Drug reference

Midostaurin

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AdalimumabSevereDatabaseDDInter
AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AnagrelideSevereDatabaseDDInter

Mechanism

Midostaurin is an inhibitor of multiple tyrosine kinases. This action leads to the inhibition of growth and proliferation of cancer cells.

Indications

Acute myeloid leukaemia (specialist use only)Aggressive systemic mastocytosis (specialist use only)Systemic mastocytosis with associated haematological neoplasm (specialist use only)Mast cell leukaemia (specialist use only)newly diagnosed FLT-mutant AML (in combination with cytarabine and daunorubicin)systemic mastocytosis with associated leukemiaAdvanced Systemic Mastocytosis (AdvSM)Mast Cell Leukemia (MCL)

Dosing

Adult: For Acute myeloid leukaemia: 50 mg twice daily, on days 8–21 of induction and consolidation chemotherapy cycles. For Aggressive systemic mastocytosis, Systemic mastocytosis with associated haematological neoplasm, Mast cell leukaemia: 100 mg twice daily. For dose adjustment or treatment interruption due to side-effects, consult product literature.

Pharmacokinetics

Half-life

19 h (parent midostaurin)

Bioavailability

>90%

Protein binding

>99.8%

Metabolism

Metabolized by CYP3A4

Excretion

—

Contraindications

Active severe infection (control before initiation of monotherapy)
Elderly (limited experience)
Patients at risk of congestive heart failure
Risk factors for QT-interval prolongation

Side effects

Common

AstheniaBruisingChillsConcentration impairedConstipationCoughCystitisDiarrhoeaDizzinessDyspepsiaDyspnoeaFallFebrile neutropeniaFeverHaemorrhageHeadacheHyperglycaemiaHypersensitivityHypotensionIncreased risk of infectionNauseaOedemaOropharyngeal painRespiratory disordersSepsisTremorVertigomucositisupper respiratory tract infectiondiarrheamusculoskeletal painDiarrhea (intolerance due to)

Serious