Everolimus

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

2009

www.ebi.ac.uk

First approval year: 2009
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Everolimus
www.ebi.ac.uk

Molecular weight: 958.24
www.ebi.ac.uk

Structure (SMILES): CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](OCCO)[C@H](OC)C2)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/1C
www.ebi.ac.uk

afinitor
Afinitor
afinitor disperz
Afinitor disperz
certican
Certican
votubia
Votubia
zortress
Zortress

40 o 2 hydroxyethyl rapamycin
40-o-(2-hydroxyethyl)-rapamycin
42 o 2 hydroxyethyl rapamycin
42-o-(2-hydroxyethyl)rapamycin
afinitor
Afinitor
Afinitor (everolimus)
Certican
Certican®
Drug: Everolimus
everolimus
Everolimus
EVEROLIMUS
Everolimus (10 mg QD)
Everolimus (Afinitor) tablets
Everolimus (Afinitor®)
Everolimus (Certican)
Everolimus (EVR)
Everolimus (RAD 001)
everolimus (RAD)
everolimus (RAD001)
Everolimus (RAD001)
Everolimus (reduced tacrolimus)
Everolimus (tacrolimus elimination)
EVEROLIMUS [EMA EPAR]

And 56 more, listed on the interactive page.

CAS registry numbers

159351-69-6

ChEMBL ID: CHEMBL1908360
www.ebi.ac.uk

InChIKey: HKVAMNSJSFKALM-GKUWKFKPSA-N
www.ebi.ac.uk

PubChem compound IDs

6442177

RxNorm IDs (RxCUI)

141704

FDA ingredient codes (UNII)

9HW64Q8G6G

L01EG02
L01XE10
L04AH02

Sources for recorded values

www.ebi.ac.uk

Applicant: NOVARTIS
Approval date: 30 Mar 2009
Application number: NDA022334

Status: Authorised
Status date: 2 Aug 2009
Authorisation date: 2 Aug 2009
Approved indications: Hormone-receptor-positive advanced breast cancer Afinitor is indicated for the treatment of hormone-receptor-positive, HER2/neu-negative advanced breast cancer, in combination with exemestane, in post-menopausal women without symptomatic visceral disease after recurrence or progression following a non-steroidal aromatase inhibitor. Neuroendocrine tumours of pancreatic origin Afinitor is indicated for the treatment of unresectable or metastatic, well or moderately differentiated neuroendocrine tumours of pancreatic origin in adults with progressive disease. Neuroendocrine tumours of gastrointestinal or lung origin Afinitor is indicated for the treatment of unresectable or metastatic, well-differentiated (Grade 1 or Grade 2) non-functional neuroendocrine tumours of gastrointestinal or lung origin in adults with progressive disease. Renal-cell carcinoma Afinitor is indicated for the treatment of patients with advanced renal-cell carcinoma, whose disease has progressed on or after treatment with VEGF-targeted therapy.
Product number: EMEA/H/C/001038
Authorisation holder: Novartis Europharm Limited
Priority medicines scheme: No
Generic: No
Biosimilar: No
Generic medicines: 0
Biosimilar medicines: 0
Advanced therapy: No
Conditional approval: No
Additional monitoring: No
Accelerated assessment: No
Exceptional circumstances: No

Therapeutic areas

Breast Neoplasms
Carcinoma, Renal Cell
Pancreatic Neoplasms

European medicines record

www.ema.europa.eu

Patents: 3
Designations: 3
Earliest recorded loss of exclusivity: 1 Jul 2028
First in class: No
Fast track: No
Breakthrough designation: No
Orphan designation: No
Priority review: Yes
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only
Boxed warning: Yes

Pharmacology name: everolimus
Type: Synthetic organic
Drug name stem: -imus
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral

Action
Inhibition
Action type
Inhibitor
Target
mechanistic target of rapamycin kinase
Gene symbol
MTOR
Protein identifier
P42345
Median affinity
8.7
Affinity units
pIC50
Primary target
Yes
Mechanism
FK506-binding protein 1A inhibitor
Action type
Inhibitor
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A
Protein identifier
P62942

Open Targets mechanisms

Mechanism
FK506-binding protein 1A inhibitor
Action type
Inhibitor
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A

Action type
Inhibitor
Gene symbol
MTOR
Protein identifier
P42345
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FKBP1A
Protein identifier
P62942
Organism
Homo sapiens
Target development level
Clinical

