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
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• Ciprofloxacin
• Clarithromycin
• Clopidogrel
• Cobicistat
• Conivaptan
• Cranberry, Vaccinium macrocarpon Ait.
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• Cyclosporine
• Dabrafenib
• Danazol
• Darunavir
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Delavirdine
• Dexamethasone
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• Dronedarone
• Duvelisib
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• 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
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• Nefazodone
• Nelfinavir
• Netupitant, Fosnetupitant; Palonosetron
• Nevirapine
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• Omeprazole; Amoxicillin; Rifabutin
• Phenobarbital
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• Platelet Inhibitors
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• Primidone
• Ribociclib
• Ribociclib; Letrozole
• Rifabutin
• Rifampin
• Rifapentine
• Rifaximin
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• Secobarbital
• St. John’s Wort, Hypericum perforatum
• Telithromycin
• Ticagrelor
• Ticlopidine
• Tirofiban
• Trandolapril; Verapamil
• Tucatinib
• Verapamil
• Vitamin E
• Vitamin E
• Vorapaxar
• Voriconazole
• Warfarin