Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM8X2EH)

Drug Name
Everolimus Drug Info
Synonyms
Afinitor; Afinitor (TN); CERTICAN(R); Certican; Certican (TN); Everolimus (JAN/USAN/INN); Everolimus [USAN]; MTOR kinase inhibitors; NVP-RAD-001; RAD 001; RAD-001; RAD-001C; RAD001; RAD001, SDZ-RAD, Certican, Zortress, Afinitor, Everolimus; SDZ-RAD; Zortress
Indication
Disease Entry ICD 11 Status REF
Advanced cancer 2A00-2F9Z Approved [1]
Advanced/metastatic breast cancer 2C60 Approved [2]
Brainstem neoplasm Approved [1]
Breast carcinoma Approved [1]
Graft-versus-host disease 4B24 Approved [1]
Intracranial meningioma Approved [1]
Leukemia Approved [1]
Lung cancer 2C25.0 Approved [1]
Mucosal melanoma Approved [1]
Multiple sclerosis 8A40 Approved [1]
Plasma cell myeloma 2A83.1 Approved [1]
Prostate cancer 2C82.0 Approved [1]
Renal cell carcinoma 2C90 Approved [3]
Salivary gland squamous cell carcinoma Approved [1]
Tuberous sclerosis LD2D.2 Approved [1]
Kidney cancer 2C90.0 Phase 3 [3]
Castration-resistant prostate carcinoma Investigative [1]
Colon cancer 2B90.Z Investigative [1]
Middle East Respiratory Syndrome (MERS) 1D64 Investigative [4]
Neuroblastoma 2D11.2 Investigative [1]
Pancreatic acinar cell carcinoma Investigative [1]
Polycystic kidney disease GB8Y Investigative [1]
Severe acute respiratory syndrome (SARS) 1D65 Investigative [4]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
6442177
ChEBI ID
CHEBI:68478
CAS Number
CAS 159351-69-6
TTD Drug ID
DM8X2EH
VARIDT Drug ID
DR00224
INTEDE Drug ID
DR0674
ACDINA Drug ID
D00260

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Serine/threonine-protein kinase mTOR (mTOR) TTCJG29 MTOR_HUMAN Inhibitor [5]
HUMAN mammalian target of rapamycin (mTOR) TT7HQAF MTOR_HUMAN Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [7]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Serine/threonine-protein kinase mTOR (mTOR) DTT MTOR 5.425 4.35 5.106 5.188
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Advanced cancer
ICD Disease Classification 2A00-2F9Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Serine/threonine-protein kinase mTOR (mTOR) DTT MTOR 2.16E-05 -0.44 -2.3
P-glycoprotein 1 (ABCB1) DTP P-GP 2.04E-02 -1.13E+00 -1.00E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 5.84E-01 -1.61E-01 -3.61E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Everolimus FDA Label
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 URL: 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).
4 Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.
5 Mammalian 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.
6 Closer to the Site of Action: Everolimus Concentrations in Peripheral Blood Mononuclear Cells Correlate Well With Whole Blood Concentrations. Ther Drug Monit. 2015 Oct;37(5):675-80.
7 The evolving experience using everolimus in clinical transplantation. Transplant Proc. 2004 Mar;36(2 Suppl):495S-499S.