Midostaurin

Structural formula
General
Surname	Midostaurin
other names	CGP 41251; N - [(9 S , 10 R , 11 R , 13 R ) -2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1 H , 9 H -diindolo [1,2,3- gh : 3 ', 2', 1'- lm ] pyrrolo [3,4- j ] [1,7] benzodiazonin-11-yl] - N -methylbenzamide; N -Benzoylstaurosporine; PKC-412;
Molecular formula	C 35 H 30 N 4 O 4
Brief description	white solid
External identifiers / databases
PubChem	9829523
ChemSpider	8005258
DrugBank	DB06595
Wikidata	Q6842945
Drug information
ATC code	L01 XE39
properties
Molar mass	570.646 g mol −1
Physical state	firmly
Melting point	235-260 ° C
solubility	soluble in DMSO (15 mg / ml); soluble in MDC (10 mg / ml), methanol (5 mg / ml), ethanol (2.5 mg / ml) and DMF (20 mg / ml);
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Midostaurin (trade name Rydapt ) is a tyrosine kinase inhibitor that has been studied in the treatment of acute myeloid leukemia , myelodysplastic syndrome, and advanced systemic mastocytosis . It is a semi-synthetic derivative of staurosporine , an alkaloid from the bacterium Streptomyces staurosporeus . The active ingredient has been approved in the USA since 2017. In Europe, the European Medicines Agency for FLT3-positive AML and three forms of systemic mastocytosis received marketing authorization in September 2017.

literature

FDA: FDA information

Individual evidence

↑ ^a ^b ^c Data sheet Midostaurin hydrate, ≥98% (HPLC), solid from Sigma-Aldrich , accessed on November 4, 2017 ( PDF ).
↑ ^a ^b Datasheet Midostaurin at AlfaAesar, accessed on November 4, 2017 ( PDF )(JavaScript required) .
↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ Pharmaceutical newspaper online: Midostaurin: A new multitarget kinase inhibitor: Pharmaceutical newspaper online: Midostaurin: A new multitarget kinase inhibitor , accessed on November 4, 2017.
^ Hillard Lazarus, Molly Miller: Midostaurin: an emerging treatment for acute myeloid leukemia patients. In: Journal of Blood Medicine. , P. 73, doi : 10.2147 / JBM.S100283 .
^ Gordon W. Gribble: Heterocyclic Scaffolds II: Reactions and Applications of Indoles . Springer Science & Business Media, 2010, ISBN 978-3-642-15732-5 , p. 18 ( limited preview in Google Book search).
↑ Approval: Midostaurin is now an option for AML and mastocytosis: Approval: Midostaurin is now an option for AML and mastocytosis , accessed on September 1, 2019.

[Sigma-1] Data sheet Midostaurin hydrate, ≥98% (HPLC), solid from Sigma-Aldrich , accessed on November 4, 2017 ( PDF ).

[Alfa-2] Datasheet Midostaurin at AlfaAesar, accessed on November 4, 2017 ( PDF )(JavaScript required) .

[NV-3] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[Pharmazeutische_Zeitung_online-4] Pharmaceutical newspaper online: Midostaurin: A new multitarget kinase inhibitor: Pharmaceutical newspaper online: Midostaurin: A new multitarget kinase inhibitor , accessed on November 4, 2017.

[DOI10.2147/JBM.S100283-5] Hillard Lazarus, Molly Miller: Midostaurin: an emerging treatment for acute myeloid leukemia patients. In: Journal of Blood Medicine. , P. 73, doi : 10.2147 / JBM.S100283 .

[Gordon_W._Gribble-6] Gordon W. Gribble: Heterocyclic Scaffolds II: Reactions and Applications of Indoles . Springer Science & Business Media, 2010, ISBN 978-3-642-15732-5 , p. 18 ( limited preview in Google Book search).

[Zulassung:_Midostaurin_ist_jetzt_Option_bei_AML_und_Mastozytose-7] Approval: Midostaurin is now an option for AML and mastocytosis: Approval: Midostaurin is now an option for AML and mastocytosis , accessed on September 1, 2019.