Condition
Carcinoma, Squamous Cell
Highest recorded phase
2
Condition identifier
EFO:0000181
Subject identifier
D002294
Condition
Carcinoma, Hepatocellular
Highest recorded phase
2
Condition identifier
EFO:0000182
Subject identifier
D006528
Condition
Hodgkin Disease
Highest recorded phase
2
Condition identifier
EFO:0000183
Subject identifier
D006689
Condition
Myelodysplastic Syndromes
Highest recorded phase
2
Condition identifier
EFO:0000198
Subject identifier
D009190
Condition
Neoplasms, Plasma Cell
Highest recorded phase
1
Condition identifier
EFO:0000200
Subject identifier
D054219
Condition
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Highest recorded phase
1
Condition identifier
EFO:0000220
Subject identifier
D054198
Condition
Leukemia, Myeloid, Acute
Highest recorded phase
2
Condition identifier
EFO:0000222
Subject identifier
D015470
Condition
Adenocarcinoma
Highest recorded phase
1
Condition identifier
EFO:0000228
Subject identifier
D000230
Condition
Carcinoma, Adenoid Cystic
Highest recorded phase
2
Condition identifier
EFO:0000231
Subject identifier
D003528
Condition
Astrocytoma
Highest recorded phase
4
Condition identifier
EFO:0000272
Subject identifier
D001254
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0000305
Subject identifier
D001943
Condition
Carcinoma
Highest recorded phase
3
Condition identifier
EFO:0000313
Subject identifier
D002277
Condition
Glioma
Highest recorded phase
2
Condition identifier
EFO:0000326
Subject identifier
D005910
Condition
Chondrosarcoma
Highest recorded phase
2
Condition identifier
EFO:0000333
Subject identifier
D002813
Condition
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Highest recorded phase
1
Condition identifier
EFO:0000339
Subject identifier
D015464
Condition
Carcinoma, Renal Cell
Highest recorded phase
4
Condition identifier
EFO:0000349
Subject identifier
D002292
Condition
Colorectal Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0000365
Subject identifier
D015179
Condition
Melanoma
Highest recorded phase
2
Condition identifier
EFO:0000389
Subject identifier
D008545
Condition
Lymphoma, Large B-Cell, Diffuse
Highest recorded phase
3
Condition identifier
EFO:0000403
Subject identifier
D016403
Condition
Epilepsy
Highest recorded phase
2
Condition identifier
EFO:0000474
Subject identifier
D004827
Condition
Neoplasms, Germ Cell and Embryonal
Highest recorded phase
2
Condition identifier
EFO:0000514
Subject identifier
D009373
Condition
Glioblastoma
Highest recorded phase
2
Condition identifier
EFO:0000519
Subject identifier
D005909
Condition
Infections
Highest recorded phase
3
Condition identifier
EFO:0000544
Subject identifier
D007239
Condition
Sarcoma, Kaposi
Highest recorded phase
2
Condition identifier
EFO:0000558
Subject identifier
D012514
Condition
Leukemia
Highest recorded phase
1
Condition identifier
EFO:0000565
Subject identifier
D007938

And 122 more, listed on the interactive page.

Condition identifier
EFO_0000181
Highest recorded phase
2
Condition identifier
EFO_0000182
Highest recorded phase
2
Condition identifier
EFO_0000183
Highest recorded phase
2
Condition identifier
EFO_0000198
Highest recorded phase
2
Condition identifier
EFO_0000200
Highest recorded phase
2
Condition identifier
EFO_0000222
Condition identifier
EFO_0000228
Highest recorded phase
2
Condition identifier
EFO_0000231
Highest recorded phase
2
Condition identifier
EFO_0000272
Condition identifier
EFO_0000305
Condition identifier
EFO_0000313
Highest recorded phase
3
Condition identifier
EFO_0000333
Highest recorded phase
2
Condition identifier
EFO_0000365
Highest recorded phase
2
Condition identifier
EFO_0000389
Highest recorded phase
2
Condition identifier
EFO_0000403
Highest recorded phase
3
Condition identifier
EFO_0000474
Highest recorded phase
2
Condition identifier
EFO_0000514
Highest recorded phase
2
Condition identifier
EFO_0000519
Highest recorded phase
2
Condition identifier
EFO_0000544
Highest recorded phase
3
Condition identifier
EFO_0000558
Highest recorded phase
2
Condition identifier
EFO_0000574
Highest recorded phase
2
Condition identifier
EFO_0000588
Highest recorded phase
2
Condition identifier
EFO_0000612
Condition identifier
EFO_0000616
Condition identifier
EFO_0000637
Highest recorded phase
2

And 268 more, listed on the interactive page.

