Classification: Kinase Inhibitor
About Trametinib (Mekinist®)
BRAF is a protein kinase that plays a role in regulating genes that are responsible for cell replication and survival. It is estimated that 50% of melanomas contain an abnormal form of BRAF (also called/known as a BRAF mutation). This mutated form of BRAF appears to promote overgrowth of these cancer cells. Trametinib works by blocking the actions of the abnormal BRAF, inhibiting cell replication and potentially causing cell death.
How to Take Trametinib
Trametinib is given in a tablet form to be taken by mouth, typically taken once a day. Your dose may be modified throughout treatment depending on the type and degree of side effects you are experiencing. Trametinib tablets should be taken on an empty stomach (1 hour before or 2 hours after meals) and should not be crushed, broken or chewed. If you miss a dose and it has been less than 12 hours since your regular dose time, take it as soon as you remember. If it has been more than 12 hours, skip the dose. Do not take 2 doses at once to make up for a missed dose.
This medication only works in melanoma that has one of two specific BRAF mutations called V600E or V600K, and this abnormality must be tested for prior to starting the medication to identify patients appropriate for therapy. In order to test for mutated BRAF, a sample of the tumor is sent to a special laboratory that performs this test.
Storage and Handling
Store your medication in the original, labeled container in the refrigerator. It should remain in the original bottle with the desiccant packet to be protected from light and moisture. This medication should not be stored in a pillbox. Keep containers out of reach of children and pets.
If a caregiver prepares your dose for you, they should consider wearing gloves or pour the pills directly from their container into the cap, a small cup, or directly into your hand. They should avoid touching the pills. They should always wash their hands before and after giving you the medication. Pregnant or nursing women should not prepare the dose for you. Ask your oncology team where to return any unused medication for disposal. Do not flush down the toilet or throw in the trash.
Where do I get this medication?
Trametinib is available through select specialty pharmacies. Your oncology team will work with your prescription drug plan to identify an in-network specialty pharmacy for distribution of this medication and shipment directly to your home.
This medication may be covered under your prescription drug plan. Patient assistance may be available to qualifying individuals without prescription drug coverage. Co-pay cards, which reduce the patient co-pay responsibility for eligible commercially (non-government sponsored) insured patients, are also available. Your care team can help you find these resources, if they are available.
Possible Side Effects of Trametinib
There are a number of things you can do to manage the side effects of trametinib. Talk to your doctor or nurse about these recommendations. They can help you decide what will work best for you. These are some of the most common side effects:
Rash & Hand Foot Syndrome
Some patients will develop skin rash, redness, or a rash that looks like acne. This rash can become severe and result in a skin infection and hospitalization. Your skin may become very dry. Use an alcohol free moisturizer on your skin and lips; avoid moisturizers with perfumes or scents. If your skin does crack or bleed, be sure to keep the area clean to avoid infection. Be sure to notify your healthcare provider of any rash that develops, as this can be a serious reaction. They can give you more tips on caring for your skin and prescribe topical or oral therapy to help with the itching and rash.
Hand-foot syndrome is a skin reaction that appears on the palms of the hands and/or the soles of the feet as a result of certain chemotherapy agents. It can start as a feeling of tingling or numbness in the palms and/or soles and progress to swelling, redness, peeling skin, and tenderness or pain.
Notify your healthcare team right away if you notice any skin reactions so they can make recommendations or dose changes to prevent them from getting worse.
High Blood Pressure
This medication can cause high blood pressure (hypertension). Hypertension typically occurs within the first few months of therapy. Patients should have their blood pressure checked regularly during therapy. If you develop headaches, light headedness or dizziness, notify your healthcare team.
Diarrhea can be a serious side effect that can lead to dehydration. Notify your healthcare provider if you develop diarrhea.
Your oncology team can recommend medications to relieve diarrhea. Also, try eating low-fiber, bland foods, such as white rice and boiled or baked chicken. Avoid raw fruits, vegetables, whole grain breads, cereals and seeds. Soluble fiber is found in some foods and absorbs fluid, which can help relieve diarrhea. Foods high in soluble fiber include: applesauce, bananas (ripe), canned fruit, orange sections, boiled potatoes, white rice, products made with white flour, oatmeal, cream of rice, cream of wheat, and farina. Drink 8-10 glasses on non-alcoholic, un-caffeinated fluid a day to prevent dehydration.
Trametinib can cause a heart problem called cardiomyopathy, which affects the heart muscle, making it weaker and less able to pump blood (called heart failure). Your healthcare provider will monitor for this problem with periodic heart scans (called MUGA scans), before and during treatment. If you develop shortness of breath, swelling in the legs, feet or ankles, irregular heartbeats, light-headedness or chest pain, notify your healthcare provider right away.
This medication may cause eye problems, including retinal pigment epithelial detachment and retinal vein occlusion. Symptoms of these conditions include blurry vision, loss or change in vision, seeing colored dots or halos (blurry outline around objects). If you develop any of these symptoms, notify your healthcare provider right away. You will be referred to an eye doctor for monitoring of these vision changes.
In a few cases, patients developed a rare lung problem called Interstitial Lung Disease (ILD) while receiving trametinib. Notify your healthcare team right away if you develop shortness of breath, new or worsening cough or have any difficulty breathing.
Exposure of an unborn child to this medication could cause birth defects, so you should not become pregnant or father a child while on this medication. Effective birth control is necessary during treatment and for at least 4 months after treatment. Even if your menstrual cycle stops or you believe you are not producing sperm, you could still be fertile and conceive. You should consult with your healthcare team before breastfeeding while receiving this medication.
Side Effects Seen When Taken With Dabrafenib
This medication is often given with another medication called dabrafenib. The following side effects were seen in studies of this combination, but not when trametinib was given alone. You should be aware of these side effects regardless if you are taking both medications or not.
New Skin Cancer
In clinical trials, some patients developed a new skin cancer (melanoma or squamous cell cancer). You should have skin examinations every 2 months while on therapy, and for 6 months after the medication has been stopped. Check your own skin regularly and report any new "warts", sores or bumps that bleed or do not heal, or notice any changes in moles to your healthcare provider.
These medications can increase the risk of blood clots in your arms, legs or lungs (DVT, pulmonary embolism or PE). Symptoms can include: swelling, redness, or pain in a leg or arm, chest pain or pressure, or shortness of breath. If you experience symptoms of these problems, you should contact your healthcare provider immediately or go to an emergency room.
These medications may increase the risk of bleeding. If you experience headaches, dizziness, cough up blood or blood clots, vomit blood or have red or black tar like looking stools, contact your care team immediately.
Fever can be a serious side effect of these medications. If you develop a fever of 101 or greater, call your healthcare team right away and before taking the next dose of medication.
High Blood Sugar
These medications can cause elevated blood sugar levels in patients with and without diabetes. Your healthcare team will monitor your blood sugar. If you develop increased thirst, urination or hunger, blurry vision, headaches or your breath smells like fruit, notify your healthcare team. Diabetics should monitor their blood sugar closely and report elevations to the healthcare team.