General
Preferred name
EVEROLIMUS
Synonyms
RAD001, Afinitor, Zortress, Everolimus, Afinitor Disperz ()
Certican ()
RAD001 ()
SDZ-RAD ()
EverolimusAfinitor ()
Afinitor Disperz ()
RAD-001 ()
RAD-666 ()
Votubia ()
Sdz rad ()
Rapamycin, 42-o-(2-hydroxyethyl)- ()
40-o-(2-hydroxyethyl)-rapamycin ()
Afinitor ()
RAD 666 ()
42-o-(2-hydroxyethyl)rapamycin ()
Zortress ()
P&D ID
PD004083
CAS
159351-69-6
Tags
available
probe
drug
Approved by
FDA
PMDA
EMA
First approval
2009
Drug indication
Acute coronary syndrome
Middle East Respiratory Syndrome (MERS)
Diffuse large B-cell lymphoma
Advanced kidney cancer
Kidney cancer
Severe acute respiratory syndrome (SARS)
Renal cell carcinoma
Drug Status
approved
Max Phase
4.0
Probe info
Probe type
P&D approved
calculated probe
Probe selectivity
protein-selective
Probe sources
High-quality chemical probes
Probe Miner (suitable probes)
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Everolimus is a Type-3 kinase inhibitor and was first approved by the FDA in 2009. There is some ambiguity in the literature as to the exact stereochemistry of everolimus. The structure shown here matches that in the Pubchem entry linked to above. Other common representations include CID 46930999, CID 70789204 and CID 16211121.
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.
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.
DESCRIPTION Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].
DESCRIPTION Everolimus is a Type-3 kinase inhibitor and it was first approved by the FDA in 2009. There is some ambiguity in the literature as to the exact stereochemistry of everolimus. The structure shown here matches that in the Pubchem entry listed in the Database Links table. Other common representations include CID 46930999, CID 70789204 and CID 16211121. (GtoPdb)
DESCRIPTION Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12. Everolimus is a derivative of Rapamycin. It is currently used as an immunosuppressant to prevent rejection of organ transplants. (Enamine Bioactive Compounds)
DESCRIPTION Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors. (TargetMol Bioactive Compound Library)
DESCRIPTION Irreversible TrxR inhibitor (Tocris Bioactive Compound Library)
Cell lines
9
Organisms
0
Compound Sets
29
Cayman Chemical Bioactives
11597
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL1908360
ChEMBL Drugs
CHEMBL1908360
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5889
Concise Guide to Pharmacology 2019/20
5889
Concise Guide to Pharmacology 2021/22
5889
Concise Guide to Pharmacology 2023/24
5889
Drug Repurposing Hub
DrugBank
DB01590
DrugBank Approved Drugs
DB01590
DrugCentral
1118
DrugCentral Approved Drugs
1118
DrugMAP
DM8X2EH
DM17TYR
DrugMAP Approved Drugs
DM8X2EH
Enamine Bioactive Compounds
EBC-11277
Guide to Pharmacology
5889
High-quality chemical probes
PD004083
MedChem Express Bioactive Compound Library
HY-10218
NCATS Inxight Approved Drugs
9HW64Q8G6G
NIH Approved Oncology Drugs
48430111
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Probe Miner (suitable probes)
P42345/1012475
ReFrame library
TargetMol Bioactive Compound Library
T1784
Tocris Bioactive Compound Library
6188
VGSC-DB
NA0198
NA0197
External IDs
39
Properties
(calculated by RDKit )
Molecular Weight
957.58
Hydrogen Bond Acceptors
14
Hydrogen Bond Donors
3
Rotatable Bonds
9
Ring Count
4
Aromatic Ring Count
0
cLogP
6.2
TPSA
204.66
Fraction CSP3
0.75
Chiral centers
15.0
Largest ring
29.0
QED
0.13
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
MTOR
MOA
non-specific serine-threonine protein kinase inhibitor
Inhibitor
Inhibitors of Signal Transduction Pathways
Mammalian Target of Rapamycin (mTOR
FRAP1) Inhibitors
Rotamase (FKBP12) Inhibitors
Angiogenesis Inhibitors
mTOR inhibitor
Target
FK506-binding protein 1A
Bacterial
FKBP
mTOR (FKBP12)
Pathway
Apoptosis
Autophagy
PI3K/Akt/mTOR signaling
Anti-infection
Cell Cycle/DNA Damage
Immunology/Inflammation
PI3K/Akt/mTOR
Primary Target
mTOR
Member status
member
Disease Area
oncology, neurology/psychiatry, genetics, urology
Indication
breast cancer, neuroendocrine tumors of pancreatic origin (PNET), renal cell carcinoma (RCC), subependymal giant cell astrocytoma (SEGA), tuberous sclerosis complex (TSC), renal angiomyolipoma
Therapeutic Class
Anticancer Agents
Antiviral Agents
VGSC Target
Nav1.5
Source data