Warning
Black Box Warning
Effect
carcinogenicity
Warning
Black Box Warning
Effect
cardiotoxicity
Warning
Black Box Warning
Effect
immune system toxicity
Warning
Black Box Warning
Effect
infectious disease
Warning
Black Box Warning
Effect
musculoskeletal toxicity
Warning
Black Box Warning
Effect
nephrotoxicity
Warning
Black Box Warning
Effect
neurotoxicity
Warning
Black Box Warning
Effect
vascular toxicity

Warning
Black Box Warning
Effect
carcinogenicity
Country
United States
Warning
Black Box Warning
Effect
cardiotoxicity
Country
United States
Warning
Black Box Warning
Effect
immune system toxicity
Country
United States
Warning
Black Box Warning
Effect
infectious disease
Country
United States
Warning
Black Box Warning
Effect
musculoskeletal toxicity
Country
United States
Warning
Black Box Warning
Effect
nephrotoxicity
Country
United States
Warning
Black Box Warning
Effect
neurotoxicity
Country
United States
Warning
Black Box Warning
Effect
vascular toxicity
Country
United States

Event
bk virus infection
Reports
205
Reporting signal score
520.43
Event
blood creatinine increased
Reports
586
Reporting signal score
498.759
Event
breast cancer metastatic
Reports
282
Reporting signal score
680.603
Event
cough
Reports
977
Reporting signal score
446.301
Event
decreased appetite
Reports
884
Reporting signal score
525.153
Event
diarrhoea
Reports
1,838
Reporting signal score
509.398
Event
disease progression
Reports
602
Reporting signal score
391.538
Event
fatigue
Reports
1,567
Reporting signal score
392.898
Event
hyperglycaemia
Reports
399
Reporting signal score
436.205
Event
interstitial lung disease
Reports
508
Reporting signal score
491.882
Event
kidney transplant rejection
Reports
234
Reporting signal score
524.944
Event
lung disorder
Reports
333
Reporting signal score
324.496
Event
malignant neoplasm progression
Reports
1,440
Reporting signal score
2,515.76
Event
metastases to bone
Reports
440
Reporting signal score
919.502
Event
metastases to liver
Reports
451
Reporting signal score
961.144
Event
metastases to lung
Reports
230
Reporting signal score
430.64
Event
mouth ulceration
Reports
286
Reporting signal score
330.337
Event
mucosal inflammation
Reports
437
Reporting signal score
539.961
Event
neoplasm progression
Reports
410
Reporting signal score
576.723
Event
oedema peripheral
Reports
586
Reporting signal score
319.916
Event
oral pain
Reports
241
Reporting signal score
302.551
Event
pleural effusion
Reports
497
Reporting signal score
408.236
Event
pneumonitis
Reports
657
Reporting signal score
1,172.71
Event
polyomavirus-associated nephropathy
Reports
170
Reporting signal score
424.288
Event
post transplant lymphoproliferative disorder
Reports
165
Reporting signal score
322.063

And 5 more, listed on the interactive page.

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And 451 more, listed on the interactive page.

Dose: 10 mg
Route: Oral
How often: Once daily

Hydrogen bond acceptors: 14
Hydrogen bond donors: 3
Polar surface area: 204.66
Calculated partition coefficient (ALogP): 6.2
Calculated partition coefficient (XLogP): 5.9
Prodrug: No
Chirality: Single enantiomer
Inorganic: No
Rule-of-five violations: 3
Rotatable bonds: 9
Heavy atoms: 68
Molecular formula: C53H83NO14
Monoisotopic mass: 957.58135632
Natural product: Yes

0054-0470
0054-0471
0054-0472
0054-0480
0054-0481
0054-0482
0054-0497
0054-0604
0078-0414
0078-0415
0078-0417
0078-0422
0078-0566
0078-0567
0078-0594
0078-0620
0078-0626
0078-0627
0078-0628
0093-7766
0093-7767
0093-7768
0093-7769
0245-0822
0245-0823

And 59 more, listed on the interactive page.

Recorded assays: 726
Active assays: 121

Confirmatory
Other
Summary

MTOR Inhibitors
id.nlm.nih.gov
Immunosuppressive Agents
id.nlm.nih.gov

Oral bioavailability

Median: 20
Mean: 20
Minimum: 20
Maximum: 20
Unit: %
Assays: 1
Standard deviation: 0
Summary method: median
Censored results excluded: 0
Other units excluded: 0
Unknown units excluded: 0

Measurement types

Related records

Trials (785)

