Details of the Drug
General Information of Drug (ID: DMI6E0R)
Drug Name |
Midostaurin
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Synonyms |
PKC412; 120685-11-2; Cgp 41251; 4'-N-Benzoylstaurosporine; CGP-41251; Benzoylstaurosporine; PKC-412; RYDAPT; PKC 412; UNII-ID912S5VON; N-Benzoylstaurosporine; ID912S5VON; CHEMBL608533; CHEBI:63452; Cgp 41 251; N-[(5S,6R,7R,9R)-6-methoxy-5-methyl-14-oxo-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-7-yl]-N-methylbenzamide; PKC-412(Midostaurin); Midostaurin (PKC412); Midostaurin (USAN/INN); Midostaurin [USAN:INN]; CGP 41231; Rydapt (TN); CPG 41251
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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 is unavailable | 2D MOL | ||||||||||||||||||||||||||||||||||
#Ro5 Violations (Lipinski): 1 | Molecular Weight (mw) | 570.6 | |||||||||||||||||||||||||||||||||
Logarithm of the Partition Coefficient (xlogp) | 4.8 | ||||||||||||||||||||||||||||||||||
Rotatable Bond Count (rotbonds) | 3 | ||||||||||||||||||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 1 | ||||||||||||||||||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 4 | ||||||||||||||||||||||||||||||||||
ADMET Property | |||||||||||||||||||||||||||||||||||
Chemical Identifiers |
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Cross-matching ID | |||||||||||||||||||||||||||||||||||
Combinatorial Drugs (CBD) | Click to Jump to the Detailed CBD Information of This Drug | ||||||||||||||||||||||||||||||||||
Repurposed Drugs (RPD) | Click to Jump to the Detailed RPD Information of This Drug | ||||||||||||||||||||||||||||||||||
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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Drug Off-Target (DOT) |
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Molecular Interaction Atlas (MIA) | ||||||||||||||||||||||||||||||||||||||||||||||||||||
Molecular Expression Atlas of This Drug
The Studied Disease | Acute myeloid leukaemia | |||||||||||||||||||||||||||||||||||
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ICD Disease Classification | 2A60 | |||||||||||||||||||||||||||||||||||
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Molecular Expression Atlas (MEA) | ||||||||||||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Same Disease as Midostaurin
Coadministration of a Drug Treating the Disease Different from Midostaurin (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
References
1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018 | ||||
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2 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | ||||
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: 5702). | ||||
4 | Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds | ||||
5 | Swaminathan R: Magnesium metabolism and its disorders. Clin Biochem Rev. 2003 May;24(2):47-66. | ||||
6 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. | ||||
7 | Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007. | ||||
8 | Midostaurin, a novel protein kinase inhibitor for the treatment of acute myelogenous leukemia: insights from human absorption, metabolism, and excretion studies of a BDDCS II drug. Drug Metab Dispos. 2017 May;45(5):540-555. | ||||
9 | Selective inhibition of aldo-keto reductase 1C3: a novel mechanism involved in midostaurin and daunorubicin synergism. Arch Toxicol. 2021 Jan;95(1):67-78. doi: 10.1007/s00204-020-02884-2. Epub 2020 Oct 6. | ||||
10 | Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76. | ||||
11 | FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies. Oncogene. 2005 Dec 15;24(56):8259-67. doi: 10.1038/sj.onc.1208989. | ||||
12 | Oral small-molecule tyrosine kinase inhibitor midostaurin (PKC412) inhibits growth and induces megakaryocytic differentiation in human leukemia cells. Toxicol In Vitro. 2009 Sep;23(6):979-85. doi: 10.1016/j.tiv.2009.06.027. Epub 2009 Jun 30. | ||||
13 | Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells. PLoS One. 2011;6(9):e25351. doi: 10.1371/journal.pone.0025351. Epub 2011 Sep 28. | ||||
14 | Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA. | ||||
15 | Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y "Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers." Cancer Chemother Pharmacol 72 (2013): 1223-34. [PMID: 24085261] | ||||
16 | Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL. | ||||
17 | Canadian Pharmacists Association. | ||||
18 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
19 | Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ. | ||||
20 | Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
21 | Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
22 | Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
23 | Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176] | ||||
24 | Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI. | ||||
25 | Cerner Multum, Inc. "Australian Product Information.". | ||||
26 | Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA. | ||||
27 | Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA. | ||||
28 | Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA. | ||||
29 | Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC. | ||||
30 | Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO. | ||||
31 | Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE. | ||||
32 | Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA. | ||||
33 | Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
34 | Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE. | ||||
35 | Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO. | ||||
36 | Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA. | ||||
37 | Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT. | ||||
38 | Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
39 | Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA. | ||||
40 | Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
41 | Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA. | ||||
42 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
43 | Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC. | ||||
44 | Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA. | ||||
45 | Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA. | ||||
46 | 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] | ||||
47 | Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA. | ||||
48 | EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.". | ||||
49 | Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA. | ||||