DGIdb - EVEROLIMUS Drug Record

EVEROLIMUS chembl:CHEMBL1908360 ApprovedAntineoplasticImmunotherapy

Alternate Names:

SDZ-RAD
AFINITOR DISPERZ
ZORTRESS
RAD001
RAD 666
RAD-666
AFINITOR
CERTICAN
RAD-001
VOTUBIA
EVEROLIMUS
42-O-(2-HYDROXYETHYL)RAPAMYCIN
40-O-(2-HYDROXYETHYL)-RAPAMYCIN
chembl:CHEMBL1908360
rxcui:141704
drugbank:01590
chemidplus:159351-69-6
pubchem.compound:6442177

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	immunosuppressant
FDA Approval	Pancreatic, gastrointestinal, or lung origin neuroendocrine tumors; Renal cell carcinoma, Subependymal giant cell astrocytoma associated with tuberous sclerosis, Breast cancer (ER+, HER2-)
Notes	rapalogue
Drug Class	Kinase Inhibitors
Drug Class	immunosuppressive agents
Year of Approval	2009

(13 More Sources)

Publications:

Powles et al., 2016, Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma., J. Clin. Oncol.
Klümpen et al., 2011, mTOR inhibitor treatment of pancreatic cancer in a patient With Peutz-Jeghers syndrome., J. Clin. Oncol.
Donovan et al., 2016, Widely metastatic atypical pituitary adenoma with mTOR pathway STK11(F298L) mutation treated with everolimus therapy., CNS Oncol
Carita et al., 2016, Dual inhibition of protein kinase C and p53-MDM2 or PKC and mTORC1 are novel efficient therapeutic approaches for uveal melanoma., Oncotarget
Kato et al., 2017, RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients., Clin. Cancer Res.
Schneider et al., 2015, Beneficial Effects of the mTOR Inhibitor Everolimus in Patients with Advanced Medullary Thyroid Carcinoma: Subgroup Results of a Phase II Trial., Int J Endocrinol
Wong CP et al., 2015, Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway., J Nat Prod
Salomé C et al., 2014, Benzofuran derivatives as anticancer inhibitors of mTOR signaling., Eur J Med Chem
Voss et al., 2014, Tumor genetic analyses of patients with metastatic renal cell carcinoma and extended benefit from mTOR inhibitor therapy., Clin. Cancer Res.
Wagle et al., 2014, Activating mTOR mutations in a patient with an extraordinary response on a phase I trial of everolimus and pazopanib., Cancer Discov
Lim et al., 2016, Next-generation sequencing reveals somatic mutations that confer exceptional response to everolimus., Oncotarget
Raushenbakh et al., 1976, [Induction of tyrosine aminotransferase by blastomogenic metabolites of tryptophan and tyrosine]., Biull Eksp Biol Med
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
Wagle et al., 2014, Response and acquired resistance to everolimus in anaplastic thyroid cancer., N. Engl. J. Med.
Ettenger et al., 2008, Multicenter trial of everolimus in pediatric renal transplant recipients: results at three year., Pediatr Transplant
Teachey et al., 2009, Mammalian target of rapamycin inhibitors and their potential role in therapy in leukaemia and other haematological malignancies., Br. J. Haematol.
Coppin, 2010, Everolimus: the first approved product for patients with advanced renal cell cancer after sunitinib and/or sorafenib., Biologics
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
George et al., 2009, Role of everolimus in the treatment of renal cell carcinoma., Ther Clin Risk Manag
Rostaing et al., mTOR inhibitor/proliferation signal inhibitors: entering or leaving the field?, J. Nephrol.
Albert et al., 2010, New inhibitors of the mammalian target of rapamycin signaling pathway for cancer., Expert Opin Investig Drugs
Stjepanovic N et al., 2015, Elucidating the genomic landscape of breast cancer: how will this affect treatment?, Pharmacogenomics
Di Nicolantonio et al., 2010, Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus., J. Clin. Invest.
Mohseni et al., 2010, PIK3CA and KRAS mutations predict for response to everolimus therapy: now that's RAD001., J. Clin. Invest.
Seront et al., 2012, Phase II study of everolimus in patients with locally advanced or metastatic transitional cell carcinoma of the urothelial tract: clinical activity, molecular response, and biomarkers., Ann. Oncol.
Kim et al., 2017, Prospective phase II trial of everolimus in PIK3CA amplification/mutation and/or PTEN loss patients with advanced solid tumors refractory to standard therapy., BMC Cancer
Shoji et al., 2012, Genotype-dependent efficacy of a dual PI3K/mTOR inhibitor, NVP-BEZ235, and an mTOR inhibitor, RAD001, in endometrial carcinomas., PLoS ONE
Weigelt et al., 2011, PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs., Oncogene
