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Koselugo

selumetinib
MEK1/2 InhibitorFDA Approved 2020AstraZeneca
Route
Oral
Half-Life
~11 hrs
FDA Approved
2020
Manufacturer
AstraZeneca
1. Indications and Usage

Pediatric patients 1 year and older and adults with NF1 who have symptomatic, inoperable plexiform neurofibromas.

2. Dosage and Administration

Adults: 75 mg orally twice daily on empty stomach. Pediatric: 25 mg/m2 BSA twice daily.

3. Dosage Forms and Strengths

Capsules: 10 mg, 25 mg; Granules for oral suspension: 10 mg

4. Contraindications

None listed in the prescribing information.

5. Warnings and Precautions
  • Cardiomyopathy: Assess LVEF at baseline and periodically.
  • Ocular Toxicity: Including RPED. Ophthalmologic exams at baseline and regularly.
  • GI Toxicity: Diarrhea and severe nausea/vomiting.
  • Rash: Manage with dose modification.
  • Embryo-Fetal Toxicity: Can cause fetal harm.
6. Adverse Reactions
Most Common Adverse Reactions

Vomiting (66%), Rash (62%), Abdominal Pain (56%), Diarrhea (54%), Nausea (50%), Dry Skin (40%), Fatigue (36%), Musculoskeletal Pain (32%), Paronychia (30%)

Vomiting
66%
Rash
62%
Abdominal Pain
56%
Diarrhea
54%
Nausea
50%
Dry Skin
40%
Fatigue
36%
Musculoskeletal Pain
32%
Paronychia
30%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

7. Drug Interactions

Strong CYP3A4/CYP2C19 Inhibitors: Reduce dose.
Strong CYP3A4 Inducers: Avoid.

8. Use in Specific Populations
Pregnancy

Consult the full prescribing information for pregnancy-related considerations.

Lactation

Refer to prescribing information for lactation guidance.

Pediatric Use

Pediatric safety and efficacy information is detailed in the full label.

Hepatic/Renal Impairment

Dose modifications for organ impairment are specified in the complete prescribing information.

12. Clinical Pharmacology
Mechanism of Action

Selumetinib is a selective, non-ATP-competitive inhibitor of MEK1 and MEK2 in the RAS-RAF-MEK-ERK pathway, reducing downstream signaling and tumor cell proliferation in NF1-driven neurofibromas.

Pharmacokinetics

Tmax: 1-1.5 hours. Protein binding: ~99%. Half-life: ~8 hours. Elimination: urine 59%, feces 19%.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Selumetinib Trials on ClinicalTrials.gov ↗ 📚 PubMed: Selumetinib Clinical Trials ↗
FDA-Approved Tumor Types

Koselugo has FDA-approved indications across the following cancer types covered on CancerDrugEvidence:

Neuroendocrine Tumors
External Resources
📋 DailyMed Label ↗🏛️ FDA Drugs@FDA ↗🔬 ClinicalTrials.gov ↗📚 PubMed Pivotal Trials ↗
Important Notice: This page is intended as a navigational reference to the FDA-approved prescribing information for Koselugo. It does not replace the full prescribing information. Healthcare professionals should consult the complete package insert available at DailyMed before making prescribing decisions. Patient-specific factors should always guide clinical decision-making.

Frequently Asked Questions

What is Koselugo (selumetinib) approved for?

Koselugo (selumetinib) is an FDA-approved oncology agent. Refer to the full prescribing information for complete indication details.

How is Koselugo (selumetinib) administered?

Refer to the full prescribing information for dosing schedules, administration instructions, and dose modifications.

How does Koselugo (selumetinib) work?

Selumetinib is a selective, non-ATP-competitive inhibitor of MEK1 and MEK2 in the RAS-RAF-MEK-ERK pathway, reducing downstream signaling and tumor cell proliferation in NF1-driven neurofibromas.

What are the most common side effects?

Vomiting (66%), Rash (62%), Abdominal Pain (56%), Diarrhea (54%), Nausea (50%), Dry Skin (40%), Fatigue (36%), Musculoskeletal Pain (32%), Paronychia (30%) Vomiting 66% Rash 62% Abdominal Pain 56% Diarrhea 54% Nausea 50% Dry Skin 40% Fatigue 36% Musculoskeletal Pain 32% Paronychia 30%

← All TherapiesFull Prescribing Information ↗