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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.

    —

    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