Prostate Cancer1
2TerminatedTreatmentColorectal Cancers1
2TerminatedTreatmentCutaneous T-Cell Lymphoma (CTCL)1
2TerminatedTreatmentEndocrine Breast Diseases / Neoplasms Metastasis / Neoplasms, Breast1
2TerminatedTreatmentEstrogen Receptor-Positive Breast Cancer / Gastrinoma / Glucagonoma / HER2-Negative Breast Cancer / Insulinoma / Mucositis / Oral Complications / Pancreatic Polypeptide Tumor / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Recurrent Islet Cell Carcinoma / Renal Cell Cancer, Recurrent / Somatostatinoma / Stage III Renal Cell Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer / Stage IV Renal Cell Cancer1
2TerminatedTreatmentGastrinoma / Glucagonoma / Hepatic Metastases / Insulinoma / Pancreatic Polypeptide Tumor / Recurrent Islet Cell Carcinoma / Somatostatinoma1
2TerminatedTreatmentGlioblastoma Multiforme (GBM)1
2TerminatedTreatmentIntracranial Meningioma1
2TerminatedTreatmentIslet Cell Tumor1
2TerminatedTreatmentKaposi s Sarcoma (KS)1
2TerminatedTreatmentKidney (Renal Cell) Cancer / Neoplasms, Kidney1
2TerminatedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2TerminatedTreatmentMalignant Lymphomas1
2TerminatedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentMetastatic Clear Cell Renal Carcinoma1
2TerminatedTreatmentMetastatic Melanoma1
2TerminatedTreatmentMetastatic Renal Cancer1
2TerminatedTreatmentMetastatic Renal Cell Carcinoma1
2TerminatedTreatmentMyelodysplastic Syndromes1
2TerminatedTreatmentPeutz-Jeghers Syndrome (PJS)1
2TerminatedTreatmentPlexiform Neurofibroma Associated With Neurofibromatosis Type 11
2TerminatedTreatmentProgressive Neuroendocrine Tumors of pancreatic origin1
2TerminatedTreatmentRecurrent Hepatitis C1
2TerminatedTreatmentRenal Cancers1
2TerminatedTreatmentRenal Cell Adenocarcinoma1
2TerminatedTreatmentSarcomas1
2TerminatedTreatmentSporadic Angiomyolipomas (AMLs)1
2TerminatedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2Unknown StatusTreatmentCancer, Breast1
2Unknown StatusTreatmentCholangiocarcinomas2
2Unknown StatusTreatmentHead and Neck Carcinoma1
2Unknown StatusTreatmentHepatic Failure / Liver Cirrhosis / Liver Diseases / Neoplasms, Hepatic1
2Unknown StatusTreatmentHormone Receptor Positive Malignant Neoplasm of Breast1
2Unknown StatusTreatmentKidney Diseases1
2Unknown StatusTreatmentMesothelioma, Malignant1
2Unknown StatusTreatmentNeoplasms, Breast1
2Unknown StatusTreatmentNeuroendocrine Tumors1
2Unknown StatusTreatmentProstate Cancer2
2Unknown StatusTreatmentRefractory or Relapsed Osteosarcoma1
2Unknown StatusTreatmentRefractory or Relapsed RMS and Soft Tissue Sarcomas1
2Unknown StatusTreatmentRenal Insufficiency,Chronic / Transplantation, Liver1
2WithdrawnTreatmentCancer, Breast3
2WithdrawnTreatmentLocally Metastatic Malignant Neoplasm1
2WithdrawnTreatmentMultiple Myeloma (MM)1
2WithdrawnTreatmentNeoplasms Metastasis / Neoplastic Processes / Peutz-Jeghers Syndrome (PJS)1
2WithdrawnTreatmentSegmental Overgrowth Syndrome1
2WithdrawnTreatmentSturge Weber Syndrome1
2, 3Active Not RecruitingTreatmentUterine Cancers1
2, 3Not Yet RecruitingTreatmentFacial Angiofibromas1
2, 3RecruitingTreatmentRenal Cell Cancer Metastatic1
2, 3RecruitingTreatmentTSC Related Autism / TSC Related Cognitive Disability / TSC Related Learning Problems / Tuberous Sclerosis Complex (TSC)1
