Drug Information

Drug General Information
Drug ID
D0K3QS
Former ID
DAP001223
Drug Name
Everolimus
Synonyms
Afinitor; Certican; Zortress; Everolimus [USAN]; RAD 001; RAD001; Afinitor (TN); CERTICAN(R); Certican (TN); RAD-001; RAD-001C; SDZ-RAD; NVP-RAD-001; Everolimus (JAN/USAN/INN); RAD001, SDZ-RAD, Certican, Zortress, Afinitor, Everolimus; (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34as)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-9,27-dihydroxy-3-((1R)-2-((1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl)-1-methylethyl)-10,21-dimethoxy-6,8,12,14,20,26-hexamethy; 40-O-(2-hydroxyethyl)-rapamycin; 42-O-(2-Hydroxyethyl)rapamycin; MTOR kinase inhibitors
Drug Type
Small molecular drug
Indication Renal cancer [ICD9: 140-229, 189; ICD10:C64] Approved [530677], [541186]
Advanced kidney cancer [ICD9: 189; ICD10:C64] Phase 3 [530677], [541186]
Therapeutic Class
Anticancer Agents
Company
Novartis
Structure
Download
2D MOL

3D MOL
Formula
C53H83NO14
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
InChIKey
HKVAMNSJSFKALM-GKUWKFKPSA-N
CAS Number
CAS 159351-69-6
PubChem Compound ID
6442177
PubChem Substance ID
12014881, 14767667, 14865574, 50044230, 50112765, 56311446, 56312241, 56312580, 56313164, 91613187, 104178966, 134338463, 135156085, 136340120, 136929859, 137140572, 139754909, 143493384, 144206063, 151990396, 152236848, 152258132, 160645716, 160646971, 162189189, 174527790, 175265707, 177748738, 179150022, 203355779, 226396389
SuperDrug ATC ID
L01XE10; L04AA18
SuperDrug CAS ID
cas=159351696
Drug Resistance Mutation (DRM)
DRM DRM Info
Target and Pathway
Target(s) Serine/threonine-protein kinase mTOR Target Info Inhibitor [537621]
KEGG Pathway ErbB signaling pathway
HIF-1 signaling pathway
mTOR signaling pathway
PI3K-Akt signaling pathway
AMPK signaling pathway
Insulin signaling pathway
Thyroid hormone signaling pathway
Adipocytokine signaling pathway
Type II diabetes mellitus
Pathways in cancer
Proteoglycans in cancer
MicroRNAs in cancer
Glioma
Prostate cancer
Acute myeloid leukemia
Central carbon metabolism in cancer
Choline metabolism in cancer
PANTHER Pathway Hypoxia response via HIF activation
Interleukin signaling pathway
Pathway Interaction Database IL4-mediated signaling events
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
IL12-mediated signaling events
CDC42 signaling events
LKB1 signaling events
Regulation of Telomerase
mTOR signaling pathway
CXCR4-mediated signaling events
EGFR-dependent Endothelin signaling events
IL2 signaling events mediated by PI3K
IFN-gamma pathway
ErbB1 downstream signaling
ErbB2/ErbB3 signaling events
CXCR3-mediated signaling events
Class I PI3K signaling events mediated by Akt
PathWhiz Pathway Leucine Stimulation on Insulin Signaling
Reactome PIP3 activates AKT signaling
Macroautophagy
mTORC1-mediated signalling
HSF1-dependent transactivation
CD28 dependent PI3K/Akt signaling
VEGFR2 mediated vascular permeability
TP53 Regulates Metabolic Genes
Constitutive Signaling by AKT1 E17K in Cancer
WikiPathways ErbB Signaling Pathway
Senescence and Autophagy in Cancer
Interferon type I signaling pathways
Insulin Signaling
EGF/EGFR Signaling Pathway
Wnt Signaling Pathway Netpath
Extracellular vesicle-mediated signaling in recipient cells
Cardiac Hypertrophic Response
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
PIP3 activates AKT signaling
Polycystic Kidney Disease Pathway
Alpha 6 Beta 4 signaling pathway
BDNF signaling pathway
Oncostatin M Signaling Pathway
Prostate Cancer
TSLP Signaling Pathway
FSH signaling pathway
Leptin signaling pathway
TSH signaling pathway
RANKL/RANK Signaling Pathway
SREBF and miR33 in cholesterol and lipid homeostasis
Integrated Breast Cancer Pathway
SREBP signalling
Signaling by Insulin receptor
Costimulation by the CD28 family
Type II diabetes mellitus
MicroRNAs in cardiomyocyte hypertrophy
TOR Signaling
AMPK Signaling
References
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 541186(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5889).
Ref 537621Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9.

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