André et al., 2016, Molecular Alterations and Everolimus Efficacy in Human Epidermal Growth Factor Receptor 2-Overexpressing Metastatic Breast Cancers: Combined Exploratory Biomarker Analysis From BOLERO-1 and BOLERO-3., J. Clin. Oncol.
Seront et al., 2013, PTEN deficiency is associated with reduced sensitivity to mTOR inhibitor in human bladder cancer through the unhampered feedback loop driving PI3K/Akt activation., Br. J. Cancer
Templeton et al., 2013, Phase 2 trial of single-agent everolimus in chemotherapy-naive patients with castration-resistant prostate cancer (SAKK 08/08)., Eur. Urol.
Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
André et al., 2014, Everolimus for women with trastuzumab-resistant, HER2-positive, advanced breast cancer (BOLERO-3): a randomised, double-blind, placebo-controlled phase 3 trial., Lancet Oncol.
Andre et al., 2010, Phase I study of everolimus plus weekly paclitaxel and trastuzumab in patients with metastatic breast cancer pretreated with trastuzumab., J. Clin. Oncol.
Jerusalem et al., 2011, Phase I trial of oral mTOR inhibitor everolimus in combination with trastuzumab and vinorelbine in pre-treated patients with HER2-overexpressing metastatic breast cancer., Breast Cancer Res. Treat.
Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
Kiessling et al., 2016, Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma., PLoS ONE
Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
Jain P et al., 2017, Overcoming resistance to single-agent therapy for oncogenic <i>BRAF</i> gene fusions <i>via</i> combinatorial targeting of MAPK and PI3K/mTOR signaling pathways., Oncotarget
Hsieh et al., 2017, Genomic Biomarkers of a Randomized Trial Comparing First-line Everolimus and Sunitinib in Patients with Metastatic Renal Cell Carcinoma., Eur. Urol.
Basho et al., 2017, Targeting the PI3K/AKT/mTOR Pathway for the Treatment of Mesenchymal Triple-Negative Breast Cancer: Evidence From a Phase 1 Trial of mTOR Inhibition in Combination With Liposomal Doxorubicin and Bevacizumab., JAMA Oncol
Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.
Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
Iyer et al., 2012, Genome sequencing identifies a basis for everolimus sensitivity., Science
Franz et al., 2013, Efficacy and safety of everolimus for subependymal giant cell astrocytomas associated with tuberous sclerosis complex (EXIST-1): a multicentre, randomised, placebo-controlled phase 3 trial., Lancet
Mo et al., 2016, mTOR Inhibitors Suppress Homologous Recombination Repair and Synergize with PARP Inhibitors via Regulating SUV39H1 in BRCA-Proficient Triple-Negative Breast Cancer., Clin. Cancer Res.
Nakamura M et al., 2013, [A case of metastatic renal cell carcinoma associated with Birt-Hogg-Dubé syndrome treated with molecular-targeting agents]., Hinyokika Kiyo
Goutagny et al., 2015, Phase II study of mTORC1 inhibition by everolimus in neurofibromatosis type 2 patients with growing vestibular schwannomas., J. Neurooncol.
Watkin et al., 1989, Sequential combination chemotherapy and radiotherapy in locally advanced non-small cell carcinoma of the bronchus., Respir Med
Karajannis et al., 2014, Phase II study of everolimus in children and adults with neurofibromatosis type 2 and progressive vestibular schwannomas., Neuro-oncology
Guglielmelli et al., 2011, Safety and efficacy of everolimus, a mTOR inhibitor, as single agent in a phase 1/2 study in patients with myelofibrosis., Blood
Lesche D et al., 2015, Influence of CYP3A5 genetic variation on everolimus maintenance dosing after cardiac transplantation., Clin Transplant
Schoeppler KE et al., 2014, The impact of genetic polymorphisms, diltiazem, and demographic variables on everolimus trough concentrations in lung transplant recipients., Clin Transplant

EVEROLIMUS TSC2

Interaction Score: 6.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25295501 23158522

Sources:
CIViC OncoKB
EVEROLIMUS TSC1

Interaction Score: 4.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22923433 26859683 11010 2015 24622468 23158522

Sources:
CIViC OncoKB
EVEROLIMUS KDM5C

Interaction Score: 1.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27751729

Sources:
CIViC
EVEROLIMUS FLCN

Interaction Score: 1.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23995526

Sources:
CIViC
EVEROLIMUS NF2

Interaction Score: 1.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25567352 2556735 24311643

