Trametinib and Dabrafenib for Melanoma Treatment

Learn all about dabrafenib (Tafinlar) and trametinib (Mekinist) as separate drugs. Trametinib is a targeted therapy that targets the MEK 1 and MEK 2 protein (kinase) within the cell. It is usually given in combination with a BRAF kinase inhibitor. Dabrafenib is a type of biological therapy drug called a cancer growth blocker. It is also known by its brand name Tafinlar.

Mekinist (trametinib) is a kinase inhibitor used to treat patients with melanoma with BRAF V600E or V600K mutations that are metastatic or unable to be removed by surgery (unresectable). Common side effects of Mekinist include acne, rosacea, dry skin, itching, rash, infection of the skin around a fingernail or toenail, diarrhea, inflammation of the lining of the mouth, abdominal pain, fluid retention and swelling of the limbs, peripheral edema (swelling in the hands and feet), high blood pressure (hypertension), bleeding, fever, chills, tiredness, nausea, vomiting, cough, headache, joint and muscle pain, night sweats, decreased appetite, and constipation.

Dabrafenib blocks the activity of a mutated protein called BRAF, a molecule that helps regulate cell growth. A BRAF mutation signals cells to develop abnormally and divide out of control. These cells grow into a melanoma tumor. About half of all melanomas have a BRAF mutation. Dabrafenib specifically targets the V600E mutated BRAF protein. The drug interferes with abnormal BRAF signals to slow or stop the out-of-control cell growth.

Mekinist is a cancer medicine. Mekinist is the original medicine to cure metastatic melanoma. Mekinist is the prescribed medicine for advanced melanoma, patients. The Mekinist generic name is Trametinib. Actually, Trametinib is a generic pill available in lesser price than the original Mekinist pill. Mekinist is recommended as it interferes with the spread and growth of cancer cells in the body.

Tafinlar in combination with Mekinist, or Mekinist alone, can cause severe bleeding, and in some cases can lead to death. Patients should be advised to call their healthcare provider and get medical help right away if they have headaches, dizziness, or feel weak, cough up blood or blood clots, vomit blood or their vomit looks like “coffee grounds,” have red or black stools that look like tar, or any unusual signs of bleeding.

Trametinib and Dabrafenib for Melanoma Treatment

Trametinib and Dabrafenib for Melanoma Treatment

Melanoma cells often have genetic mutations that cause the cells to rapidly divide and grow. Targeted therapy focuses on these mutations within specific molecules to block the growth of cancer, such as melanoma Trametinib is not indicated for patients that have received prior BRAF inhibitor therapy. Trametinib is a highly selective reversible allosteric inhibitor of MEK1 and MEK2 activity Dabrafenib (Tafinlar) is a drug that shrinks tumors and helps patients with advanced melanoma live longer.

Melanoma with BRAF V600E or V600K mutations

BRAF V600E is a determinant of sensitivity to proteasome inhibitors. Vulnerability to proteasome inhibitors is dependent on persistent BRAF signaling, because BRAF-V600E blockade by PLX4720 reversed sensitivity to carfilzomib in BRAF-mutant colorectal cancer cells. Proteasome inhibition might represent a valuable targeting strategy in BRAF V600E-mutant colorectal tumors. More than 90% of the BRAF mutations in melanoma are identified at codon 600, and about 80% of these are BRAF V600E mutations. The second most common mutation is the BRAF V600K mutation, representing 14% to 28% of BRAF mutations in melanoma.

MEK inhibitor for Melanoma Treatment

The MEK gene works together with the BRAF gene, so drugs that block MEK proteins can also help treat melanomas with BRAF gene changes. The MEK inhibitors trametinib (Mekinist) and cobimetinib (Cotellic) have been shown to shrink some melanomas with BRAF changes. They are pills taken once a day. Common side effects can include rash, nausea, diarrhea, swelling, and sensitivity to sunlight. Rare but serious side effects can include heart damage, excess bleeding, loss of vision, lung problems, and skin infections.

Trametinib (Mekinist) Anti-Cancer Drug

Trametinib dimethyl sulfoxide is a kinase inhibitor. Trametinib (trade name Mekinist) is a cancer drug. It is a MEK inhibitor drug with anti-cancer activity. Trametinib (MEKINIST) is a first-in-class, orally administered selective inhibitor of MEK1/2 serine-threonine kinase. Trametinib inhibits RAF-dependent phosphorylation of MEK1 on S217 and thus prevents the dual phosphorylation of MEK (S217 and S221) required for MEK activation.

Dabrafenib (Tafinlar) Cancer Blocker Drug

Dabrafenib is a targeted therapy used to treat melanoma that has spread. It is also called Tafinlar. Tafinlar is a kinase inhibitor. These drugs work by blocking the action of enzymes called kinases, which are involved in many cell functions, including cell signaling, growth, and division. These enzymes may be too active or found at high levels in some types of cancer cells, and blocking them may help keep cancer cells from growing. Specifically, Tafinlar targets BRAF V600 kinases, which may be involved in cancer cell growth in metastatic melanoma. Tafinlar is indicated as a single agent for the treatment of patients with unresectable (unable to be removed with surgery) or metastatic melanoma with BRAF V600E mutation, as detected by an FDA-approved test. Tafinlar is also indicated in combination with Mekinist (trametinib) for the treatment of patients with unresectable or metastatic melanoma with a confirmed BRAF V600E or V600K mutation.

Trametinib and Dabrafenib Combination Therapy

The combination of dabrafenib and trametinib targets specific molecules that regulate cancer cell growth. Dabrafenib with trametinib as combination therapy works only in patients whose melanoma has tested positive for the BRAF V600E or V600K mutation. The combination of dabrafenib and trametinib blocks the signaling pathway of the abnormal BRAF molecules. Patients in the combination-therapy group had a 12-month survival rate of 72 percent, compared with 65 percent in the vemurafenib group. The dabrafenib-trametinib group also had a better median progression-free survival than the vemurafenib group.

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