What do MEK inhibitors do?

MEK inhibitors bind to and inhibit MEK, inhibiting MEK-dependent cell signaling. This inhibition leads to cell death and the inhibition of tumor growth. These are allosteric binding inhibitors of MEK which inhibit either MEK1 alone, or both MEK1 and MEK2.

What drugs are MEK inhibitors?

To date, four MEK inhibitors have been approved by the United States Food and Drug Administration (FDA), including trametinib, binimetinib, selumetinib, and cobimetinib [19–22].

What are the side effects of MEK?

* Breathing Methyl Ethyl Ketone can irritate the nose and throat causing coughing and wheezing. * Exposure can cause dizziness, lightheadedness, headache, nausea, blurred vision, and may cause you to pass out. * Repeated high exposure can damage the nervous system and may affect the brain.

Is MEK inhibitor chemotherapy?

A new class of chemotherapeutic agents, MEK inhibitors, has recently been developed and is proving to be an effective treatment for a number of cancers. A pattern of ocular adverse events has followed these drugs through clinical trials and their association with retinopathy is only just beginning to be recognized.

What is a MEK inhibitor trametinib?

Trametinib (Mekinist™) is a reversible and highly selective allosteric inhibitor of MEK1 and MEK2 with anticancer activity against metastatic melanoma carrying the BRAF V600 mutation.

How is trametinib taken?

Trametinib comes as a tablet to take by mouth. It is usually taken once a day on an empty stomach, at least 1 hour before or 2 hours after a meal. Take trametinib at around the same time every day.

What is trametinib used for?

Dabrafenib and trametinib are types of targeted cancer drugs called cancer growth blockers. They are used together to treat: melanoma skin cancer that can’t be removed with surgery (unresectable) or has spread to other areas of the body (metastatic or advanced melanoma)

What are the possible side effects of mek1/mek2 inhibitors?

In some studies on mice, intermittent dosing was associated with improved survival, and perhaps less toxicity. MEK1/MEK2 inhibitors have a tendency to cause a papulopustular rash, seen in 57% of patients. Other side effects include diarrhea in 43%, whereas peripheral edema is observed in 26%.

What is the role of MEK inhibitors in cancer treatment?

The first therapies to target this pathway were BRAF inhibitors, but intrinsic and acquired tumor resistance quickly led to treatment failure by reactivation of the MAPK pathway. MEK inhibitors have emerged to partially overcome these resistance mechanisms and are now used in combination with BRAF inhibitors to extend the time to resistance.

Which ophthalmologic findings are characteristic of MEK inhibitor toxicity?

Ocular toxicity, comprising blurring of vision and reversible chorioretinopathy (especially central serous retinopathy, CSR) is another feature of MEK inhibitor toxicity. Among these, retinal vein occlusion is irreversible. For this reason, a baseline ophthalmologic examination should be recorded.

What is Mekmek?

MEK is a downstream protein kinase which can be targeted to prevent reactivation of the MAPK pathway in the presence of BRAF or RAS mutations. Normally, ERK1/2 activation initiates a variety of cellular and nuclear pathways, while also inhibiting Raf activity by a feedback loop to modulate the activity of the MAPK pathway.