Drug General Information
Drug ID
D07NVU
Former ID
DCL000165
Drug Name
Midostaurin
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
Drug Type
Small molecular drug
Indication Acute myeloid leukaemia [ICD-11: 2A60] Approved [1]
Systemic mastocytosis [ICD-11: 2A21.0; ICD-9: 202.6, 757.33] Approved [2]
Chronic myelomonocytic leukaemia [ICD-11: 2A40; ICD-10: C93.1] Phase 2 [3], [4]
Colorectal cancer [ICD-11: 2B91.Z] Phase 1 [3], [4]
Therapeutic Class
Anticancer Agents
Company
Novartis
Structure
Download
2D MOL

Formula
C35H30N4O4
Canonical SMILES
CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC
InChI
1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m1/s1
InChIKey
BMGQWWVMWDBQGC-IIFHNQTCSA-N
CAS Number
CAS 120685-11-2
PubChem Compound ID
PubChem Substance ID
ChEBI ID
CHEBI:63452
Target and Pathway
Target(s) Fms-like tyrosine kinase 3 (FLT-3) Target Info Inhibitor [5], [6]
Protein kinase C gamma (PRKCG) Target Info Inhibitor [5], [6]
KEGG Pathway Cytokine-cytokine receptor interaction
Hematopoietic cell lineage
Pathways in cancer
Transcriptional misregulation in cancer
Acute myeloid leukemia
Central carbon metabolism in cancer
Phosphatidylinositol signaling system
Sphingolipid signaling pathway
mTOR signaling pathway
Vascular smooth muscle contraction
Wnt signaling pathway
VEGF signaling pathway
Focal adhesion
Tight junction
Gap junction
Natural killer cell mediated cytotoxicity
Fc gamma R-mediated phagocytosis
Leukocyte transendothelial migration
Circadian entrainment
Long-term potentiation
Retrograde endocannabinoid signaling
Glutamatergic synapse
Cholinergic synapse
Serotonergic synapse
GABAergic synapse
Dopaminergic synapse
Long-term depression
Inflammatory mediator regulation of TRP channels
Insulin secretion
Melanogenesis
Thyroid hormone synthesis
Thyroid hormone signaling pathway
Oxytocin signaling pathway
Aldosterone-regulated sodium reabsorption
Endocrine and other factor-regulated calcium reabsorption
Salivary secretion
Gastric acid secretion
Pancreatic secretion
Amphetamine addiction
Morphine addiction
Vibrio cholerae infection
African trypanosomiasis
Amoebiasis
Hepatitis B
Pathways in cancer
Proteoglycans in cancer
MicroRNAs in cancer
Glioma
Non-small cell lung cancer
Choline metabolism in cancer
Panther Pathway Alpha adrenergic receptor signaling pathway
Alzheimer disease-amyloid secretase pathway
Angiogenesis
Apoptosis signaling pathway
EGF receptor signaling pathway
Endothelin signaling pathway
FGF signaling pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Muscarinic acetylcholine receptor 1 and 3 signaling pathway
VEGF signaling pathway
Wnt signaling pathway
5HT2 type receptor mediated signaling pathway
Histamine H1 receptor mediated signaling pathway
Oxytocin receptor mediated signaling pathway
Thyrotropin-releasing hormone receptor signaling pathway
Pathway Interaction Database Endothelins
Thromboxane A2 receptor signaling
Role of Calcineurin-dependent NFAT signaling in lymphocytes
Retinoic acid receptors-mediated signaling
IL8- and CXCR2-mediated signaling events
PAR1-mediated thrombin signaling events
IL8- and CXCR1-mediated signaling events
Reactome Calmodulin induced events
Disinhibition of SNARE formation
Trafficking of GluR2-containing AMPA receptors
G alpha (z) signalling events
WNT5A-dependent internalization of FZD4
Response to elevated platelet cytosolic Ca2+
WikiPathways Calcium Regulation in the Cardiac Cell
Wnt Signaling Pathway
Wnt Signaling Pathway and Pluripotency
MAPK Signaling Pathway
Wnt Signaling Pathway Netpath
G Protein Signaling Pathways
Myometrial Relaxation and Contraction Pathways
DAG and IP3 signaling
Signaling Pathways in Glioblastoma
miRs in Muscle Cell Differentiation
Opioid Signalling
Response to elevated platelet cytosolic Ca2+
References
REF 1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018
REF 2 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
REF 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).
REF 4 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
REF 5 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.
REF 6 CBL exon 8/9 mutants activate the FLT3 pathway and cluster in core binding factor/11q deletion acute myeloid leukemia/myelodysplastic syndrome subt... Clin Cancer Res. 2009 Apr 1;15(7):2238-47.

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