MEKTOVI (Binimetinib)

What is this medication?

MEKTOVI (Binimetinib)
Antifungal Agent

MEKTOVI (Binimetinib) is a kinase inhibitor that inhibits mitogen-activated extracellular kinase (MEK) 1 and 2 activation and kinase activity.  MEKTOVI (Binimetinib) in combination with encorafenib is used in the treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation.

ALERT: WARNING
MEKTOVI (Binimetinib) can cause serious organ toxicities and must be dosed with caution. Retinopathy, retinal vein occlusion (RVO) and uveitis can occur and patients should be regularly assessed by an ophthalmologist for any visual disturbances. Patients should be assessed for new or progressive unexplained pulmonary symptoms or findings for possible interstitial lung disease.  Hepatotoxicity has been reported with MEKTOVI (Binimetinib), liver function tests should be done before and during treatment. Monitor creatine phosphokinase and creatinine periodically for signs of rhabdomyolysis.

Advise females with reproductive potential of potential risk to the fetus and to use effective contraception while on MEKTOVI (Binimetinib).

How does this medication work? 

MEKTOVI (Binimetinib) reversibly inhibits mitogen-activated extracellular kinase (MEK) 1 and 2 activation and kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. Binimetinib inhibits ERK phosphorylation and viability and MEK-dependent phosphorylation of the protein kinase B-raf (BRAF) mutant cell lines. The combination of binimetinib and encorafenib allows for greater antitumor activity in BRAF V600 mutant cell lines; in animal studies, the combination also delayed the emergence of resistance in BRAF V600E mutant cells compared to either drug alone.

How should I take this medication? 

Oral: Take 45mg twice daily, 12 hours apart (in combination with Encorafenib) until disease progression or unacceptable toxicity.

How to Take: MEKTOVI may be taken with or without food.

Note: Confirm BRAF V600 mutation status prior to treatment initiation. MEKTOVI (Binimetinib) is associated with a moderate or high emetic potential; antiemetics may be recommended to prevent nausea and vomiting.

What should I watch for while using this medication? 

Before starting MEKTOVI (Binimetinib) make sure to tell your doctor if you have any heart problems, high blood pressure, or a history of blood clots.  Also advise of any current or past history of eye problems, difficulty with breathing, liver or kidney problems.  For women, tell your doctor if you are pregnant or plan to become pregnant. MEKTOVI (Binimetinib) can harm your unborn baby. Women who are able to become pregnant should use effective birth control (contraception) during treatment with MEKTOVI (Binimetinib) and for at least 30 days after the final dose of MEKTOVI (Binimetinib).

What if I miss a dose?

If you forget or miss a dose, do not take a missed dose if <6 hours until the next dose. Do not take an additional dose if vomiting occurs after MEKTOVI (Binimetinib) administration; resume with the next scheduled dose.

How should I store this medication?

MEKTOVI (Binimetinib) should be stored at room temperature, 15 to 30 ˚C (59 to 86 ˚F). Protect from moisture.

What are the possible side effects of using this medication?

Fatigue, nausea, diarrhea, vomiting, and abdominal pain. MEKTOVI (Binimetinib) has been associated with toxicities with heart failure, interstitial pulmonary fibrosis, dermatological toxicity, ocular toxicity and thromboembolism.

Note this is not a complete list of side effects for MEKTOVI (Binimetinib), only common ones.