2, 3TerminatedTreatmentDelayed Graft Function1
2, 3TerminatedTreatmentGraft Versus Host Disease (GVHD)1
2, 3TerminatedTreatmentPolycystic Kidney Diseases1
3Active Not RecruitingTreatmentAdvanced Gastric Cancer / Esophagogastric Junction Cancer1
3Active Not RecruitingTreatmentAdvanced NET of GI Origin / Advanced NET of Lung Origin / Neuroendocrine Tumors1
3Active Not RecruitingTreatmentAdvanced or Metastatic (Medically or Surgically Unresectable) Clear-cell Renal Cell Carcinoma1
3Active Not RecruitingTreatmentBreast Cancer Metastatic1
3Active Not RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
3Active Not RecruitingTreatmentPost Menopausal Breast Cancer1
3Active Not RecruitingTreatmentPrevention of Acute Rejection in Paediatric Recipients of a Renal Transplant1
3Active Not RecruitingTreatmentRenal Cancers1
3Active Not RecruitingTreatmentRenal Cell Adenocarcinoma1
3CompletedBasic ScienceHepatitis C Recurrence After Liver Transplant1
3CompletedPreventionCardiac Transplantation1
3CompletedPreventionDe Novo Kidney Transplant Recipients / Transplantation, Renal1
3CompletedPreventionHeart Transplantation1
3CompletedPreventionLymphoma, Large B-Cell, Diffuse (DLBCL)1
3CompletedPreventionRejection, Transplant1
3CompletedPreventionTransplantation, Kidney2
3CompletedPreventionTransplantation, Renal3
3CompletedTreatmentAdvanced Gastric Cancer1
3CompletedTreatmentAdvanced Neuroendocrine Tumors of Pancreatic Origin1
3CompletedTreatmentCancer, Breast3
3CompletedTreatmentCarcinoid Tumors / Malignant Carcinoid Syndrome1
3CompletedTreatmentCarcinoma NOS1
3CompletedTreatmentDe Novo Renal Transplantation1
3CompletedTreatmentHER2/Neu Over-expressing Locally Advanced Breast Cancer / Metastatic Breast Cancer (MBC)1
3CompletedTreatmentHeart Transplantation1
3CompletedTreatmentLiver Transplant Recipients1
3CompletedTreatmentLymphangioleiomyomatosis (LAM) / Tuberous Sclerosis Complex (TSC)1
3CompletedTreatmentMetastatic Breast Cancer (MBC)1
3CompletedTreatmentMetastatic Renal Cell Carcinoma1
3CompletedTreatmentOrgan Transplantation, Renal Transplantation1
3CompletedTreatmentRejection, Transplant1
3CompletedTreatmentRejection, Transplant / Transplantation, Kidney1
3CompletedTreatmentRenal Interstitial Fibrosis1
3CompletedTreatmentSubependymal Giant Cell Astrocytoma / Tuberous Sclerosis1
3CompletedTreatmentTransplant, Kidney2
3CompletedTreatmentTransplant; Failure, Kidney1
3CompletedTreatmentTransplantation, Kidney2
3CompletedTreatmentTransplantation, Liver4
3CompletedTreatmentTransplantation, Lung2
3CompletedTreatmentTransplantation, Renal2
3CompletedTreatmentTuberous Sclerosis Complex-associated Refractory Seizures1
3Not Yet RecruitingPreventionTransplantation, Liver1
3Not Yet RecruitingTreatmentEpilepsy and Focal Cortical Dysplasia II1
3Not Yet RecruitingTreatmentProstate Cancer1
3RecruitingTreatmentAutosomal Dominant Polycystic Kidney Disease (ADPKD)1
3RecruitingTreatmentCancer, Breast2
3RecruitingTreatmentCancer, Breast / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast / Locally Advanced Malignant Neoplasm / Metastatic Breast Cancer (MBC)1
3RecruitingTreatmentCardiac Allograft Vasculopathy / Chronic Kidney Disease (CKD) / Heart Transplant Failure and Rejection / Heart Transplant Infection / Immunosuppression / Pediatric Heart Transplantation / Post-Transplant Lymphoproliferative Disorder1