Sources:
CIViC
EVEROLIMUS BAP1

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27751729

Sources:
CIViC
EVEROLIMUS FKBP1A

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction FK506-binding protein 1A inhibitor

Direct Interaction yes

PMIDs:
24836070

Sources:
DTC ClearityFoundationClinicalTrial ChemblInteractions
EVEROLIMUS GNA11

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AEB071 + Everolimus

Indication/Tumor Type uveal melanoma

Response Type predicted – sensitive

PMIDs:
27507190

Sources:
JAX-CKB
EVEROLIMUS RPTOR

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EVEROLIMUS PBRM1

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27751729

Sources:
CIViC
EVEROLIMUS MTOR

Interaction Score: 0.35

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status case report

PMIDs:
26176165 24836070 24622468 24625776 26859683 11010 2015 25295501 18466433 19344392 20531964 11752352 19774211 20155724 20569080 25893859

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial TEND DoCM CIViC MyCancerGenomeClinicalTrial PharmGKB TTD OncoKB
EVEROLIMUS VHL

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal cell carcinoma

Response Type sensitive

Approval Status Phase I

PMIDs:
26951309

Sources:
JAX-CKB CIViC
EVEROLIMUS MPL

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type myelofibrosis

Response Type sensitive

Approval Status Phase II

PMIDs:
21725052

Sources:
JAX-CKB
EVEROLIMUS STK11

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status case report

Pathway activation

Variant Effect loss-of-function

PMIDs:
21189378 27615706

Sources:
JAX-CKB DoCM
EVEROLIMUS GNAQ

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AEB071 + Everolimus

Indication/Tumor Type uveal melanoma

Response Type predicted – sensitive

PMIDs:
27507190

Sources:
JAX-CKB
EVEROLIMUS PTEN

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
20664172 20664174 22473592 28330462 26951309 22662154 21358673 27091708 23989949 23582881

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC
EVEROLIMUS NOTCH1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Everolimus

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB
EVEROLIMUS RB1

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Everolimus

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB
EVEROLIMUS HRAS

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type predicted – sensitive

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
26544513

Sources:
JAX-CKB CIViC
EVEROLIMUS NRAS

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
23629727 26821351

Sources:
JAX-CKB CIViC
EVEROLIMUS PIK3CA

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
21358673 27091708 27797976 26951309 27893038 22662154 23629727 20664172 20664174

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC
EVEROLIMUS BRAF

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Everolimus + Selumetinib

Indication/Tumor Type malignant glioma

Response Type predicted – sensitive

PMIDs:
20664172 20664174 23629727 27797976 27217440 29156677

Sources:
JAX-CKB CIViC
EVEROLIMUS BRCA2

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Everolimus + Talazoparib

Indication/Tumor Type triple-receptor negative breast cancer

Response Type sensitive

PMIDs:
26546619

Sources:
JAX-CKB
EVEROLIMUS KRAS

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

PMIDs:
23629727 22662154 26725216 20664172 20664174

Sources:
ClearityFoundationBiomarkers JAX-CKB
EVEROLIMUS RET

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Phase II

PMIDs:
27683183 26294908

Sources:
JAX-CKB
EVEROLIMUS AKT2

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
EVEROLIMUS AKT3

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
EVEROLIMUS ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase III

Response Type sensitive

PMIDs:
24742739 20975068 21107682

Sources:
JAX-CKB PharmGKB FDA
EVEROLIMUS FGFR4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EVEROLIMUS ATM

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Vandetanib + Everolimus

Indication/Tumor Type thyroid medullary carcinoma

Response Type predicted – sensitive

PMIDs:
27683183

Sources:
JAX-CKB
EVEROLIMUS PIK3R1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EVEROLIMUS CYP3A5

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26458301 24628014

Sources:
PharmGKB
EVEROLIMUS AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Phase Ib/II

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB MyCancerGenomeClinicalTrial
EVEROLIMUS BRCA1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy Olaparib + Everolimus

Indication/Tumor Type triple-receptor negative breast cancer

PMIDs:
26546619

Sources:
JAX-CKB
EVEROLIMUS ESR2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EVEROLIMUS EGFR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Everolimus + Pimasertib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
23629727

Sources:
JAX-CKB
EVEROLIMUS ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
EVEROLIMUS ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EVEROLIMUS AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

MyCancerGenome: EVEROLIMUS

Version: 20-Jun-2017

Alternate Names:

RAD001 Development Name

EVEROLIMUS Generic Name

AFINITOR Trade Name

Drug Info:

