Trametinib (MEKINIST)

Melanoma, adjuvant with BRAF V600E or BRAF V600K mutation

Melanoma, advanced or metastatic with BRAF V600E or BRAF V600K mutation

Melanoma, adjuvant with BRAF V600E or BRAF V600K mutation

• Dose – Oral: 2 mg once daily continuously for up to 12 months
• Given in combination with dabrafenib

Melanoma, advanced or metastatic with BRAF V600E or BRAF V600K mutation

• Dose – Oral: 2 mg once daily continuously until disease progression or unacceptable toxicity
• Given as monotherapy or in combination with dabrafenib

Available as 0.5 mg and 2 mg film-coated tablets. Tablets should NOT be crushed or broken. Refrigerate and protect from moisture and light.

Mitogen-activated Extracellular Kinase (MEK) Inhibitor

Take on an empty stomach at least one hour before or 2 hours after a meal. When given in combination, trametinib should be administered once daily with either the morning or evening dose of dabrafenib.

If a dose is missed, patients should be instructed to take it as soon as they can if it is within 12 hours of the missed dose. If it is over 12 hours since the missed dose, patients should skip the missed dose and resume with the next scheduled dose.

Common: Diarrhea, ALT increase, AST increase, Rash, Skin toxicities (nail changes, skin infections).

Less Common: Cardiomyopathy, Ocular effects (retinal pigment epithelial detachment, retinal detachment, retinal vein occlusion), Gastrointestinal perforation, Colitis, Bleeding events/hemorrhage, Hypertension, Pulmonary embolism, Rhabdomyolysis, Interstitial lung disease/pneumonitis, Dermatitis acneiform, Left ventricular ejection fraction decrease or heart failure

The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.

Baseline before treatment: CBC & differential, platelets, creatinine, sodium, potassium, calcium, magnesium, alkaline phosphatase, ALT, albumin, ECG, echocardiogram, blood pressure.  

During treatment: alkaline phosphatase, ALT, albumin, blood pressure, echocardiogram (at week 8, then every 12 weeks ), dermatologic evaluation (at week 8, then every 12 weeks), skin toxicities.

If clinically indicated: Ophthalmic exam for ocular effects.

• Current drug interaction databases should be consulted for more information.

• Avoid in pregnancy and lactation.
• Trametinib increases the frequency and severity of dabrafenib-associated pyrexia, manage according to the Canadian Consensus statement on BRAF pyrexia management.
• Due to risk of ocular effects, ophthalmic exams should be performed at baseline if clinically indicated, and any time a patient reports new visual disturbances.

BC Cancer. BC Cancer Drug Manual. Trametinib. Vancouver, British Columbia: BC Cancer Agency. Available at: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Trametinib_monograph.pdf. Updated December 1, 2019. Accessed January 22, 2024.

Lexicomp. Trametinib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at: https://online-lexi-com.qe2a-proxy.mun.ca/lco/action/doc/retrieve/docid/patch_f/4519182?cesid=4Hxwg6L1JBh&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dtrametinib%26t%3Dname%26acs%3Dfalse%26acq%3Dtrametinib. Updated January 24, 2024. Accessed January 28, 2024.

Cancer Care Ontario. Trametinib Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/drugs/monograph/44331. Updated June 2021. Accessed January 22, 2024.

Novartis Pharmaceuticals Canada Inc. MEKINIST® Product monograph. Dorval, Quebec. Updated December 14, 2016.