3RecruitingTreatmentChronic Kidney Disease (CKD)1
3RecruitingTreatmentNeuroendocrine Tumors1
3RecruitingTreatmentNeuroendocrine Tumors / Progressive Neuroendocrine Tumors of pancreatic origin1
3RecruitingTreatmentPrimary Non-metastatic Breast Cancer / Who Remain Disease-free / Who Remain Disease-free After Receiving at Least 1 Year of Adjuvant Hormone Therapy1
3RecruitingTreatmentRenal Cell Adenocarcinoma1
3RecruitingTreatmentTransplantation, Liver1
3RecruitingTreatmentTuberous Sclerosis Complex (TSC)1
3SuspendedTreatmentCancer, Breast1
3TerminatedTreatmentChronic Renal Failure (CRF)1
3TerminatedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage III Renal Cell Cancer AJCC v7 / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC V71
3TerminatedTreatmentMetastatic Breast Cancer (MBC)1
3Unknown StatusTreatmentCardiac Transplantation / Skin Cancers1
3Unknown StatusTreatmentCoronary Artery Disease / Coronary Artery Restenosis1
4Active Not RecruitingNot AvailableGrowth and Development1
4Active Not RecruitingBasic ScienceHuman Immunodeficiency Virus (HIV) / Transplant, Kidney / Transplantation, Liver1
4Active Not RecruitingPreventionInfections, Cytomegalovirus / Transplantation Infection1
4Active Not RecruitingTreatmentCytomegalovirus / Transplantation, Kidney1
4Active Not RecruitingTreatmentInfections, Cytomegalovirus / Transplantation Infection1
4CompletedNot AvailableFunction of Renal Transplant1
4CompletedDiagnosticCardiac Transplant1
4CompletedOtherHER2/Neu-negative Carcinoma of Breast / Hormone Receptor Positive Malignant Neoplasm of Breast / Recurrent Breast Cancer1
4CompletedOtherRenal Failure1
4CompletedOtherTransplant, Kidney1
4CompletedPreventionCardiac Transplantation1
4CompletedPreventionChronic Rejection of Cardiac Transplant1
4CompletedPreventionDisorder Related to Cardiac Transplantation1
4CompletedPreventionHeart Transplantation1
4CompletedPreventionTransplantation, Kidney1
4CompletedPreventionTransplantation, Renal3
4CompletedSupportive CareHepatitis C Viral Infection / Renal Allograft1
4CompletedTreatmentAutosomal Dominant Polycystic Kidney Disease (ADPKD)1
4CompletedTreatmentBK Virus Infection1
4CompletedTreatmentCarcinoma, Large Cell / Neuroendocrine Tumors1
4CompletedTreatmentCardiac Transplantation / Renal Insufficiency,Chronic1
4CompletedTreatmentChronic Allograft Dysfunction in Renal Transplantation1
4CompletedTreatmentChronic Kidney Disease (CKD) / End Stage Renal Disease (ESRD) / Hemodialysis-dependent patients / Renal Replacement Therapies / Transplantation, Renal1
4CompletedTreatmentChronic Renal Failure (CRF)1
4CompletedTreatmentComparative Study / Immunosuppressive Agents1
4CompletedTreatmentFailure of Exactly One Prior VEGF-targeted Therapy / Metastatic Renal Cell Carcinoma1
4CompletedTreatmentHeart Transplantation2
4CompletedTreatmentInfections, Cytomegalovirus / Renal Transplant Failure / Transplant; Complication, Rejection1
4CompletedTreatmentInterstitial Fibrosis (IF) / Transplant dysfunction1
4CompletedTreatmentKidney Transplantation, Renal Transplantation1
4CompletedTreatmentLocally Advanced Metastatic Breast Cancer / Locally Advanced or Metastatic Breast Cancer / Metastatic Breast Cancer (MBC) / Postmenopausal Women1
