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Koselugo
selumetinib
Adult Dosing .
Dosage forms: CAP: 10 mg, 25 mg: GRANULE: 5 mg, 7.5 mg
Special Note
- [strength clarification]
- Info: 10 mg cap contains 32 mg vitamin E; 25 mg cap contains 36 mg vitamin E
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing including toxicity-related dose adjustments
neurofibromatosis, type 1
- [cap form, BSA 1.1-1.29 m^2]
- Dose: 30 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, BSA 1.3-1.49 m^2]
- Dose: 35 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, BSA 1.5-1.69 m^2]
- Dose: 40 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, BSA 1.7-1.89 m^2]
- Dose: 45 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, BSA >1.9 m^2]
- Dose: 50 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [granule form, BSA 1.1-1.29 m^2]
- Dose: 30 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, BSA 1.3-1.49 m^2]
- Dose: 35 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, BSA 1.5-1.69 m^2]
- Dose: 40 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, BSA 1.7-1.89 m^2]
- Dose: 45 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, BSA >1.9 m^2]
- Dose: 50 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
renal dosing
- [no adjustment]
- renal impairment: no adjustment
- HD/PD: no adjustment; no supplement
hepatic dosing
- [BSA 1.1-1.29 m^2]
- Child-Pugh Class B: 25 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [BSA 1.3-1.49 m^2]
- Child-Pugh Class B: 30 mg PO qam, 25 mg PO qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [BSA 1.5-1.69 m^2]
- Child-Pugh Class B: 35 mg PO qam, 30 mg PO qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [BSA 1.7-1.89 m^2]
- Child-Pugh Class B: 35 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [BSA >1.9 m^2]
- Child-Pugh Class B: 40 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
Peds Dosing .
- Dosage forms: CAP: 10 mg, 25 mg: GRANULE: 5 mg, 7.5 mg
Special Note
- [strength clarification]
- Info: 10 mg cap contains 32 mg vitamin E; 25 mg cap contains 36 mg vitamin E
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing including toxicity-related dose adjustments
neurofibromatosis, type 1
- [cap form, 1 yo and older, BSA 0.55-0.69 m^2]
- Dose: 20 mg PO qam, 10 mg PO qpm (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA 0.7-0.89 m^2]
- Dose: 20 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA 0.9-1.09 m^2]
- Dose: 25 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA 1.1-1.29 m^2]
- Dose: 30 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA 1.3-1.49 m^2]
- Dose: 35 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA 1.5-1.69 m^2]
- Dose: 40 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA 1.7-1.89 m^2]
- Dose: 45 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [cap form, 1 yo and older, BSA >1.9 m^2]
- Dose: 50 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; do not open cap
- [granule form, 1 yo and older, BSA 0.4-0.59 m^2]
- Dose: 12.5 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 0.6-0.69 m^2]
- Dose: 15 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 0.7-0.89 m^2]
- Dose: 20 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 0.9-1.09 m^2]
- Dose: 25 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 1.1-1.29 m^2]
- Dose: 30 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 1.3-1.49 m^2]
- Dose: 35 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 1.5-1.69 m^2]
- Dose: 40 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA 1.7-1.89 m^2]
- Dose: 45 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
- [granule form, 1 yo and older, BSA >1.9 m^2]
- Dose: 50 mg PO bid (25 mg/m^2/dose PO bid); Info: for patients with symptomatic, inoperable plexiform neurofibromas; must open cap, but do not crush/chew granules
renal dosing
- [no adjustment]
- renal impairment: no adjustment
- HD/PD: no adjustment; no supplement
hepatic dosing
- [cap form, BSA 0.55-0.69 m^2]
- Child-Pugh Class B: 10 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA 0.7-0.89 m^2]
- Child-Pugh Class B: 20 mg qam, 10 mg qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA 0.9-1.09 m^2]
- Child-Pugh Class B: 20 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA 1.1-1.29 m^2]
- Child-Pugh Class B: 25 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA 1.3-1.49 m^2]
