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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Mitogen-activated protein kinase (MEK) inhibitors
selumetinib
L01EE04
Forms & Strengths
- Capsule, oral: 10 mg
- Capsule, oral: 25 mg
Adult Dosing
- Not formally indicated for adult neurofibromatosis type 1 (NF1) in standard guidelines, though pediatric trials included adolescents aged 18.
Pediatric Dosing
- Pediatric patients 2 years of age and older with NF1 and symptomatic, inoperable plexiform neurofibromas: 25 mg/m² orally twice daily (approx. every 12 hours) until disease progression or unacceptable toxicity.
Indications
- Treatment of pediatric patients 2 years of age and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas.
Mechanism of Action
- Mitogen-activated protein kinase kinase (MEK) 1 and MEK 2 inhibitor.
- Inhibits MEK1/2 phosphorylation and prevents downstream signaling of the MAPK pathway, reducing cellular proliferation in tumors driven by NF1 mutations.
Contraindications
- History of severe hypersensitivity to selumetinib or any of its excipients.
Adverse Reactions
- Vomiting, nausea, and abdominal pain
- Rash, dermatitis acneiform, and dry skin
- Diarrhea and stomatitis
- Fatigue and pyrexia
- Decreased ejection fraction and cardiomyopathy
- Ocular toxicity, including retinal vein occlusion and detachment
- Increased blood creatine phosphokinase (CPK)
Drug Interactions
- Strong and moderate CYP3A4 inhibitors (e.g., itraconazole, fluconazole): May increase selumetinib exposure; reduce selumetinib dose if coadministration is unavoidable.
- Strong and moderate CYP3A4 inducers (e.g., rifampin, carbamazepine): May significantly decrease selumetinib efficacy; avoid coadministration.
- Vitamin E containing products: Selumetinib capsules contain vitamin E (TPGS); concomitant use of high-dose vitamin E supplements should be avoided.
Curated Content: Needs Vetting Before Put to Clinical Use