Midostaurin is a small-molecule multikinase inhibitor used in oncology. It inhibits several receptor tyrosine kinases, including FLT3 and KIT, as well as members of the protein kinase C (PKC) family. Midostaurin is used in the treatment of newly diagnosed acute myeloid leukemia (AML) with FLT3 mutations, in combination with standard chemotherapy, and for certain patients with advanced systemic mastocytosis.
Midostaurin is also known by development and research names including CGP 41251, PKC412 and NVP-PKC412. Its CAS number is 120685-11-2.
Midostaurin is a specialized oncology pharmaceutical API requiring stringent control of assay, related substances, stereochemical purity, residual solvents and other critical quality attributes.
The FDA identifies Midostaurin as having the molecular formula C35H30N4O4 and molecular weight approximately 570.65 g/mol.
CAS Number: 120685-11-2
Molecular Formula: C35H30N4O4
Molecular Weight: 570.65 g/mol
Synonyms: CGP 41251, CGP-41251, PKC412, NVP-PKC412, N-Benzoylstaurosporine
Drug Class: Multikinase Inhibitor
Therapeutic Class: Antineoplastic Agent
Therapeutic Area: Oncology / Hematology
Molecule Type: Small-Molecule Kinase Inhibitor
Midostaurin inhibits multiple kinases. FDA information identifies activity against wild-type and mutant FLT3, KIT, PDGFRα/β and PKC-family kinases.
Its kinase-inhibitory activity makes it relevant to:
Midostaurin is associated with pharmaceutical applications involving:
Midostaurin is commercially formulated as oral soft capsules. The U.S. product contains 25 mg of midostaurin per capsule.
Midostaurin is a highly lipophilic compound. Published data report a melting-point range of approximately 235–260°C.
FDA quality assessment reports very poor aqueous solubility, below 0.001 mg/mL across the aqueous pH range of approximately 1.0–6.8.
A controlled Midostaurin API manufacturing process may involve:
A published commercial API technical specification reports:
These values are from a manufacturer's published technical product sheet and should not automatically be represented as a universal pharmacopoeial specification.
For API storage, follow the validated manufacturer stability data and approved storage specification. Published technical data report stability studies at 25°C/60% RH and 40°C/75% RH.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.1% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Melting Point | 235–260°C |