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midostaurin (Rydapt)

Indications: - acute myeloid leukemia (AML), FLT3 mutation positive - for use in combination with standard cytarabine & daunorubicin induction & cytarabine consolidation - aggressive systemic mastocytosis or systemic mastocytosis with associated hematological neoplasm, or mast cell leukemia Dosage: - AML: - 50 mg every 12 hours* on days 8-21 of each induction cycle with cytarabine & daunorubicin & on days 8-21 of each consolidation cycle with high-dose cytarabine - systemic mastocytosis or mast cell leukemia: - 100 mg PO BID* - continue until disease progression or unacceptable toxicity * with food Capsules: 25 mg Adverse effects: - >= 20% - febrile neutropenia - nausea, vomiting - mucositis - headache - petechiae - musculoskeletal pain - epistaxis - device-related infection - hyperglycemia Drug interactions: - strong CYP3A4 Inhibitors may increase exposure to midostaurin & its active metabolite Mechanism of action: - inhibits FLT3 receptor tyrosine kinase

Interactions

drug adverse effects of tyrosine kinase inhibitor(s)

General

antineoplastic agent (chemotherapeutic agent) tyrosine kinase inhibitor

Database Correlations

PUBCHEM correlations

References

  1. Gotlib J, Kluin-Nelemans HC, George TI et al Efficacy and Safety of Midostaurin in Advanced Systemic Mastocytosis. N Engl J Med. 2016 Jun 30;374(26):2530-41. PMID: 27355533 Free Article
  2. O'Neil A, Klil-Drori AJ. AML: FLT3 Inhibitor Shows 'Robust' Activity as Frontline Therapy - Overall response rate 100% in patients with FLT3- mutated disease in early research. MedPage Today. Jan 17, 2018 https://www.medpagetoday.com/reading-room/asco/hematologic-malignancies/70559
  3. RYDAPT prescribing information https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/rydapt.pdf