MEK Inhibitor Mechanism of Action Side Effects and Uses

The most common adverse effects of MEK inhibitors (e.g., trametinib) are rash, diarrhea, peripheral edema, fatigue, and dermatitis acneiform. MEK inhibitors also have unique cardiac and ophthalmologic side effects. Central serous retinopathy can occur during treatment with trametinib.

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 [1922].

How do BRAF and MEK inhibitors work?

MEK inhibitors

The MEK gene works together with the BRAF gene, so drugs that block MEK proteins can also help treat melanomas with BRAF gene changes. MEK inhibitors include trametinib (Mekinist), cobimetinib (Cotellic), and binimetinib (Mektovi).

What does MEK stand for in MEK inhibitor?

MEK stands for MAPK/ERK kinase because of its role in activating the MAPK/ERK pathway; other names for this kinase are MAP2K and MAPKK. Because of its activity upstream of this pathway, MEK affects cellular processes such as proliferation, differentiation, and transcription.

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 does MEK stand for?


Acrónimo Definición
MEK Metil etil cetona
MEK Mujahadeen-e-Khalq (Iranian organization)
MEK Marine Engineering Knowledge
MEK Mojahedin-E Khalq Organization (Iran)


What MEK solvent?

Metil etil cetona (MEK) is a colorless liquid that has a sweet odor and is soluble in water. It is a highly volatile chemical and is frequently used as a commercial cleaner and solvent for glues, paints, coatings, and printing inks.

What does MAPK stand for?

Mitogen-activated protein kinase (MAPK) modules containing three sequentially activated protein kinases are key components of a series of vital signal transduction pathways that regulate processes such as cell proliferation, cell differentiation, and cell death in eukaryotes from yeast to humans (Fig.

Why are BRAF and MEK inhibitors given together?

In comparison with single agent BRAF inhibitors, the combination of BRAF and MEK inhibitors have shown significant improvement in response rates, PFS and OS in addition to fewer side effects related to paradoxical activation of the MAPK pathway; the combination has now become the standard of care in patients with …

Is BRAF inhibitor immunotherapy?

Specifically, two types of therapies, BRAF targeted therapy (TT), which target the constitutively active mitogen activated protein kinase (MAPK) pathway resulting from oncogenic BRAF mutations present in 4050% of patients, and immunotherapy, which target the human immune system to enhance anti-tumor immunity, have ...

How does vemurafenib treat melanoma?

Targeted therapy is cancer treatment that focuses on specific molecules within cancer cells. The drugs work by blocking the function of abnormal molecules to slow the growth and spread of cancer, such as melanoma.

What does MEK stand for kinase?

Mitogen-activated protein kinase kinase (MEK) activity is required for inhibition of skeletal muscle differentiation by insulin-like growth factor 1 or fibroblast growth factor 2. Endocrinology.

What is MEK biology?

MEK, also known as Mitogen-activated protein kinase kinase and MAP2K, is a kinase enzyme that phosphorylates mitogen activated protein kinases (MAPKs), ERK, p38 and JNK. Seven MEK subtypes have been identified, all mediate cellular responses to different growth signals.

¿Qué hay en Keytruda?

Keytruda contiene la droga pembrolizumab. Pertenece a una clase de medicamentos llamados inhibidores de PD-1. Keytruda es un medicamento de inmunoterapia, lo que significa que le dice a ciertas partes de su sistema inmunológico que ataquen las células cancerosas. Keytruda se administra como infusión intravenosa (IV) por proveedores de atención médica.

How many MEK inhibitors are there?

Hasta la fecha, Digital XNUMXk MEK inhibitors have been approved by the United States Food and Drug Administration (FDA), including trametinib, binimetinib, selumetinib, and cobimetinib [19,20,21,22].

Is trametinib a MEK inhibitor?

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.

Why is trametinib used with dabrafenib?

The combination of dabrafenib and trametinib blocks the signaling pathway of the abnormal BRAF molecules. This action slows or stops the out-of-control cell growth: Dabrafenib targets the V600E-mutated BRAF molecule to block its signaling.

Is MEK a protein kinase?

Mitogen-activated protein kinase kinase (also known as MAP2K, MEK, MAPKK) is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK).

Is MEK a tyrosine kinase?

The MEK phosphorylates and activates a mitogen-activated protein kinase (MAPK). RAF and MAPK/ERK are both serine/threonine-specific protein kinases. MEK is a serine/tyrosine/threonine kinase.

What is MEK1 and MEK2?

MEK1 and MEK2 are dual-specificity kinases that activate ERK1 and ERK2 by phosphorylating them at conserved threonine and tyrosine residues in the T-E-Y motif found in their activation loop.

Who uses MEK?

Methyl ethyl ketone is used in many industries. It is used as a solvent and in the manufacture of synthetic rubber, paraffin wax, and to make other chemical products. Some examples of workers at risk of being exposed to methyl ethyl ketone include the following: Workers who work in printing plants.

What does MEK do to your body?

* 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.

What is the difference between acetone and MEK?

MEK or Methyl Ethyl Ketone is stronger than Acetone, because it has a slower evaporation rate and boils at a higher temperature. These differences are why MEK can be a stronger cleaning agent than acetone.

What is the function of MAPK?

The mitogen-activated protein kinases (MAPKs) regulate diverse cellular programs by relaying extracellular signals to intracellular responses. In mammals, there are more than a dozen MAPK enzymes that coordinately regulate cell proliferation, differentiation, motility, and survival.

Why is MAPK important?

ABSTRACT. MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. … The above effects are fulfilled by regulation of cell cycle engine and other cell proliferation related proteins.

Is mTOR a kinase?

The mammalian target of rapamycin (mTOR), a phosphoinositide 3-kinase-related protein kinase, controls cell growth in response to nutrients and growth factors and is frequently deregulated in cancer.

¿Cuál es el tratamiento más efectivo para el melanoma?

The main treatment for melanoma is surgical removal, or excision, of the primary melanoma on the skin. The extent of the surgery depends on the thickness of the melanoma. Most melanomas are found when they are less than 1.0 mm thick, and outpatient surgery is often the only treatment needed.

When is immunotherapy used for melanoma?

Immunotherapy. Immunotherapy is used to treat advanced (stage 4) melanoma, and it’s sometimes offered to people with stage 3 melanoma as part of a clinical trial. Immunotherapy uses medicine to help the body’s immune system find and kill melanoma cells.

How does targeted therapy work for melanoma?

Targeted therapy is a type of melanoma treatment that uses drugs to more precisely identify and stop the action of molecules that are key to the growth of cancer cells. Targeted therapy ‘targets’ the changes in these cancer cells that help them grow, divide, and spread.

When is targeted therapy used?

Targeted therapy is a cancer treatment that uses drugs to target specific genes and proteins that are involved in the growth and survival of cancer cells. Targeted therapy can affect the tissue environment that helps a cancer grow and survive or it can target cells related to cancer growth, like blood vessel cells.

Where is melanoma found in the body?

Melanoma can develop anywhere on the body, including the head and neck, the skin under the fingernails, the genitals, and even the soles of the feet or palms of the hands. Melanoma may not be colored like a mole. It may have no color or be slightly red, which is called amelanotic melanoma.

Who makes vemurafenib?

You may report side effects to the FDA at (800) FDA-1088 or You may also report side effects to Genentech al (888) 835-2555.


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Tommy E. Junkins

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