Midostaurin

Midostaurin

Systematic (IUPAC) name
(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiamzonine-1-one
Clinical data
Pregnancy cat.	?
Legal status	Investigational
Routes	Oral
Identifiers
CAS number	120685-11-2
ATC code	None
PubChem	CID 9829523
UNII	ID912S5VON Y
Synonyms	4'-N-benzoylstaurosporine
Chemical data
Formula	C35H30N4O4
Mol. mass	570.637 g/mol
SMILES	eMolecules & PubChem
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 Key:BMGQWWVMWDBQGC-IIFHNQTCSA-N

Midostaurin (PKC412) is a multi-target protein kinase inhibitor being investigated for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium Streptomyces staurosporeus, and is active in patients with mutations of CD135 (FMS-like tyrosine kinase 3 receptor).^[1]

After successful Phase II clinical trials, a Phase III trial for AML has started in 2008. It is testing midostaurin in combination with daunorubicin and cytarabine.^[2] In another trial, the substance has proven ineffective in metastatic melanoma.^[3]

References

1. ^ Fischer, T.; Stone, R. M.; Deangelo, D. J.; Galinsky, I.; Estey, E.; Lanza, C.; Fox, E.; Ehninger, G. et al. (2010). "Phase IIB Trial of Oral Midostaurin (PKC412), the FMS-Like Tyrosine Kinase 3 Receptor (FLT3) and Multi-Targeted Kinase Inhibitor, in Patients with Acute Myeloid Leukemia and High-Risk Myelodysplastic Syndrome with Either Wild-Type or Mutated FLT3". Journal of Clinical Oncology 28 (28): 4339. doi:10.1200/JCO.2010.28.9678. PMID 20733134.  edit
2. ^ ClinicalTrials.gov NCT00651261 Daunorubicin, Cytarabine, and Midostaurin in Treating Patients With Newly Diagnosed Acute Myeloid Leukemia
3. ^ Millward, M. J.; House, C.; Bowtell, D.; Webster, L.; Olver, I. N.; Gore, M.; Copeman, M.; Lynch, K. et al. (2006). "The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study". British Journal of Cancer 95 (7): 829. doi:10.1038/sj.bjc.6603331. PMC 2360547. PMID 16969355. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2360547.  edit

This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it.v · Categories: Protein kinase inhibitors Alkaloids Lactams Indolocarbazoles Antineoplastic and immunomodulating drug stubs Wikimedia Foundation. 2010. Игры ⚽ Нужно сделать НИР? Mindoro Stripe-faced Fruit Bat Midotiopsis Look at other dictionaries: midostaurin — A substance that is being studied in the treatment of leukemia. It belongs to the family of drugs called protein kinase inhibitors. Also called N benzoyl staurosporine and PKC412 …   English dictionary of cancer terms Staurosporine — drugbox IUPAC name = ( 9S,10R,11R,13R ) 2,3,10,11,12,13 Hexahydro 10 methoxy 9 methyl 11 (methylamino) 9,13 epoxy 1 H ,9 H diindolo [1,2,3 gh:3 ,2 ,1 lm] pyrrolo [3,4 j] [1,7] benzodiazonin 1 one CAS number = 62996 74 1 ATC prefix = ATC suffix =… …   Wikipedia N-benzoyl-staurosporine — A substance that is being studied in the treatment of leukemia. It belongs to the family of drugs called protein kinase inhibitors. Also called PKC412 and midostaurin …   English dictionary of cancer terms PKC412 — A substance that is being studied in the treatment of leukemia. It belongs to the family of drugs called protein kinase inhibitors. Also called N benzoyl staurosporine and midostaurin …   English dictionary of cancer terms 18+ © Academic, 2000-2024 Contact us: Technical Support, Advertising Dictionaries export, created on PHP, Joomla, Drupal, WordPress, MODx. Mark and share Search through all dictionaries Translate… Search Internet Share the article and excerpts Direct link … Do a right-click on the link above and select “Copy Link”