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Selumetinib Dosage

Medically reviewed by Drugs.com. Last updated on May 7, 2020.

Applies to the following strengths: 10 mg; 25 mg

Usual Pediatric Dose for Fibromatosis

2 years and older:
25 mg/m2 orally 2 times a day (approximately every 12 hours) until disease progression or unacceptable toxicity

RECOMMENDED DOSE BASED ON BODY SURFACE AREA (BSA):
-BSA less than 0.55 mg/m2: No dose recommendation.
-BSA 0.55 to 0.69 m2: 20 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 0.7 to 0.89 m2: 20 mg/m2 orally in the morning and 20 mg/m2 in the evening
-BSA 0.9 to 1.09 m2: 25 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.1 to 1.29 m2: 30 mg/m2 orally in the morning and 30 mg/m2 in the evening
-BSA 1.3 to 1.49 m2: 35 mg/m2 orally in the morning and 35 mg/m2 in the evening
-BSA 1.5 to 1.69 m2: 40 mg/m2 orally in the morning and 40 mg/m2 in the evening
-BSA 1.7 to 1.89 m2: 45 mg/m2 orally in the morning and 45 mg/m2 in the evening
-BSA 1.9 mg/m2 or greater: 50 mg orally in the morning and 50 mg/m2 in the evening

Use: Treatment of pediatric patients 2 years and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN)

Renal Dose Adjustments

Mild/moderate/severe renal impairment or end stage renal disease: No adjustment recommended.

Liver Dose Adjustments

DOSE ADJUSTMENTS FOR HEPATIC IMPAIRMENT:
MILD HEPATIC IMPAIRMENT (Child-Pugh A): No adjustment recommended.
MODERATE HEPATIC IMPAIRMENT (Child-Pugh B):
-Body surface area (BSA) 0.55 to 0.69 m2: 10 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 0.7 to 0.89 m2: 20 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 0.9 to 1.09 m2: 20 mg/m2 orally in the morning and 20 mg/m2 in the evening
-BSA 1.1 to 1.29 m2: 25 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.3 to 1.49 m2: 30 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.5 to 1.69 m2: 35 mg/m2 orally in the morning and 30 mg/m2 in the evening
-BSA 1.7 to 1.89 m2: 35 mg/m2 orally in the morning and 35 mg/m2 in the evening
-BSA 1.9 mg/m2 or greater: 40 mg orally in the morning and 40 mg/m2 in the evening
SEVERE HEPATIC IMPAIRMENT (Child-Pugh C): Not recommended.

Dose Adjustments

RECOMMENDED DOSE REDUCTIONS FOR ADVERSE REACTIONS:
BSA 0.55 to 0.69 m2:
-First dose reduction: Reduce dose to 10 mg/m2 orally in the morning and 10 mg/m2 in the evening
-Second dose reduction: Reduce dose to 10 mg/m2 orally once a day
BSA 0.7 to 0.89 m2:
-First dose reduction: Reduce dose to 20 mg/m2 orally in the morning and 10 mg/m2 in the evening
-Second dose reduction: Reduce dose to 10 mg/m2 orally in the morning and 10 mg/m2 in the evening
BSA 0.9 to 1.09 m2:
-First dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 10 mg/m2 in the evening
-Second dose reduction: Reduce dose to 10 mg/m2 orally in the morning and 10 mg/m2 in the evening
BSA 1.1 to 1.29 m2:
-First dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 20 mg/m2 in the evening
-Second dose reduction: Reduce dose to 20 mg/m2 orally in the morning and 10 mg/m2 in the evening
BSA 1.3 to 1.49 m2:
-First dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 25 mg/m2 in the evening
-Second dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 10 mg/m2 in the evening
BSA 1.5 to 1.69 m2:
-First dose reduction: Reduce dose to 30 mg/m2 orally in the morning and 30 mg/m2 in the evening
-Second dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 20 mg/m2 in the evening
BSA 1.7 to 1.89 m2:
-First dose reduction: Reduce dose to 35 mg/m2 orally in the morning and 30 mg/m2 in the evening
-Second dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 20 mg/m2 in the evening
BSA 1.9 m2 or greater:
-First dose reduction: Reduce dose to 35 mg/m2 orally in the morning and 35 mg/m2 in the evening
-Second dose reduction: Reduce dose to 25 mg/m2 orally in the morning and 25 mg/m2 in the evening
*Permanently discontinue this drug in patients unable to tolerate it after 2 dose reductions.

CARDIOMYOPATHY:
-Asymptomatic decrease in left ventricular ejection (LVEF) of 10% or greater from baseline and less than lower level of normal: Withhold therapy until resolution; resume at reduced dose.
-Symptomatic decreased LVEF: Permanently discontinue therapy.
-Grade 3 or 4 decreased LVEF: Permanently discontinue therapy.

