Mekinist

Trametinib

As monotherapy or in combination w/ dabrafenib for the treatment of adult patients w/ unresectable or metastatic melanoma w/ BRAF V600 mutation. In combination w/ dabrafenib for the adjuvant treatment of adult patients w/ Stage III melanoma w/ BRAF V600 mutation, following complete resection. In combination w/ dabrafenib for the treatment of adult patients w/ advanced non-small cell lung cancer w/ a BRAF V600 mutation.

2 mg once daily.

Should be taken on an empty stomach: Take at least 1 hr before or 2 hr after meals. Swallow w/ a full glass of water, do not chew/crush. Take at the same time every day. When taken in combination w/ dabrafenib, the once-daily dose of trametinib should be taken at the same time each day w/ either the morning dose or the evening dose of dabrafenib.

Hypersensitivity.

Patients who have progressed on a prior BRAF inhibitor therapy; patients whose melanoma tested negative for BRAF V600 mutation; patients w/ a BRAF V600 mutation positive melanoma which has metastasised to the brain. Risk of new malignancies, cutaneous & non-cutaneous; haemorrhage; decreased left ventricular ejection fraction/left ventricular dysfunction; pyrexia; HTN; interstitial lung disease or pneumonitis; disorders associated w/ visual disturbance, including retinal pigment epithelial detachment & retinal vein occlusion; rash; rhabdomyolysis; renal failure; pancreatitis; hepatic adverse events; pulmonary embolism or DVT; colitis & GI perforation. Severe renal impairment. Moderate to severe hepatic impairment. Female patients of reproductive potential should use highly effective contraception during treatment & for 4 mth after treatment. May decrease efficacy of hormonal contraceptives. May impair fertility. Minor influence on the ability to drive & use machines. Pregnancy & lactation. Childn <18 yr.

Monotherapy: Rash, diarrhoea, fatigue, oedema peripheral, nausea, dermatitis acneiform. HTN, haemorrhage; cough, dyspnoea; vomiting, constipation, abdominal pain, dry mouth; dry skin, pruritus, alopecia; pyrexia; increased AST & ALT. Combination therapy: Pyrexia, fatigue, nausea, chills, headache, diarrhoea, vomiting, arthralgia, rash. Nasopharyngitis; decreased appetite; dizziness; HTN, haemorrhage; cough; abdominal pain, constipation; dry skin, pruritus, erythema; myalgia, pain in extremity, muscle spasms; asthenia, oedema peripheral, flu-like illness; increased ALT & AST.

Possible increased levels w/ strong P-gp inhibitors (eg, verapamil, cyclosporine, ritonavir, quinidine, itraconazole). May result in transient inhibition of BCRP substrates (eg, pitavastatin) in the gut.

Targeted Cancer Therapy

L01EE01 - trametinib ; Belongs to the class of mitogen-activated protein kinase (MEK) inhibitors. Used in the treatment of cancer.

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