Trametinib

What is Trametinib

Trametinib is a mitogen-activated extracellular signal-regulated kinase (MEK)1 and MEK2 inhibitor. It inhibits cell growth in BRAF V600 mutation-positive tumors by blocking MEK1 and MEK2 which are proteins activated in the BRAF pathway. Using an FDA-approved test, confirm the presence of the BRAF V600 mutation in tumor specimens prior to initiation of treatment.

Trametinib is indicated as single-agent therapy in patients with BRAF inhibitor-naive, BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma.

In combination with dabrafenib, trametinib is used for the treatment of BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma, as adjuvant therapy following complete resection in patients with BRAF V600E or V600K mutation-positive melanoma and lymph node involvement, for the treatment of BRAF V600E mutation-positive metastatic non-small cell lung cancer, and for the treatment of BRAF V600E mutation-positive locally advanced or metastatic anaplastic thyroid cancer (ATC) in patients with no satisfactory locoregional treatment options.

Venous thromboembolism and interstitial lung disease have been reported with trametinib therapy.

Brand Name

Mekinist

Indications

  1. malignant melanoma
  2. non-small cell lung cancer (NSCLC)
  3. thyroid cancer

Side Effects

  1. abdominal pain
  2. acneiform rash
  3. anemia
  4. anorexia
  5. arthralgia
  6. asthenia
  7. bleeding
  8. blurred vision
  9. bradycardia
  10. cardiomyopathy
  11. chills
  12. colitis
  13. cough
  14. dehydration
  15. diarrhea
  16. dizziness
  17. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  18. dysgeusia
  19. dyspnea
  20. edema
  21. elevated hepatic enzymes
  22. epistaxis
  23. fatigue
  24. fever
  25. folliculitis
  26. GI bleeding
  27. GI perforation
  28. headache
  29. heart failure
  30. hematoma
  31. hemoptysis
  32. hemorrhoids
  33. hyperglycemia
  34. hypertension
  35. hypoalbuminemia
  36. hyponatremia
  37. hypophosphatemia
  38. hypotension
  39. hypoxia
  40. infection
  41. interstitial lung disease
  42. intracranial bleeding
  43. leukopenia
  44. lymphopenia
  45. macular edema
  46. maculopapular rash
  47. malaise
  48. melena
  49. musculoskeletal pain
  50. myalgia
  51. nausea
  52. neutropenia
  53. new primary malignancy
  54. ocular hemorrhage
  55. oral ulceration
  56. peripheral edema
  57. pleural effusion
  58. pneumonitis
  59. pruritus
  60. pulmonary embolism
  61. purpura
  62. QT prolongation
  63. rash
  64. renal failure (unspecified)
  65. retinal detachment
  66. rhabdomyolysis
  67. Stevens-Johnson syndrome
  68. stomatitis
  69. syncope
  70. thrombocytopenia
  71. thromboembolism
  72. thrombosis
  73. vaginal bleeding
  74. vesicular rash
  75. visual impairment
  76. vomiting
  77. xerophthalmia
  78. xerosis
  79. xerostomia

Monitoring Parameters

  • echocardiogram
  • ejection fraction
  • multi-gated radionuclide angiography (MUGA)
  • ophthalmologic exam
  • pregnancy testing
  • skin cancer screening exam

Contraindications

  • bleeding
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • cardiomyopathy
  • children
  • colitis
  • contraception requirements
  • dehydration
  • diabetes mellitus
  • fever
  • geriatric
  • GI bleeding
  • GI perforation
  • glaucoma
  • heart failure
  • hyperglycemia
  • hypertension
  • hypotension
  • infants
  • infection
  • infertility
  • inflammatory bowel disease
  • intracranial bleeding
  • male-mediated teratogenicity
  • neonates
  • new primary malignancy
  • pleural effusion
  • pneumonitis
  • pregnancy
  • pregnancy testing
  • pulmonary disease
  • QT prolongation
  • renal failure
  • reproductive risk
  • retinal detachment
  • serious rash
  • thromboembolic disease
  • ventricular dysfunction

Interactions

  • Chloroquine
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Loperamide
  • Loperamide; Simethicone
  • Paclitaxel
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
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