- Child-Pugh Class B: 30 mg qam, 25 mg qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA 1.5-1.69 m^2]
- Child-Pugh Class B: 35 mg qam, 30 mg qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA 1.7-1.89 m^2]
- Child-Pugh Class B: 35 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [cap form, BSA >1.9 m^2]
- Child-Pugh Class B: 40 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 0.4-0.59 m^2]
- Child-Pugh Class B: 10 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 0.6-0.69 m^2]
- Child-Pugh Class B: 12.5 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 0.7-0.89 m^2]
- Child-Pugh Class B: 15 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 0.9-1.09 m^2]
- Child-Pugh Class B: 20 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 1.1-1.29 m^2]
- Child-Pugh Class B: 25 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 1.3-1.49 m^2]
- Child-Pugh Class B: 30 mg PO qam, 25 mg PO qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 1.5-1.69 m^2]
- Child-Pugh Class B: 35 mg PO qam, 30 mg PO qpm (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA 1.7-1.89 m^2]
- Child-Pugh Class B: 35 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
- [granule form, BSA >1.9 m^2]
- Child-Pugh Class B: 40 mg bid (20 mg/m^2/dose bid); Child-Pugh Class C: not defined
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- vitamin E use, concurrent (cap form)
- avoid: breastfeeding during tx and x1wk after D/C
- caution: patients of childbearing potential
- caution: male patients of reproductive potential
- caution: hepatic impairment, Child-Pugh Class B-C
- caution: cardiac disease history
- caution: LVEF <55%
Drug Interactions .
Overview
selumetinib
kinase inhibitor
- CYP3A4 substrate
- antiplatelet/anticoagulant effects
- cardiotoxic effects
- immunomodulatory effects
- rhabdomyolysis
- avoid supplemental vitamin E if daily vitamin E intake greater than recommended or safe limits; combo may incr. risk of bleeding; additive effects, antiplatelet and anticoagulant effects augmented by vitamin E content in selumetinib capsules
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- cardiomyopathy
- left ventricular dysfunction
- ocular toxicity
- retinal vein occlusion
- retinal pigment epithelial detachment
- central serous retinopathy
- diarrhea, severe
- GI toxicity, severe
- rash, severe
- hand-foot syndrome
- cellulitis
- rhabdomyolysis
- hypoxia
- acute kidney injury
Common Reactions
- vomiting
- rash
- CK incr.
- abdominal pain
- diarrhea
- nausea
- xeroderma
- musculoskeletal pain
- fatigue
- fever
- albumin decr.
- stomatitis
- paronychia
- headache
- pruritus
- ALT or AST incr.
- dermatitis
- constipation
- alopecia
- hair discoloration
- amylase incr.
- lipase incr.
- epistaxis
- electrolyte abnormalities
- hematuria
- proteinuria
- appetite decr.
- LVEF decr.
- edema
- tachycardia
- skin infection
- alk phos incr.
- visual impairment
- xerostomia
- weight gain
- acute kidney injury
- dyspnea
- HTN
- gastroenteritis
- URI
- eczema
- Hgb decr.
- neutrophils decr.
- lymphocytes decr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; LVEF at baseline, then q3mo x1y, then q6mo and as clinically indicated; CK at baseline, then periodically and as clinically indicated; ophthalmic exam at baseline, then regularly and if ocular signs/symptoms; dermatologic exams
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; risk of spontaneous abortion based on limited human data; risk of teratogenicity and embryo-fetal death based on animal data at 5x systemic exposure and drug's mechanism of action
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x1wk after D/C in patients of childbearing potential and male patients
Lactation
Clinical Summary
avoid breastfeeding during tx and x1wk after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for selumetinib: liver; CYP450: 1A2, 2A6, 2C9, 2C19, 2E1, 3A4 (primary), 3A5 substrate; UGT: 1A1, 1A3 substrate; Info: active metabolite
Excretion: for selumetinib: feces 59% (19% unchanged), urine 33% (<1% unchanged); Half-life: 9h
Subclass: Kinase Inhibitors, MEK Inhibitors ; Neurofibromatosis
Mechanism of Action
for selumetinib: inhibits mitogen-activated protein kinase (MAPK) kinases 1 and 2 (MEK1 and MEK2), resulting in inhibition of downstream phosphorylation of extracellular signal-related kinase (ERK) pathway and cell proliferation
Formulary .
No Formulary Selected
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