Drug Class Kinase Inhibitors

Notes rapalogue

FDA Approval Pancreatic, gastrointestinal, or lung origin neuroendocrine tumors; Renal cell carcinoma, Subependymal giant cell astrocytoma associated with tuberous sclerosis, Breast cancer (ER+, HER2-)

Publications:

TEND: EVEROLIMUS
- Version: 01-August-2011
Alternate Names:

EVEROLIMUS Primary Drug Name

Drug Info:

Year of Approval 2009

Drug Class immunosuppressive agents

Publications:
TdgClinicalTrial: EVEROLIMUS
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications immunosuppressant

Drug Class Small Molecule

FDA Approval approved

Publications:

DTC: EVEROLIMUS

Version: 02-September-2020

Alternate Names:

CHEMBL1908360 ChEMBL Drug ID

Drug Info:

Publications:

Wong CP et al., 2015, Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway., J Nat Prod

Salomé C et al., 2014, Benzofuran derivatives as anticancer inhibitors of mTOR signaling., Eur J Med Chem

JAX-CKB: Everolimus

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Powles et al., 2016, Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma., J. Clin. Oncol.

Schneider et al., 2015, Beneficial Effects of the mTOR Inhibitor Everolimus in Patients with Advanced Medullary Thyroid Carcinoma: Subgroup Results of a Phase II Trial., Int J Endocrinol

Kato et al., 2017, RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients., Clin. Cancer Res.

DoCM: EVEROLIMUS

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Klümpen et al., 2011, mTOR inhibitor treatment of pancreatic cancer in a patient With Peutz-Jeghers syndrome., J. Clin. Oncol.

Wagle et al., 2014, Activating mTOR mutations in a patient with an extraordinary response on a phase I trial of everolimus and pazopanib., Cancer Discov

Voss et al., 2014, Tumor genetic analyses of patients with metastatic renal cell carcinoma and extended benefit from mTOR inhibitor therapy., Clin. Cancer Res.

PharmGKB: everolimus

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Stjepanovic N et al., 2015, Elucidating the genomic landscape of breast cancer: how will this affect treatment?, Pharmacogenomics

Lesche D et al., 2015, Influence of CYP3A5 genetic variation on everolimus maintenance dosing after cardiac transplantation., Clin Transplant

Schoeppler KE et al., 2014, The impact of genetic polymorphisms, diltiazem, and demographic variables on everolimus trough concentrations in lung transplant recipients., Clin Transplant

CIViC: EVEROLIMUS

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Iyer et al., 2012, Genome sequencing identifies a basis for everolimus sensitivity., Science

Franz et al., 2013, Efficacy and safety of everolimus for subependymal giant cell astrocytomas associated with tuberous sclerosis complex (EXIST-1): a multicentre, randomised, placebo-controlled phase 3 trial., Lancet

Hsieh et al., 2017, Genomic Biomarkers of a Randomized Trial Comparing First-line Everolimus and Sunitinib in Patients with Metastatic Renal Cell Carcinoma., Eur. Urol.

TALC: EVEROLIMUS
- Version: 12-May-2016
Alternate Names:

EVEROLIMUS Primary Drug Name

EVEROLIMUS Drug Generic Name

AFINITOR Drug Trade Name

Drug Info:

Publications:
TTD: Everolimus
- Version: 2020.06.01
Alternate Names:

D0K3QS TTD Drug ID

Drug Info:

Publications:
ChemblInteractions: CHEMBL1908360
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1908360
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Everolimus
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: EVEROLIMUS
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: EVEROLIMUS
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
OncoKB: Everolimus
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: EVEROLIMUS
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	FK506-binding protein 1A inhibitor
Direct Interaction	yes

combination therapy	AEB071 + Everolimus
Indication/Tumor Type	uveal melanoma
Response Type	predicted – sensitive

Variant Effect	gain-of-function
Pathway	activation
Clinical Status	case report

Indication/Tumor Type	renal cell carcinoma
Response Type	sensitive
Approval Status	Phase I

Indication/Tumor Type	myelofibrosis
Response Type	sensitive
Approval Status	Phase II

Indication/Tumor Type	breast cancer
Response Type	sensitive
Approval Status	Preclinical - Cell culture

combination therapy	Ribociclib + Everolimus
Indication/Tumor Type	T-cell adult acute lymphocytic leukemia
Response Type	sensitive

Indication/Tumor Type	urinary bladder cancer
Response Type	predicted – sensitive
Indication/Tumor Type	Advanced Solid Tumor

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

combination therapy	Everolimus + Selumetinib
Indication/Tumor Type	malignant glioma
Response Type	predicted – sensitive

combination therapy	Everolimus + Talazoparib
Indication/Tumor Type	triple-receptor negative breast cancer
Response Type	sensitive