4CompletedTreatmentMetastatic Renal Cell Carcinoma1
4CompletedTreatmentMetastatic Renal Cell Carcinoma (mRCC)1
4CompletedTreatmentNeuroendocrine Tumors1
4CompletedTreatmentOestrogen Receptor Positive Advanced Breast Cancer1
4CompletedTreatmentPlanned Kidney Transplantation1
4CompletedTreatmentRenal Function1
4CompletedTreatmentRenal Function and Chronic Allograft Vasculopathy1
4CompletedTreatmentRenal Transplanted Recipients1
4CompletedTreatmentTransplant, Kidney1
4CompletedTreatmentTransplantation, Kidney1
4CompletedTreatmentTransplantation, Organ1
4CompletedTreatmentTransplantation, Renal3
4Not Yet RecruitingTreatmentDisorder Related to Renal Transplantation / Immunosuppression Related Infectious Disease / Virus Diseases1
4Not Yet RecruitingTreatmentRenal Angiomyolipomas1
4RecruitingNot AvailableLeft Ventricular Hypertrophy1
4RecruitingOtherTransplantation, Liver1
4RecruitingPreventionKidney Transplant Infection1
4RecruitingTreatmentBK Virus Nephropathy After Kidney Transplantation1
4RecruitingTreatmentChronic Renal Failure (CRF) / Graft Failure / Kidney Transplant Rejection / Transplant; Failure, Kidney1
4RecruitingTreatmentDrug Interaction Potentiation / Transplantation, Kidney1
4RecruitingTreatmentGastrointestinal Disorder, Functional / Kidney Transplant Rejection1
4RecruitingTreatmentHepatocellular,Carcinoma1
4RecruitingTreatmentLeft Ventricular Hypertrophy1
4RecruitingTreatmentNeoplasms1
4RecruitingTreatmentProgressive Neuroendocrine Tumors of pancreatic origin1
4RecruitingTreatmentRenal Cell Adenocarcinoma1
4RecruitingTreatmentTransplant, Kidney1
4TerminatedBasic ScienceDisorder Related to Renal Transplantation / Exercise, Aerobic / Strength, Muscle1
4TerminatedOtherRenal Cell Adenocarcinoma1
4TerminatedPreventionHeart Transplantation / Renal Function Abnormal1
4TerminatedPreventionImpaired Renal Function1
4TerminatedPreventionTransplantation, Renal1
4TerminatedTreatmentTransplantation, Renal2
4Unknown StatusPreventionDisorder Related to Renal Transplantation1
4Unknown StatusPreventionHeart Transplantation / Kidney Diseases1
4Unknown StatusPreventionImmunosuppression / Transplantation, Homologous1
4Unknown StatusPreventionKidney Transplant Recipients1
4Unknown StatusPreventionKidney; Complications, Allograft1
4Unknown StatusTreatmentCardiac Transplant1
4Unknown StatusTreatmentDelayed Function of Renal Transplant1
4Unknown StatusTreatmentImmunosuppression / Transplant, Kidney1
4Unknown StatusTreatmentInfections, Cytomegalovirus1
4Unknown StatusTreatmentTransplantation, Renal1
4WithdrawnNot AvailableTransplantation, Kidney1
4WithdrawnTreatmentTransplantation, Kidney1
Not AvailableActive Not RecruitingDiagnosticAdvanced Solid Tumors / Cancers1
Not AvailableActive Not RecruitingOtherHormone Receptor Positive Malignant Neoplasm of Breast / Metastatic Breast Cancer (MBC)1
Not AvailableActive Not RecruitingPreventionRenal Failure1
Not AvailableActive Not RecruitingTreatmentEnd Stage Renal Failure With Renal Transplant1
Not AvailableActive Not RecruitingTreatmentRecurrent Childhood Brain Tumor1
Not AvailableAvailableNot AvailableGastrointestinal Stromal Tumors1
Not AvailableCompletedNot AvailableCancer, Breast1
