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 does a MEK inhibitor 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.

How does BRAF inhibitor work?

The BRAF inhibitors vemurafenib, dabrafenib and encorafenib are used in the treatment of patients with BRAF-mutant melanoma. They selectively target BRAF kinase and thus interfere with the mitogen-activated protein kinase (MAPK) signalling pathway that regulates the proliferation and survival of melanoma cells.

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.

Why are MEK inhibitors given along with BRAF inhibitors?

Therefore, the premise behind the subsequent clinical trials combining inhibitors of both MEK and mutant BRAF kinase was that they would help to delay this MAPK-driven acquired resistance and result in longer duration of responses, higher rate of tumor responses, and decrease the toxicities observed from paradoxical …

What does BRAF stand for?

BRAF is a human gene that encodes a protein called B-Raf. The gene is also referred to as proto-oncogene B-Raf and v-Raf murine sarcoma viral oncogene homolog B, while the protein is more formally known as serine/threonine-protein kinase B-Raf.

Why are BRAF and MEK inhibitors used 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 MEK inhibitor ImmunoTherapy?

The MEK inhibitor selumetinib complements CTLA-4 blockade by reprogramming the tumor immune microenvironment | Journal for ImmunoTherapy of Cancer.

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.

What is Mekinist used for?

TAFINLAR and MEKINIST are prescription medicines that can be used in combination to treat a type of lung cancer called non-small cell lung cancer (NSCLC) that has spread to other parts of the body (metastatic NSCLC), and that has a certain type of abnormal “BRAF V600E” gene.

What is BRAF MEK inhibitors?

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 is Dabrafenib and Trametinib?

Dabrafenib (Tafinlar®) and trametinib (Mekinst®) are targeted therapy drugs. They are given together to treat melanoma and non-small cell lung cancer.

How are BRAF and MEK inhibitors used to treat cancer?

Combinations of BRAF inhibitors and MEK inhibitors (BRAFi + MEKi) are FDA-approved to treat BRAF V600E/K -mutant melanoma. Efficacy of BRAFi + MEKi associates with cancer cell death and alterations in the tumor immune microenvironment; however, the links are poorly understood.

Is there a combination therapy for BRAF and MEK?

In an attempt to delay resistance to BRAF inhibition and explore the safety of combination therapy with BRAF and MEK inhibition, we conducted a phase 1 and 2 study to investigate the combination of the BRAF inhibitor dabrafenib and the MEK inhibitor trametinib in patients with metastatic BRAF V600 melanoma.

Can a melanoma patient have had a BRAF inhibitor?

In part C only, patients could have undergone no more than one previous chemotherapy regimen for advanced or metastatic melanoma, but those who had previously received BRAF or MEK inhibitors were not eligible.

Which is better for patients with BRAF V600 mutations?

Targeted inhibition of the RAF–MEK–ERK (MAPK) pathway with BRAF inhibitors dabrafenib or vemurafenib, as compared with chemotherapy, improves the progression-free and overall survival of patients who have metastatic melanoma with BRAF V600 mutations.