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Selumetinib is an oral small molecule kinase inhibitor that is a selective inhibitor of mitogen-activated protein kinase kinase 1/2 (MEK1/2).
1. Generic name: Selumetinib
2. Trade name: Koselugo
3. English name: Selumetinib
Indicated for the treatment of pediatric patients 2 years of age and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN).
10mg capsules, 25mg capsules.
1. Active ingredient: Selumetinib.
2. Excipients: Vitamin E polyethylene glycol succinate (TPGS). (Note: 10 mg capsules contain 32 mg of vitamin E, and 25 mg capsules contain 36 mg of vitamin E).
1. Recommended dose: 25mg/m², orally, twice a day (about once every 12 hours) until disease progression or unacceptable toxicity occurs.
2. Administration method:
(1) Take on an empty stomach: Avoid eating 2 hours before taking the medicine and 1 hour after taking the medicine.
(2) Swallow the capsule whole: Swallow the capsule whole with water. Do not chew, dissolve or open the capsule.
(3) Patients who are unable to swallow the entire capsule should not use it.
1. Based on body surface area (BSA): The specific dose needs to be determined based on the patient's body surface area table.
2. Based on adverse reactions:According to the severity of adverse reactions (divided into grades 1-4), measures such as suspending the administration, reducing the dose, or permanently discontinuing the drug will be taken.
Common conditions that require dose adjustment include:
(1), cardiomyopathy (decreased left ventricular ejection fraction, LVEF).
(2) Ocular toxicity (such as retinal vein occlusion RVO, retinal pigment epithelial detachment RPED).
(3), severe diarrhea or rash.
(4). Creatine phosphokinase (CPK) is significantly increased or rhabdomyolysis.
3. Based on liver function:
(1) Moderate liver damage (Child-PughB): The dose should be reduced to 20mg/m², twice daily.
(2) Severe liver injury (Child-PughC): The recommended dose has not yet been determined.
4. Based on drug interactions:
Avoid coadministration with strong or moderate CYP3A4 inhibitors (such as itraconazole) or fluconazole. If this cannot be avoided, the dose of selumetinib needs to be reduced according to the table.
1. Before and after meals: Must be taken on an empty stomach.
2. Missed dose: If it is more than 6 hours before the next dose, you should take it as soon as possible; otherwise, you should skip the missed dose and take the next dose as originally planned. Do not take supplementary doses or double the dose.
3. Vomiting: If vomiting occurs after taking the medicine, additional doses should not be taken and the next planned dose should be taken on time.
1. Pregnant women: It may cause fetal harm and is contraindicated.
2. Breastfeeding women: Breastfeeding is prohibited during treatment and within 1 week after the last dose.
3. Women/men of childbearing potential: Effective contraceptive measures must be taken during treatment and within 1 week after the last dose.
4. Children: Suitable for children 2 years old and above. Safety and effectiveness in children younger than 2 years of age have not been established.
5. Elderly people:Clinical studies did not include a sufficient number of patients aged 65 and above.
6. Patients with hepatic insufficiency: Dosage reduction is required for moderate injuries and avoid use for severe injuries.
7. Patients with renal insufficiency: No dose adjustment is required.
1. Very common (≥40%): Vomiting, rash (all types), abdominal pain, diarrhea, nausea, dry skin, fatigue, musculoskeletal pain, fever, acne-like rash, stomatitis, headache, paronychia, itching.
2. Serious warnings and precautions:
Cardiomyopathy, ocular toxicity (can cause blindness), severe diarrhea, severe skin toxicity, elevated CPK and rhabdomyolysis, elevated vitamin E levels and risk of bleeding.
None.
1. Strong/moderate inhibitors of CYP3A4 (such as itraconazole, clarithromycin) or fluconazole: Avoid combined use. If combined use is necessary, the dose of selumetinib needs to be reduced.
2. Strong/moderate CYP3A4 inducers (such as rifampicin, carbamazepine): Avoid combined use, as it will reduce the efficacy of selumetinib.
3. Vitamin K antagonists (such as warfarin) or antiplatelet drugs (such as aspirin, clopidogrel): Combined use may increase the risk of bleeding and requires strengthened monitoring.
4. Food: Grapefruit/grapefruit juice will affect drug metabolism and should be avoided.
1. Store at 25°C (77°F), allowed to fluctuate between 15°C and 30°C (59°F and 86°F).
2. Keep the medicine bottle in its original packaging, and do not take out the desiccant package inside the bottle.
3. Moisture-proof.