| Drug General Information |
| Drug ID |
D07NVU
|
| Former ID |
DCL000165
|
| Drug Name |
Midostaurin
|
| Synonyms |
CPG 41251; PKC412; N-Benzoylstaurosporine; PKC-412; Midostaurin (USAN/INN)
|
| Drug Type |
Small molecular drug
|
| Indication |
Acute myeloid leukemia [ICD9: 205; ICD10:C92.0]
|
Approved |
[1]
|
|---|
|
Colon cancer; Breast cancer; CLL; AML; GIST [ICD9: 140-199, 150-159, 200, 202, 202.8, 204.1, 205.0, 210-229; ICD10:C00-C75, C15-C26, C7A, C7B, C81-C86, C82-C85, C91.1, C92.0, D10-D36, D3A]
|
Phase 2 |
[2],
[3]
|
|
Breast cancer; Colorectal cancer [ICD9: 153, 154, 174, 175; ICD10:C18-C21, C50]
|
Phase 1 |
[2],
[3]
|
| Therapeutic Class |
Anticancer Agents
|
| Company |
Novartis
|
| Structure |
|
Download
2D MOL
|
| Formula |
C35H30N4O4
|
| InChI |
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 |
14788708, 14935507, 22395186, 44927646, 47206756, 53786846, 57373453, 79311635, 99302777, 103734272, 123105168, 124659175, 124950161, 134348392, 135061643, 135610396, 137241200, 143298037, 172918683, 174006478, 177748492, 178102329, 179149698, 184812273, 198965438, 210274665, 210280297, 223656331, 233822082, 241376205, 248897758, 249617730, 252156932
|
| Target and Pathway |
| Target(s) |
FL cytokine receptor |
Target Info |
Inhibitor |
[4],
[5]
|
|---|
| Protein kinase C gamma type |
Target Info |
Inhibitor |
[4],
[5]
|
|
KEGG Pathway
|
Cytokine-cytokine receptor interaction
|
|
Hematopoietic cell lineage
|
|
Pathways in cancer
|
|
Transcriptional misregulation in cancer
|
|
Acute myeloid leukemia
|
|
Central carbon metabolism in cancerhsa04010:MAPK signaling pathway
|
|
ErbB signaling pathway
|
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
Calcium signaling pathway
|
|
HIF-1 signaling pathway
|
|
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
|
|
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 (Edaravone) |
|---|
| REF 2 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. |
|---|
| REF 3 | (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 | 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 5 | CBL exon 8/9 mutants activate the FLT3 pathway and cluster in core binding factor/11q deletion acute myeloid leukemia/myelodysplastic syndrome subtypes. Clin Cancer Res. 2009 Apr 1;15(7):2238-47. Epub 2009 Mar 10. |
|---|
