Details of the Drug
General Information of Drug (ID: DMC7W6R)
Drug Name |
Selumetinib
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Synonyms |
Selumetinib; AZD-6244; ARRY142886; AZD6244; ARRY142886; AZD 6244; AZD-6244; 6UH91I579U; ARRY 142886; ARRY-142886; AZD6244 (Selumetinib); AZD6244(Selumetinib); CHEBI:90227; CHEMBL1614701; MEK inhibitors; Selumetinib (AZD6244); UNII-6UH91I579U
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Indication |
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Drug Type |
Small molecular drug
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Structure |
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3D MOL | 2D MOL | |||||||||||||||||||||||||||||||
#Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 457.7 | ||||||||||||||||||||||||||||||
Topological Polar Surface Area (xlogp) | 3.6 | |||||||||||||||||||||||||||||||
Rotatable Bond Count (rotbonds) | 6 | |||||||||||||||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 3 | |||||||||||||||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 6 | |||||||||||||||||||||||||||||||
Chemical Identifiers |
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Cross-matching ID | ||||||||||||||||||||||||||||||||
Molecular Interaction Atlas of This Drug
![]() Drug Therapeutic Target (DTT) |
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Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||||||||||||
Molecular Expression Atlas of This Drug
The Studied Disease | Melanoma | |||||||||||||||||||||||||||||
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ICD Disease Classification | 2C30 | |||||||||||||||||||||||||||||
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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 Selumetinib (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
References
1 | ClinicalTrials.gov (NCT01933932) Assess Efficacy & Safety of Selumetinib in Combination With Docetaxel in Patients Receiving 2nd Line Treatment for v-Ki-ras2 Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) Positive NSCLC (SELECT-1) | ||||
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2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
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: 5665). | ||||
4 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. | ||||
5 | 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: 1479). | ||||
6 | Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells.Br J Cancer.2012 May 8;106(10):1648-59. | ||||
7 | MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013; 6: 27. | ||||
8 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | ||||
9 | RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer.Cancer Res.2009 Sep 1;69(17):6839-47. | ||||
10 | Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells. Int J Cancer. 2013 Nov;133(9):2089-101. | ||||
11 | The dual RAF/MEK inhibitor CH5126766/RO5126766 may be a potential therapy for RAS-mutated tumor cells.PLoS One.2014 Nov 25;9(11):e113217. | ||||
12 | E6201, a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase-1 and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase kinase-1: in vivo effects on cutaneous inflammatory responses by topical administration. J Pharmacol Exp Ther. 2010 Oct;335(1):23-31. | ||||
13 | Clinical pipeline report, company report or official report of Roche. | ||||
14 | doi: 10.1158/1535-7163.TARG-13-B281 | ||||
15 | Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70. | ||||
16 | MEK inhibitors in oncology: a patent review (2015-Present).Expert Opin Ther Pat. 2017 Aug;27(8):887-906. | ||||
17 | Clinical pipeline report, company report or official report of MedKoo Biosciences. | ||||
18 | Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47. | ||||
19 | Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J Med Chem. 2002 Jan 17;45(2):529-32. | ||||
20 | Reversine increases the plasticity of lineage-committed mammalian cells. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7. | ||||
21 | The MEK1 inhibitor PD98059 sensitizes C8161 melanoma cells to cisplatin-induced apoptosis. Melanoma Res. 2001 Feb;11(1):11-9. | ||||
22 | Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors. Bioorg Med Chem Lett. 2006 Aug 1;16(15):3975-80. | ||||
23 | Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE. | ||||
24 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
25 | Multum Information Services, Inc. Expert Review Panel. | ||||