Generic Name: trametinib
Drug Class: Targeted Therapy Medications
Approval Status: Approved
Generic Version Available: No
Mekinist is a kinase inhibitor approved to treat certain cancers with BRAF V600 mutations. It can be used alone to treat people with inoperable or metastatic melanoma. It is approved in combination with the companion drug Tafinlar for treatment of inoperable or metastatic melanoma and for prevention of melanoma recurrence after surgery. The combination is also approved for metastatic non-small-cell lung cancer (NSCLC) and advanced thyroid cancer.
Mekinist is a targeted therapy that interferes with the activity of MEK (mitogen-activated extracellular signal-regulated kinase) proteins that play a role in cell growth. It is more effective when combined with the BRAF inhibitor Tafinlar. Certain BRAF gene mutations, including V600E, promote tumor growth.
Clinical trials showed that Mekinist alone delayed progression of melanoma in people with BRAF V600E or V600K mutations. The combination of Mekinist plus Tafinlar also improved survival and delayed cancer recurrence. Other studies showed that Mekinist plus Tafinlar shrank tumors in about 60% of people with metastatic NSCLC or anaplastic thyroid cancer with BRAF V600E mutations. Mekinist was first approved in 2013.
Mekinist is a once-daily pill that should be taken at least one hour before or two hours after a meal.
Common side effects of Mekinist plus Tafinlar include fever, fatigue, nausea, vomiting, diarrhea, skin rash, muscle and joint pain and swelling. More serious adverse events may include new malignancies, heavy bleeding, gastrointestinal inflammation, heart problems, blood clots, lung and eye problems, severe skin reactions, high fever and elevated blood glucose. Mekinist can cause fetal harm if used during pregnancy.
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Last Reviewed: October 23, 2019