Products
Midostaurin was approved in many countries, in the EU and in the US in 2017 in the form of soft capsules (Rydapt).
Structure and properties
Midostaurin (C35H30N4O4, Mr = 570.6 g/mol) is a -benzoyl derivative of staurosporine, an alkaloid isolated from the bacterium. The two active metabolites CGP62221 and CGP52421 are involved in the pharmacological effects. CGP52421 has a long half-life of 471 hours.
Effects
Midostaurin (ATC L01XE39) has antiproliferative and proapoptotic properties. The effects are due to inhibition of several kinases: FLT3, KIT, FGFR, VEGFR2, and protein kinase C.
Indications
- Acute myeloid leukemia (AML), in combination with standard chemotherapy.
- Advanced systemic mastocytosis (SM).
Dosage
According to the professional information. Capsules are taken in the morning and evening, 12 hours apart and with food.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Midostaurin is a substrate of CYP3A4 and corresponding drug-drug interactions have been documented.
Adverse effects
The most common potential adverse effects include: AML (with chemotherapy): febrile neutropenia, nausea, dermatitis exfoliativa, vomiting, headache, skin bleeding, and fever. SM: Nausea, vomiting, diarrhea, peripheral edema, and fatigue.