10-Years Follow-up of the EXAMINATION Trial
12 Month Athena Study: Everolimus vs. Standard Regimen in de Novo Kidney Transplant Patients
24 Months Follow-up, Two Arm Study to Compare the Cardiovascular Profile in a Regimen With Everolimus + Mycophenolic Acid (MPA) Versus (vs.) a Regimen of CNI+MPA in Maintenance Renal Transplant Recipients
3-arm Trial to Evaluate Pasireotide LAR/Everolimus Alone/in Combination in Patients With Lung/Thymus NET - LUNA Trial
4EVER - Efficacy, Safety, Health Economics, Translational Research of Postmenopausal Women With Estrogen Receptor Positive Locally Advanced or Metastatic Breast Cancer
89Zr-bevacizumab PET Imaging in Patients With Neuroendocrine Tumors
A Biological Prospective Study in Patients With Metastatic Pancreatic NETs Treated With Everolimus
A Clinical Evaluation of Everolimus Eluting Coronary Stents in the Treatment of Patients With ST-segment Elevation Myocardial Infarction: EXAMINATION Study
A Clinical Trial to Assess the Efficacy and Safety of the Conversion to Everolimus
A Comparison of Vorolanib Tablets Combined With Everolimus Versus Sunitinib in Patients With Advanced Renal Cell Carcinoma Who Have Progressed After Treatment With Immunotherapy Monotherapy or in Combination With TKI
A Facilitated Access Program to Provide Everolimus (RAD) Maintenance for Patients Completing Therapy in RAD Trials in Solid Organ Transplantation
A MolEcularly Guided Anti-Cancer Drug Off-Label Trial
A Multiple Ascending Dose Study of the mTOR Inhibitor (RAD001) in Combination With R1507 in Patients With Advanced Solid Tumors
A National Multi-center Randomized, Open Label Study to Evaluate Efficacy and Safety of Everolimus With EC-MPS Compared to Standard Treatment Combination Tacrolimus and EC-MPS in de Novo Liver Transplant Recipients
A Phase 0/I Study of Ribociclib (LEE011) in Combination With Everolimus in Preoperative Recurrent High-Grade Glioma Patients Scheduled for Resection
A Phase 1 Study Investigating the Combination of RAD001, Cetuximab and Irinotecan as Second-line Therapy After FOLFOX (or XELOX) Plus Bevacizumab in Patients With Metastatic Colorectal Cancer
A Phase 1b Study of SGN-75 in Combination With Everolimus in Patients With Renal Cell Carcinoma
A Phase 3 Study of HRS-8080 Versus Treatment Chosen by Physicians in Locally Advanced and Metastatic Breast Cancer
A Phase I Study of BKM120 and Everolimus in Advanced Solid Malignancies
A Phase Ib Study of Rad001 and Sutent to Treat Renal Cell Carcinoma

Approved for (19)

Anaplastic astrocytoma
Angiomyolipoma
Astrocytoma (excluding glioblastoma)
Breast cancer
Breast carcinoma
Breast neoplasm
Cancer
Clear cell renal carcinoma
Exocrine pancreatic carcinoma
Hamartoma
Lung neuroendocrine neoplasm
Neoplasm
Neuroendocrine neoplasm
Pancreatic neoplasm
Pancreatic neuroendocrine tumor
Renal cell adenocarcinoma
Renal cell carcinoma
Subependymal giant cell astrocytoma
Tuberous sclerosis

In development for (123)

Acute coronary syndrome Phase 1
Acute lymphoblastic leukemia Phase 1
Acute myeloid leukemia Phase 2
Adenocarcinoma Phase 1
Adenoid cystic carcinoma Phase 2
Adult oligodendroglioma Phase 2
Age-related macular degeneration Phase 2
Autosomal dominant polycystic kidney disease Phase 3
Bile duct carcinoma Phase 2
Bone sarcoma Phase 2
Brain neoplasm Phase 2
Carcinoid syndrome Phase 3
Carcinoid tumor Phase 3
Carcinoma Phase 3
Carcinoma of esophagus Phase 1
Central nervous system cancer Phase 2
Central nervous system neoplasm Phase 1
Cervical cancer Phase 1
Childhood ependymoma Phase 2
Cholangiocarcinoma Phase 2

Targets (1)

FKBP1A FK506-binding protein 1A inhibitor

Everolimus

Development status

Names and chemistry

Brand names (10)

Other names (81)

Identifiers

ATC classification codes (3)

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (2)

Open Targets mechanisms

DrugCentral mechanisms (2)

Investigated indications (147)

Open Targets indications (293)

Warnings (8)

Open Targets warnings (8)

Reported adverse events (30)

Trial references (476)

Dosing

Chemical properties

National Drug Codes

Evidence counts

Active assay types (3)

Pharmacologic actions

Biological measurements

Observed measurements

Oral bioavailability

Measurement types

Related records

Trials (785)

Approved for (19)

In development for (123)

Other linked conditions (4)

Targets (1)