Trametinib

Brands

DEA Class; Rx

Common Brand Names; Mekinist

  • Antineoplastics, MEK Inhibitors

MEK kinase inhibitor; confirm a BRAF V600 mutation using an FDA-approved test
Used as a single-agent in BRAF inhibitor-naive, advanced BRAF V600E or V600K mutation-positive melanoma, or in combination with dabrafenib for adjuvant or advanced therapy for BRAF V600E or V600K mutation-positive melanoma, metastatic NSCLC, locally advanced or metastatic anaplastic thyroid cancer, or other BRAF V600E mutation-positive solid tumors
Venous thromboembolism and interstitial lung disease have been reported

Indicated for the treatment of malignant melanoma.

For the treatment of non-small cell lung cancer (NSCLC).

For the treatment of thyroid cancer.
For the treatment of BRAF V600E-mutation positive solid tumors.

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Monotherapy

  • Increased AST (60%)

  • Rash (57%)

  • Hyperglycemia (50%)

  • Increase ALT (39%)

  • Leukopenia (38%)

  • Anemia (46%)

  • Neutropenia (44%)

  • Diarrhea (43%)

  • Hypoalbuminemia (42%)

  • Hyperphosphatemia (37%)

  • Hyperkeratosis (37%)

  • Headache (32%)

  • Lymphoedema (32%)

  • Pyrexia (28%)

  • Arthralgia (27%)

  • Papilloma (27%)

  • Increased alkaline phosphatase (24%)

  • Alopecia (22%)

  • Palmar-plantar erythrodysesthesia syndrome (20%)

  • Acneiform dermatitis (19%)

  • Stomatitis (15%)

  • Hypertension (15%)

  • Abdominal pain (13%)

  • Hemorrhage (13%)

  • Back pain (12%)

  • Cough (12%)

  • Myalgia (11%)

  • Dry skin (11%)

  • Constipation (11%)

BRAF V600E or V600K mutation-positive melanoma*

  • Increased AST (57%)

  • Hyperglycemia (60-63%)

  • Pyrexia (54-63%)

  • Fatigue (59%)

  • Neutropenia (46-47%)

  • Increased ALT (48%)

  • Hypoalbuminemia (25-48%)

  • Anemia (25-43%)

  • Hypophosphatemia (38-42%)

  • Nausea (35-40%)

  • Headache (30-39%)

  • Increased alkaline phosphatase (38%)

  • Rash (32-37%)

  • Chills (31-37%)

  • Diarrhea (31-33%)

  • Lymphopenia (26-32%)

  • Vomiting (27-28%)

  • Arthralgia (25-28%)

  • Hypertension (26%)

  • Hyponatremia (25%)

  • Peripheral edema (21%)

  • Thrombocytopenia (21%)

  • Cough (20%)

  • Myalgia (15-20%)

  • Abdominal pain (18%)

  • Hemorrhage (18%)

  • Constipation (13%)

  • Nasopharyngitis (12%)

  • Dizziness (11%)

New primary malignancies, cutaneous and noncutaneous, can occur when trametinib is used in combination with dabrafenib, and with dabrafenib as a single agent

Hemorrhage, including major hemorrhages, can occur when used in combination with dabrafenib

Venous thromboembolism can occur when used in combination with dabrafenib

Interstitial lung disease reported; withhold dose for patients with symptoms (eg, cough, dyspnea, hypoxia, pleural effusion, or infiltrates); permanently discontinue therapy for treatment-related ILD or pneumonitis

Colitis and gastrointestinal perforation can occur; monitor patients closely for colitis and gastrointestinal perforations

May cause fetal harm when administered to a pregnant woman

Based on its mechanism of action and findings from animal reproduction studies, trametinib can cause fetal harm when administered to a pregnant woman

There are no data on the presence of trametinib in human milk, or the effects of trametinib on the breastfed infant, or on milk production

Adults

2 mg PO once daily

Geriatric

2 mg PO once daily

Adolescents

Less than 26 kg: Safety and efficacy have not been established
26 kg to 37 kg: 1 mg PO once daily
38 kg to 50 kg: 1.5 mg PO once daily
51 kg or more: 2 mg PO once daily

Children

Ages 5 or younger:
Safety and efficacy have not been established.
Ages 6 to 12:
Less than 26 kg: Safety and efficacy have not been established.
26 kg to 37 kg: 1 mg PO once daily.
38 kg to 50 kg: 1.5 mg PO once daily.
51 kg or more: 2 mg PO once daily.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Trametinib 

tablet

  • 0.5mg
  • 2mg
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