Selumetinib (Koselugo) is a targeted therapeutic drug for diseases caused by specific gene mutations. Developed by AstraZeneca, it was first approved for marketing by the U.S. FDA in 2020.
What is Selumetinib (Koselugo)?
Selumetinib (Koselugo) is an oral small-molecule kinase inhibitor. It targets and inhibits MEK1/2 proteins to regulate the RAS-RAF-MEK-ERK signaling pathway, and is used for the treatment of neoplastic diseases caused by specific gene mutations.
Specifications and Properties of Selumetinib (Koselugo)
Dosage Form and Specification
10mg capsules: White opaque hard capsules marked with black "SEL10".
25mg capsules: Blue opaque hard capsules marked with black "SEL25".
Each bottle contains 60 capsules, which should be stored in the original bottle with the desiccant retained.
Ingredients and Characteristics
Active ingredient: Selumetinib (each 10mg capsule contains 12.1mg of selumetinib sulfate, and each 25mg capsule contains 30.25mg of selumetinib sulfate).
Excipient: D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) (each 10mg capsule contains 32mg of TPGS, and each 25mg capsule contains 36mg of TPGS).
Storage Conditions
Store at room temperature below 25°C (77°F). Short-term storage at 15°C - 30°C (59°F - 86°F) is allowed.
Dosage and Administration of Selumetinib (Koselugo)
Recommended Dosage
Standard dosage: 25mg/m² orally, twice daily (approximately 12 hours apart), on an empty stomach (fast for 2 hours before meals or 1 hour after meals).
Special Administration
Hepatic impairment: For moderate hepatic impairment (Child-Pugh B), reduce the dose to 20mg/m² twice daily; no recommended dose is available for severe hepatic impairment (Child-Pugh C).
Drug interactions: Avoid concurrent use with strong/moderate CYP3A4 inhibitors (e.g., itraconazole) or inducers (e.g., rifampicin). Adjust the dose if necessary.
Principles of Dose Adjustment
Cardiotoxicity (decrease in LVEF ≥ 10%): Suspend administration, and reduce the dose after recovery.
Severe diarrhea (Grade ≥ 3): Suspend administration until symptoms resolve; permanent discontinuation may be necessary if required.
Ocular toxicity (e.g., retinal vein occlusion): Discontinue administration permanently.
Precautions for Administration
Swallow the capsule whole: Do not chew, dissolve, or open the capsule.
Management of missed dose: If a dose is missed and more than 6 hours remain until the next scheduled dose, take the missed dose; otherwise, skip the missed dose.
Management of vomiting: Do not take an additional dose after vomiting; take the next dose as scheduled.