OCULAR TOXICITY:
-Retinal pigment epithelial detachment (RPED): Withhold therapy until resolution; resume at reduced dose.
-Retinal vein occlusion (RVO): Permanently discontinue therapy.

GASTROINTESTINAL TOXICITY:
-Grade 3 diarrhea: Withhold until improved to Grade 0 or 1; resume at same dose; permanently discontinue if no improvement within 3 days.
-Grade 4 diarrhea: Permanently discontinue therapy.
-Grade 3 or 4 colitis: Permanently discontinue therapy.

SKIN TOXICITY:
-Grade 3 or 4: Withhold therapy until improvement; resume at reduced dose.

INCREASED CREATININE PHOSPHOKINASE (CPK):
-Grade 4 Increased CPK: Withhold therapy until improved to Grade 0 or 1; resume at reduced dose; permanently discontinue therapy if no improvement within 3 weeks.
-Any Increased CPK and myalgia: Withhold therapy until improved to Grade 0 or 1; resume at reduced dose; permanently discontinue therapy if no improvement within 3 weeks.
-Rhabdomyolysis: Permanently discontinue therapy.

OTHER ADVERSE REACTIONS:
-Intolerable Grade 2: Withhold therapy until improved to Grade 0 or 1; resume at reduced dose.
-Grade 3: Withhold therapy until improved to Grade 0 or 1; resume at reduced dose.
-Grade 4: Withhold therapy until improved to Grade 0 or 1; resume at reduced dose; consider discontinuation of therapy.

DOSE MODIFICATIONS FOR DRUG INTERACTIONS:
STRONG OR MODERATE CYP450 3A4 INHIBITORS OR FLUCONAZOLE:
-Avoid coadministration of strong or moderate CYP450 3A4 inhibitors or fluconazole with this drug.
-If coadministration with strong or moderate CYP450 3A4 inhibitors or fluconazole cannot be avoided, reduce the dose of this drug as recommended below. After discontinuation of the strong or moderate CYP450 3A4 inhibitor or fluconazole for 3 elimination half-lives, resume the selumetinib dose that was taken prior to initiating the inhibitor or fluconazole:
RECOMMENDED DOSE OF SELUMETINIB FOR COADMINISTRATION WITH STRONG OR MODERATE CYP450 3A4 INHIBITORS OR FLUCONAZOLE:
IF THE CURRENT DOSE IS 25 MG/M2 TWICE DAILY, REDUCE TO 20 MG/M2 TWICE DAILY:
Daily doses for 20 mg/m2 twice daily:
-BSA 0.55 to 0.69 m2: 10 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 0.7 to 0.89 m2: 20 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 0.9 to 1.09 m2: 20 mg/m2 orally in the morning and 20 mg/m2 in the evening
-BSA 1.1 to 1.29 m2: 25 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.3 to 1.49 m2: 30 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.5 to 1.69 m2: 35 mg/m2 orally in the morning and 30 mg/m2 in the evening
-BSA 1.7 to 1.89 m2: 35 mg/m2 orally in the morning and 35 mg/m2 in the evening
-BSA 1.9 m2 or greater: 40 mg/m2 orally in the morning and 40 mg/m2 in the evening
IF THE CURRENT DOSE IS 20 MG/M2 TWICE DAILY, REDUCE TO 15 MG/M2 TWICE DAILY:
Daily doses for 15 mg/m2 twice daily:
-BSA 0.55 to 0.69 m2: 10 mg/m2 orally once daily
-BSA 0.7 to 0.89 m2: 10 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 0.9 to 1.09 m2: 20 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 1.1 to 1.29 m2: 25 mg/m2 orally in the morning and 10 mg/m2 in the evening
-BSA 1.3 to 1.49 m2: 25 mg/m2 orally in the morning and 20 mg/m2 in the evening
-BSA 1.5 to 1.69 m2: 25 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.7 to 1.89 m2: 30 mg/m2 orally in the morning and 25 mg/m2 in the evening
-BSA 1.9 m2 or greater: 30 mg/m2 orally in the morning and 30 mg/m2 in the evening

Precautions

CONTRAINDICATIONS:
-None

Safety and efficacy have not been established in patients younger than 2 years.

Consult WARNINGS section for additional precautions.

Dialysis

This drug is not dialyzable because it is highly protein bound and extensively metabolized.

Other Comments

Administration advice:
-This drug should be taken on an empty stomach 2 hours before or 1 hour after eating.
-Swallow capsules whole with water; do not chew, dissolve or open capsule.
-Do not administer to patients who are unable to swallow a whole capsule.
-Do not take a missed dose unless it is more than 6 hours until the next scheduled dose.
-If vomiting occurs after administration, do not take an additional dose, but continue with the next scheduled dose.

Storage requirements:
-Store at 25C (77F); excursions permitted to 15C to 30C (59F to 86F).
-Dispense in original bottle; do not remove desiccant; protect from moisture.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.