Selumetinib

What is Selumetinib

Selumetinib is a mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor indicated for the treatment of pediatric patients 2 years of age and older with neurofibromatosis type 1 who have symptomatic, inoperable plexiform neurofibromas. 

Brand Name

Koselugo

Indications & Dosage

  • plexiform neurofibromas

For the treatment of neurofibromatosis type 1 in patients with symptomatic, inoperable plexiform neurofibromas

NOTE: Selumetinib is designated by the FDA as an orphan drug for this indication.

Side Effects

  1. abdominal pain
  2. acneiform rash
  3. acneiform rash
  4. alopecia
  5. anemia
  6. anemia
  7. anorexia
  8. atopic dermatitis
  9. back pain
  10. bleeding
  11. blurred vision
  12. cardiomyopathy
  13. cardiomyopathy
  14. cataracts
  15. colitis
  16. constipation
  17. diaper dermatitis
  18. diarrhea
  19. diarrhea
  20. dyspnea
  21. edema
  22. elevated hepatic enzymes
  23. elevated hepatic enzymes
  24. epistaxis
  25. erythema
  26. exfoliative dermatitis
  27. fatigue
  28. fever
  29. fever
  30. GI obstruction
  31. GI perforation
  32. hair discoloration
  33. headache
  34. headache
  35. hematuria
  36. hematuria
  37. hyperamylasemia
  38. hyperkalemia
  39. hyperkalemia
  40. hypernatremia
  41. hypertension
  42. hypoalbuminemia
  43. hypokalemia
  44. hypokalemia
  45. hyponatremia
  46. ileus
  47. infection
  48. infection
  49. lymphopenia
  50. lymphopenia
  51. maculopapular rash
  52. malaise
  53. myalgia
  54. nausea
  55. nausea
  56. neutropenia
  57. neutropenia
  58. new primary malignancy
  59. ocular hypertension
  60. oral ulceration
  61. palmar-plantar erythrodysesthesia (hand and foot syndrome)
  62. peripheral edema
  63. photophobia
  64. proteinuria
  65. pruritus
  66. rash
  67. rash
  68. renal failure (unspecified)
  69. retinal detachment
  70. rhabdomyolysis
  71. seborrhea
  72. sinus tachycardia
  73. stomatitis
  74. urticaria
  75. visual impairment
  76. vomiting
  77. vomiting
  78. weight gain
  79. xerosis
  80. xerostomia

Monitoring Parameters

  • creatine phosphokinase (CPK)
  • echocardiogram
  • LFTs
  • ophthalmologic exam
  • pregnancy testing

Contraindications

  • bleeding
  • breast-feeding
  • cataracts
  • contraception requirements
  • heart failure
  • male-mediated teratogenicity
  • pregnancy
  • pregnancy testing
  • reproductive risk
  • retinal detachment
  • rhabdomyolysis
  • visual impairment

Interactions

  • Abciximab
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Amiodarone
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Dipyridamole
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bexarotene
  • Bosentan
  • Butabarbital
  • Carbamazepine
  • Cenobamate
  • Ceritinib
  • Chloramphenicol
  • Cilostazol
  • Ciprofloxacin
  • Clarithromycin
  • Clopidogrel
  • Cobicistat
  • Conivaptan
  • Cranberry, Vaccinium macrocarpon Ait.
  • Crizotinib
  • Cyclosporine
  • Dabrafenib
  • Danazol
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Dexamethasone
  • Diltiazem
  • Dipyridamole
  • Dronedarone
  • Duvelisib
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enzalutamide
  • Eptifibatide
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Etravirine
  • Fedratinib
  • Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
  • Fluconazole
  • Fluvoxamine
  • Fosamprenavir
  • Fosphenytoin
  • grapefruit juice
  • Idelalisib
  • Imatinib
  • Indinavir
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Lefamulin
  • Letermovir
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Methohexital
  • Mifepristone
  • Mitotane
  • Modafinil
  • Nafcillin
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Nevirapine
  • Nilotinib
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Phenobarbital
  • Phenytoin
  • Platelet Inhibitors
  • Posaconazole
  • Prasugrel
  • Primidone
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rifaximin
  • Ritonavir
  • Secobarbital
  • St. John’s Wort, Hypericum perforatum
  • Telithromycin
  • Ticagrelor
  • Ticlopidine
  • Tirofiban
  • Trandolapril; Verapamil
  • Tucatinib
  • Verapamil
  • Vitamin E
  • Vitamin E
  • Vorapaxar
  • Voriconazole
  • Warfarin
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