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Rydapt (MIDOSTAURIN)
Rydapt blocks the activity of the Kit receptor, which is involved in the growth and survival of cancer cells.
At a glance
| Generic name | MIDOSTAURIN |
|---|---|
| Sponsor | Novartis |
| Drug class | Kinase Inhibitor [EPC] |
| Target | Mast/stem cell growth factor receptor Kit |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2017 |
| Annual revenue | 200 |
Mechanism of action
Midostaurin is small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR/, as well as members of the serine/threonine kinase PKC (protein kinase C) family.Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells.
Approved indications
- Acute myeloid leukemia, disease
- Aggressive systemic mastocytosis
- Mast cell leukemia
Common side effects
- Febrile neutropenia
- Nausea
- Mucositis
- Vomiting
- Headache
- Petechiae
- Musculoskeletal pain
- Epistaxis
- Device-related infection
- Hyperglycemia
- ECG QT prolonged
- Upper respiratory tract infection
Key clinical trials
- RAD001 in Combination With PKC412 in Patients With Relapsed, Refractory or Poor Prognosis AML or MDS (PHASE1)
- Revumenib in Combination With 7+3 + Midostaurin in AML (PHASE1)
- A Global Study of Midostaurin in Combination With Chemotherapy to Evaluate Safety, Efficacy and Pharmacokinetics in Newly Diagnosed Pediatric Patients With FLT3 Mutated AML (PHASE2)
- Geriatric Assessment & Genetic Profiling to Personalize Therapy in Older Adults With Acute Myeloid Leukemia (PHASE2)
- FLT3-ITD Targeted Therapy in Fit AML Patients (PHASE2,PHASE3)
- Cladribine, Idarubicin, Cytarabine, and Venetoclax in Treating Patients With Acute Myeloid Leukemia, High-Risk Myelodysplastic Syndrome, or Blastic Phase Chronic Myeloid Leukemia (PHASE2)
- Gentuzumab Ozogamicin and Midostaurin Combination With Standard Cytarabine and Danunorubi Midostaurin as a Novel Approach to Treating Patients With Newly Diagnosed FLT-3 Mutated Acute Myeloid Leukemia (PHASE1)
- Improving Risk Assessment of AML With a Precision Genomic Strategy to Assess Mutation Clearance (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |