How it is administered
Trametinib is available as tablets for oral use (0.5 mg and 2 mg) and as a powder for oral solution (each mL of reconstituted solution contains 0.05 mg of trametinib).
Tablets should be taken on an empty stomach, at least 1 hour before or 2 hours after a meal. The oral solution is usually given with a low-fat meal or on an empty stomach. Dosage for children is based on body weight. The medication is typically taken once daily, at the same time each day.
How it works
Trametinib is a kinase inhibitor that works by blocking the activity of specific proteins called MEK1 and MEK2. These proteins are part of a signaling pathway (the RAS/RAF/MEK/ERK pathway) that helps regulate cell growth and division. In some cancers, such as those with a BRAF V600E mutation, this pathway is abnormally active, leading to uncontrolled cell growth.
By inhibiting MEK1 and MEK2, trametinib helps slow down or stop the growth of cancer cells that depend on this pathway. It is especially effective in tumors with certain mutations (like BRAF V600E or V600K), which are common in some solid tumors and rare in blood cancers. Trametinib is often used in combination with other targeted therapies, such as dabrafenib, to enhance its effectiveness and help prevent resistance to treatment.
Common side effects
Common side effects of trametinib (alone or with dabrafenib) include:
- Rash
- Diarrhea
- Lymphedema (swelling)
- Fever (pyrexia)
- Nausea and vomiting
- Chills
- Fatigue
- Headache
- High blood pressure (hypertension)
- Peripheral edema (swelling of hands/feet)
- Dry skin
- Abdominal pain
- Cough
- Hemorrhage (bleeding)
- Muscle and joint pain
Serious side effects can include heart problems, eye problems, lung inflammation, severe skin reactions, and increased blood sugar. Always report any new or worsening symptoms to your doctor.
Who Should take it
Trametinib is indicated for patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test. It is also used in combination with dabrafenib for the treatment of certain solid tumors, including some pediatric low-grade gliomas, non-small cell lung cancer, and anaplastic thyroid cancer, all with BRAF V600E mutations.
For blood cancers, trametinib may be considered in rare cases where the cancer has a BRAF V600E mutation and there are no satisfactory alternative treatment options. It is approved for use in both adults and children (1 year and older) with BRAF V600E-mutated solid tumors who have progressed after prior treatment.
Who should not take it
Trametinib should not be used in patients without a BRAF V600E or V600K mutation, as it is unlikely to be effective. It is not indicated for patients with colorectal cancer due to known resistance.
Patients who are pregnant or planning to become pregnant should avoid trametinib, as it can cause harm to an unborn baby. Caution is also advised in patients with a history of heart problems, eye disorders, or severe skin reactions. Always inform your healthcare provider about your full medical history before starting trametinib.
Commonly used with
Trametinib is most commonly used in combination with dabrafenib, another targeted therapy that inhibits the BRAF protein. This combination is more effective than either drug alone for cancers with BRAF V600 mutations.
It may also be used alongside other supportive medications to manage side effects, such as antipyretics for fever or medications for high blood pressure, depending on individual patient needs.
Commonly tested with
Trametinib is frequently tested in combination with dabrafenib in clinical trials for various cancers with BRAF mutations, including melanoma, non-small cell lung cancer, thyroid cancer, and some pediatric brain tumors.
In research settings, it may also be tested with other targeted therapies or immunotherapies to explore new treatment options for cancers with specific genetic mutations.