Not AvailableCompletedNot AvailableCancer, Breast / Renal Cell Adenocarcinoma1
Not AvailableCompletedNot AvailableNeuroendocrine Tumors1
Not AvailableCompletedBasic ScienceDifference of 12-hour AUC1
Not AvailableCompletedOtherUnspecified Adult Solid Tumor, Protocol Specific1
Not AvailableCompletedTreatmentHigh Model for End-Stage Liver Disease (MELD) Score1
Not AvailableCompletedTreatmentRenal Cell Adenocarcinoma1
Not AvailableCompletedTreatmentTransplantation, Kidney1
Not AvailableNo Longer AvailableNot AvailableMetastatic Renal Cell Cancer1
Not AvailableRecruitingNot AvailableEnd Stage Liver Diseases1
Not AvailableRecruitingNot AvailableHepatocellular,Carcinoma / Neuroendocrine Tumors1
Not AvailableRecruitingNot AvailableLymphangioleiomyomatosis1
Not AvailableRecruitingNot AvailablePancreatic Neuroendocrine Tumor, Well Differentiated and Progressive1
Not AvailableRecruitingBasic ScienceNeoplasms1
Not AvailableRecruitingTreatmentGastrointestinal Cancers1
Not AvailableRecruitingTreatmentImmunosuppression1
Not AvailableSuspendedTreatmentAdvanced Malignant Solid Neoplasm / Neoplasms / Neoplasms, Advanced Solid / Recurrent Malignant Solid Neoplasm / Recurrent Solid Neoplasm1
Not AvailableTerminatedTreatmentCalcineurin Inhibitor Toxicity / Chronic Allograft Injury1
Not AvailableTerminatedTreatmentEnd Stage Renal Failure With Renal Transplant1
Not AvailableUnknown StatusTreatmentTransplant, Kidney1
Not AvailableUnknown StatusTreatmentMicroRNA Profiles1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Chunghwa Chemical Synthesis and Biotech Co. Ltd.
  • Novartis AG
  • Quality Care
Dosage forms
FormRouteStrength
TabletOral10 mg/1
TabletOral10 mg
TabletOral2.5 mg/1
TabletOral2.5 mg
TabletOral5 mg
TabletOral5 mg/1
TabletOral7.5 mg/1
TabletOral7.5 mg
Tablet, for suspensionOral2 mg
Tablet, for suspensionOral2 mg/1
Tablet, for suspensionOral3 mg/1
Tablet, for suspensionOral3 mg
Tablet, for suspensionOral5 mg
Tablet, for suspensionOral5 mg/1
TabletOral0.25 mg
TabletOral0.50 mg
TabletOral0.75 mg
TabletOral0.25 mg/1
TabletOral0.5 mg/1
TabletOral0.75 mg/1
TabletOral1 mg/1
Prices
Unit descriptionCostUnit
Afinitor 10 mg tablet247.58USD tablet
Afinitor 5 mg tablet234.75USD tablet
Vesicare 10 mg tablet6.98USD tablet
Vesicare 5 mg tablet6.98USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6440990No1993-09-242013-09-24Us
CA2145383No2004-11-162013-09-24Canada
CA2225960No2004-05-112016-07-12Canada
US8410131Yes2006-05-012026-05-01Us
US8436010Yes2002-08-222022-08-22Us
US5665772Yes2000-03-092020-03-09Us
US6004973Yes1997-01-122017-01-12Us
US6239124Yes1998-02-112018-02-11Us
US6455518Yes1998-01-292018-01-29Us
US8778962Yes2002-08-182022-08-18Us
US9006224No2008-07-012028-07-01Us
US7741338No1999-12-062019-12-06Us
US7297703Yes2000-06-062020-06-06Us
US8617598Yes2003-03-272023-03-27Us

Properties

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

Spectra

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

Taxonomy

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

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

Enzymes

Kind
Protein
Organism
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Transporters

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

Drug created on August 29, 2007 09:37 / Updated on October 16, 2018 08:37