Selumetinib Instructions

1. Generic name: selumetinib

Product name: KOSELUGO, KOSELUGO

All names: selumetinib, Selumetinib, selumetinib Hydrogen Sulfate Capsules, selumetinib sulfate, kosulo,Selumetinib Hydrogen Sulfate Capsules

2. Indications:

Selumetinib is 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).

3. Usage and dosage:

1. Recommended dose: The recommended dose of selumetinib is based on body surface area (BSA) and is 25 mg/m2, taken orally twice a day (approximately every 12 hours) until disease progression or unacceptable toxicity occurs. Selumetinibusually needs to be taken on an empty stomach. Do not eat 2 hours before each dose or 1 hour after each dose.

There is currently no dose recommendation for patients whose body surface area is less than0.55m2; patients whose body surface area is between 0.55-0.69m2 take 20mg in the morning and 10mg in the evening; patients whose body surface area is between 0.7-0.7-0. Patients with a body surface area of 0.90-1.09m2 should take 20 mg orally twice a day; patients with a body surface area of 0.90-1.09m2 should take 25 mg orally twice a day; patients with a body surface area within 1.1-1.29m2 Patients take 30 mg orally twice a day; patients with a body surface area in1.30-1.49m2 take 35 mg orally twice a day; patients with a body surface area in1.50-1. Patients with a body surface area of 1.70-1.89 m2 take 40 mg orally twice a day; patients with a body surface area of 1.70-1.89 m2 take 45 mg orally twice a day; patients with a body surface area of 1.9 m2 or higher take 50 mg orally twice a day.

2. Dose adjustment: If a patient experiences adverse reactions while taking selumetinib, the doctor may adjust the dose of selumetinib. If the dose is reduced by two times, patients who cannot tolerate selumetinib should permanently discontinue it.

(1) For patients with moderate hepatic impairment (Child-Pugh B), reduce the recommended dose of selumetinib to 20 mg/m2 orally twice daily; for patients with severe hepatic impairment (Child-Pugh C)The recommended dose of selumetinib has not been established.

4. Adverse reactions:

The most common adverse reactions (≥40%) with selumetinib are vomiting, rash, abdominal pain, diarrhea, nausea, dry skin, fatigue, musculoskeletal pain, pyrexia, acneiform rash, stomatitis, headache, paronychia, and pruritus.

5. Storage:

Selumetinib will be stored at 20°C to 25°C (68°F to 77°F), with a tolerance of 15°C to 30°C (59°F to 86°F). Selumetinib must be packed in the original bottle, keep the bottle tightly closed, do not remove the desiccant, and prevent moisture.

6. Special groups:

1. Women: Selumetinib and its active metabolites are present in the milk of lactating mice. Since breast-fed children may have adverse reactions, it is recommended that women should not breast-feed during treatment with selumetinib and within 1 week after the last dose. It is recommended that women of reproductive potential use effective contraceptive measures during treatment and within 1 week after the last dose.

2. Men: It is recommended that male patients with female partners of reproductive potential use effective contraceptive measures during treatment with selumetinib and within 1 week after the last dose.

7. Mechanism of action:

Selumetinibis an inhibitor of mitogen-activated protein kinase kinase1 and 2 (MEK1/2). MEK1/2 protein is an upstream regulator of the extracellular signal-related kinase (ERK) pathway. Both MEK and ERK are important components of the RAS-regulated RAF-MEK-ERK pathway, which is often activated in different types of cancer. In a genetically modifiedNF1 mouse model, neurofibromas replicated the genotype and phenotype of human NF1, and oral administration of selumetinib inhibited ERK phosphorylation and reduced the number, volume, and proliferation of neurofibromas.

SelumetinibThe original drug has been launched in China, but it has not yet entered the scope of medical insurance. SpecificationThe price of 10mg*60 tablets per box may be more than 20,000 yuan, which is relatively expensive. Selumetiniboriginal drug marketed overseas, specifications10mg*60 capsules per box may cost more than RMB 50,000 (the price may fluctuate due to exchange rates). The ingredients of the original selumetinib sold domestically and abroad are basically the same. There is currently no generic version of selumetinib produced and marketed. For more drug information and specific prices, please consult the medical consultant of Yaode.