What is a MEK inhibitor trametinib?

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.

What are BRAF and MEK inhibitors?

BRAF inhibitors are drugs that can shrink or slow the growth of metastatic melanoma in people whose tumors have a BRAF mutation. BRAF inhibitors include vemurafenib (Zelboraf®), dabrafenib (Tafinlar®), and encorafenib (Braftovi®).

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?

Definition of methyl ethyl ketone : a flammable liquid compound C4H8O similar to acetone and used chiefly as a solvent —abbreviation MEK.

What is MEK and BRAF?

The BRAF and MEK genes are known to play a role in cell growth, and mutations of these genes are common in several types of cancer. Approximately half of all melanomas carry a specific BRAF mutation known as V600E. This mutation produces an abnormal version of the BRAF kinase that stimulates cancer growth.

Are MEK inhibitors chemotherapy?

Is MEK bad for you?

People exposed to MEK have nose, throat, skin and eye irritation. If MEK is inhaled with other harmful chemicals, the damage can be more serious. Animals that breathed or swallowed high levels of MEK had serious health effects, including birth defects, fainting and death.

What does MEK protein do?

MEK is a member of the MAPK signaling cascade that is activated in melanoma. When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced.

How long do BRAF and MEK inhibitors work?

2012b]. The rapid antitumor responses observed with BRAF or MEK inhibitor monotherapy are not long lasting in most cases (although in a minority can last for over 5 years) due to the development of acquired resistance with progression after a period of objective tumor response.

What does MEK activate?

MEK is a family of dual specific protein kinases which activate the extracellular signal-regulated kinases by phosphorylation of threonine and tyrosine residues.

What does MEK do to ERK?

Kinase cascade The RAF kinase phosphorylates and activates a MAPK/ERK Kinase (MEK1 or MEK2). The MEK phosphorylates and activates a mitogen-activated protein kinase (MAPK). RAF and MAPK/ERK are both serine/threonine-specific protein kinases.

What happens after you stop immunotherapy?

Data suggest that stopping immunotherapy after 1 year of treatment could lead to inferior progression-free survival and overall survival, says Lopes. However, stopping after 2 years does not appear to negatively impact survival.

What is a MEK inhibitor?

A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase kinase enzymes MEK1 and/or MEK2 . They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers.

How effective are MEK inhibitors for melanoma?

MEK inhibitors as single agents or in combination with other therapies have shown to be efficacious in treating melanoma, lung cancer, and colorectal cancer. According to available clinical data, MEK inhibitor plus a BRAF inhibitor could be a superior therapy.

Is ro5068760 a good MEK inhibitor?

RO5068760, a substituted hydantoin, is a potent, highly selective, non-ATP-competitive MEK1/2 inhibitor. In vitro, RO5068760 could inhibit MEK1 kinase activity potently with an IC50value of 0.025 ± 0.012 μmol/L in Raf/MEK/ERK cascade assay.

Is g-573 a strong allosteric inhibitor of MEK?

G-573 is a potent and selective allosteric inhibitor of MEK. Structural and functional analysis illustrates that G-573 could form a strong hydrogen bond with MEK kinase.