Details of the Drug
General Information of Drug (ID: DM8X2EH)
Drug Name |
Everolimus
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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
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Indication |
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Therapeutic Class |
Anticancer Agents
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Drug Type |
Small molecular drug
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Structure | ||||||||||||||||||||||||
3D MOL | 2D MOL | |||||||||||||||||||||||
#Ro5 Violations (Lipinski): 3 | Molecular Weight (mw) | 958.2 | ||||||||||||||||||||||
Topological Polar Surface Area (xlogp) | 5.9 | |||||||||||||||||||||||
Rotatable Bond Count (rotbonds) | 9 | |||||||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 3 | |||||||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 14 | |||||||||||||||||||||||
ADMET Property |
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Chemical Identifiers |
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Cross-matching ID | ||||||||||||||||||||||||
Molecular Interaction Atlas of This Drug
Drug Therapeutic Target (DTT) |
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Drug Transporter (DTP) |
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Drug-Metabolizing Enzyme (DME) |
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Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||
Molecular Expression Atlas of This Drug
The Studied Disease | Renal cell carcinoma | |||||||||||||||||||||||||||||||||||
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ICD Disease Classification | 2C90 | |||||||||||||||||||||||||||||||||||
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Molecular Expression Atlas (MEA) | ||||||||||||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Disease Different from Everolimus (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
References
1 | 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). | ||||
---|---|---|---|---|---|
2 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | ||||
3 | BDDCS applied to over 900 drugs | ||||
4 | Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose | ||||
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. | ||||
8 | Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65. | ||||
9 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
10 | Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75. | ||||
11 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
12 | Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772. | ||||
13 | Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98. | ||||
14 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
15 | The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76. | ||||
16 | Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. | ||||
17 | Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007. | ||||
18 | MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. | ||||
19 | Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64. | ||||
20 | Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31. | ||||
21 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. | ||||
22 | Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. | ||||
23 | Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50. | ||||
24 | Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | ||||
25 | Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20. | ||||
26 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
27 | 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. (Target id: 2109). | ||||
28 | Natural products to drugs: natural product-derived compounds in clinical trials. Nat Prod Rep. 2008 Jun;25(3):475-516. | ||||
29 | A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8. | ||||
30 | Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. | ||||
31 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
32 | Cerner Multum, Inc. "Australian Product Information.". | ||||
33 | Product Information. Afinitor (everolimus). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
34 | Product Information. Myalept (metreleptin). Bristol-Myers Squibb, Princeton, NJ. | ||||
35 | Canadian Pharmacists Association. | ||||
36 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
37 | Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA. | ||||
38 | Wong GT, Lee EY, Irwin MG. Contrast induced nephropathy in vascular surgery.?Br J Anaesth. 2016;117 Suppl 2:ii63-ii73. [PMID: 27566809] | ||||
39 | Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL. | ||||
40 | Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO. | ||||
41 | Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE. | ||||
42 | Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC. | ||||
43 | Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA. | ||||
44 | Product Information. Blincyto (blinatumomab). Amgen USA, Thousand Oaks, CA. | ||||
45 | Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO. | ||||
46 | Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN. | ||||
47 | Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA. | ||||
48 | Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
49 | Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA. | ||||
50 | Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA. | ||||
51 | Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA. | ||||
52 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
53 | Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA. | ||||
54 | Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA. | ||||
55 | CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058] | ||||
56 | Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA. | ||||