Trametinib Dimethyl Sulfoxide: A New Hope for Patients with BRAF-Mutated Cancers
Trametinib Dimethyl Sulfoxide: A New Hope for Patients with BRAF-Mutated Cancers
Cancer is a disease that occurs when cells in the body grow and divide uncontrollably. Normally, cells follow a regulated process of growth, division, and death. When this process is disrupted, cells can form tumors that can invade nearby tissues and spread to other parts of the body.
One of the factors that can cause cancer is mutations (changes) in genes that control cell growth and division. These genes are called oncogenes or tumor suppressor genes. When oncogenes are mutated, they become overactive and stimulate cell growth and division. When tumor suppressor genes are mutated, they lose their function and fail to stop cell growth and division.
One of the most common oncogenes that is mutated in cancer is BRAF. BRAF is a protein that belongs to a family of proteins called kinases. Kinases are enzymes that add phosphate groups to other proteins and regulate their activity. BRAF is part of a pathway called MAPK that controls cell growth, division, differentiation, and survival.
About half of all melanomas (a type of skin cancer) and some other cancers have mutations in the BRAF gene. These mutations result in the production of an abnormal BRAF protein that is constantly active and sends signals to the cells to grow and divide without control. This leads to the formation of tumors that are resistant to conventional treatments such as chemotherapy and radiation therapy.
Trametinib dimethyl sulfoxide is a drug that targets the abnormal BRAF protein and blocks its activity. It is also known as Mekinist1. It is a kinase inhibitor, which means it inhibits the activity of kinases such as BRAF. By blocking BRAF, trametinib dimethyl sulfoxide stops the signals that tell the cells to grow and divide uncontrollably. This can shrink or slow down the growth of tumors in some patients with BRAF-mutated cancers.
Trametinib dimethyl sulfoxide is approved by the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of several types of cancers that have mutations in the BRAF gene12. These include:
- Melanoma: Trametinib dimethyl sulfoxide can be used alone or in combination with another drug called dabrafenib (Tafinlar), which also targets the abnormal BRAF protein. Together, these drugs can improve survival, response rate, and disease control compared to placebo or standard chemotherapy in patients with unresectable or metastatic melanoma (melanoma that cannot be removed by surgery or has spread to other parts of the body). They can also reduce the risk of recurrence in patients who have had surgery to remove melanoma that has spread to the lymph nodes1.
- Non-small cell lung cancer (NSCLC): Trametinib dimethyl sulfoxide can be used in combination with dabrafenib to treat patients with metastatic NSCLC (NSCLC that has spread to other parts of the body) that has a mutation in the BRAF gene1.
- Anaplastic thyroid cancer (ATC): Trametinib dimethyl sulfoxide can be used in combination with dabrafenib to treat patients with locally advanced or metastatic ATC (ATC that has grown into nearby tissues or has spread to other parts of the body) that has a mutation in the BRAF gene and cannot be treated with local therapy1.
- Glioma: Trametinib dimethyl sulfoxide can be used alone or in combination with dabrafenib to treat children aged 1 year and older who have low-grade glioma (LGG), a type of brain tumor that affects the glial cells (the cells that surround and support the nerve cells), and have a mutation in the BRAF gene12.
- Solid tumors: Trametinib dimethyl sulfoxide can be used in combination with dabrafenib to treat adults and children aged 6 years and older who have unresectable or metastatic solid tumors (tumors that form solid masses) that have a mutation in the BRAF gene and have progressed following prior treatment and have no satisfactory alternative treatment options1.
Trametinib dimethyl sulfoxide is taken as a tablet or oral solution once daily at least 1 hour before or at least 2 hours after a meal. The dose may vary depending on the type of cancer, the combination partner, and the patient’s weight. Patients should have their blood pressure, heart function, liver function, blood sugar levels, and eye exams monitored regularly while taking trametinib dimethyl sulfoxide. Patients should also avoid sun exposure and use sunscreen while taking trametinib dimethyl sulfoxide1.
Trametinib dimethyl sulfoxide can cause serious side effects, such as bleeding, colitis, heart problems, eye problems, lung problems, skin problems, liver problems, high blood sugar levels, and new skin cancers. The most common side effects are rash, diarrhea, lymphedema, fatigue, nausea, fever, joint pain, headache, vomiting, constipation, cough, and muscle pain1.
Trametinib dimethyl sulfoxide is a new hope for patients with BRAF-mutated cancers. By targeting a specific molecular pathway that drives tumor growth, trametinib dimethyl sulfoxide can offer more effective and less toxic options than conventional chemotherapy. Trametinib dimethyl sulfoxide is also being studied in combination with other drugs for other types of cancers that have BRAF mutations or other alterations in the MAPK pathway.
If you have cancer that has spread beyond the skin or has come back after surgery or other treatments, you should ask your doctor if your tumor has a BRAF mutation. If it does, you may benefit from trametinib dimethyl sulfoxide alone or in combination with dabrafenib. Your doctor will discuss with you the best treatment options for your specific case.