Indication/Tumor Type	thyroid medullary carcinoma
Response Type	sensitive
Approval Status	Phase II

combination therapy	Vandetanib + Everolimus
Indication/Tumor Type	thyroid medullary carcinoma
Response Type	predicted – sensitive

combination therapy	Everolimus + Pimasertib
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

RAD001	Development Name
EVEROLIMUS	Generic Name
AFINITOR	Trade Name

EVEROLIMUS	Primary Drug Name
EVEROLIMUS	Drug Generic Name
AFINITOR	Drug Trade Name

EVEROLIMUS Drug Record

EVEROLIMUS chembl:CHEMBL1908360 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25295501 23158522

Sources: CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22923433 26859683 11010 2015 24622468 23158522

Sources: CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27751729

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23995526

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25567352 2556735 24311643

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27751729

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction FK506-binding protein 1A inhibitor Direct Interaction yes

PMIDs: 24836070

Sources: DTC ClearityFoundationClinicalTrial ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: combination therapy AEB071 + Everolimus Indication/Tumor Type uveal melanoma Response Type predicted – sensitive

PMIDs: 27507190

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27751729

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Variant Effect gain-of-function Pathway activation Clinical Status case report

PMIDs: 26176165 24836070 24622468 24625776 26859683 11010 2015 25295501 18466433 19344392 20531964 11752352 19774211 20155724 20569080 25893859

Sources: TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial TEND DoCM CIViC MyCancerGenomeClinicalTrial PharmGKB TTD OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type renal cell carcinoma Response Type sensitive Approval Status Phase I

PMIDs: 26951309

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type myelofibrosis Response Type sensitive Approval Status Phase II

PMIDs: 21725052

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Clinical Status case report Pathway activation Variant Effect loss-of-function

PMIDs: 21189378 27615706

Sources: JAX-CKB DoCM

Interaction Types & Directionality: n/a

Interaction Info: combination therapy AEB071 + Everolimus Indication/Tumor Type uveal melanoma Response Type predicted – sensitive

PMIDs: 27507190

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast cancer Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 20664172 20664174 22473592 28330462 26951309 22662154 21358673 27091708 23989949 23582881

Sources: ClearityFoundationBiomarkers JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ribociclib + Everolimus Indication/Tumor Type T-cell adult acute lymphocytic leukemia Response Type sensitive

PMIDs: 28151717

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ribociclib + Everolimus Indication/Tumor Type T-cell adult acute lymphocytic leukemia Response Type sensitive

PMIDs: 28151717

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type urinary bladder cancer Response Type predicted – sensitive Indication/Tumor Type Advanced Solid Tumor

PMIDs: 26544513

Interaction Types & Directionality:

n/a

PMIDs:
25295501 23158522

Sources:
CIViC OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
22923433 26859683 11010 2015 24622468 23158522

Sources:
CIViC OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
27751729

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
23995526

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
25567352 2556735 24311643

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
27751729

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction FK506-binding protein 1A inhibitor

Direct Interaction yes

PMIDs:
24836070

Sources:
DTC ClearityFoundationClinicalTrial ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AEB071 + Everolimus

Indication/Tumor Type uveal melanoma

Response Type predicted – sensitive

PMIDs:
27507190

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27751729

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status case report

PMIDs:
26176165 24836070 24622468 24625776 26859683 11010 2015 25295501 18466433 19344392 20531964 11752352 19774211 20155724 20569080 25893859

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial TEND DoCM CIViC MyCancerGenomeClinicalTrial PharmGKB TTD OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal cell carcinoma

Response Type sensitive

Approval Status Phase I

PMIDs:
26951309

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type myelofibrosis

Response Type sensitive

Approval Status Phase II

PMIDs:
21725052

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status case report

Pathway activation

Variant Effect loss-of-function

PMIDs:
21189378 27615706

Sources:
JAX-CKB DoCM

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AEB071 + Everolimus

Indication/Tumor Type uveal melanoma

Response Type predicted – sensitive

PMIDs:
27507190

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
20664172 20664174 22473592 28330462 26951309 22662154 21358673 27091708 23989949 23582881

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Everolimus

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Everolimus

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type predicted – sensitive

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
26544513

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
23629727 26821351

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
21358673 27091708 27797976 26951309 27893038 22662154 23629727 20664172 20664174

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Everolimus + Selumetinib

Indication/Tumor Type malignant glioma

Response Type predicted – sensitive

PMIDs:
20664172 20664174 23629727 27797976 27217440 29156677

Sources:
JAX-CKB CIViC