Trade name: Mekinist
Trametinib is the generic name for the trade name chemotherapy drug Mekinist. In some cases, health care professionals may use the trade name Mekinist when
referring to the generic name trametinib.
Trametinib is a targeted therapy. It is an oral MEK inhibitor - (For more detail, see "How this drug works," below.)
trametinib is used for:
- For the treatment of unresectable or metastatic melanoma that is caused by a defect in a gene called BRAF. The cancer must be (BRAF)-positive as
indicated by an FDA-approved test.
Note: If a drug has been approved for one use, physicians may elect to use this same drug for other problems if they believe it may be helpful.
trametinib is given:
- Trametinib is a pill, taken by mouth, once daily. Take at least 1 hour before or 2 hours after a meal.
- Take trametinib exactly as prescribed.
- Swallow trametinib tablets whole. Do not crush or dissolve tablets.
- Do not change your dose or stop trametinib unless your health care provider tells you to.
- If you miss a dose, take it as soon as you remember. If it has been 12 hours or more since the missed dose, skip the missed dose and go back to your
- Do not take more than 1 dose of trametinib at one time. Call your health care provider right away if you take too much.
- Store trametinib in the refrigerator between 36°F to 46°F, not the freezer.
- Keep tablets in the bottle they came in and do not move to a pill holder.
- Store in the original container. Do not remove the anti-moisture packet. Protect from light.
- Keep medication away from children and pets.
- The amount of trametinib that you will receive depends on many factors, your general health or other health problems, and the type of cancer or condition
being treated. Current recommendation is for one tablet twice daily, higher doses do not always give a better response and may cause increased toxicity.
Your doctor will determine your dose and schedule.
Important things to remember about the side effects of trametinib:
- Most people do not experience all of the side effects listed.
- Side effects are often predictable in terms of their onset and duration.
- Side effects are almost always reversible and will go away after treatment is complete.
- There are many options to help minimize or prevent side effects.
- There is no relationship between the presence or severity of side effects and the effectiveness of the medication.
The following side effects are common (occurring in greater than 30%) for patients taking
These side effects are less common side effects (occurring in about 10-29%) of patients receiving
Not all side effects are listed above. Some that are rare (occurring in less than 10% of patients) are not listed here. However, you should always
inform your health care provider if you experience any unusual symptoms.
When to contact your doctor or health care provider:
Contact your health care provider and/or go to the emergency room
, day or night, if you should experience any of the following symptoms:
- Fever of 100.4° F (38° or higher, chills)
- Signs of a reaction to the medication (wheezing; chest tightness; fever; itching; hives; bad cough; blue or grey skin color; seizures; or swelling of the
face, lips, tongue or throat)
Always inform your health care provider if you experience any unusual symptoms.
The following symptoms require medical attention, but are not an emergency. Contact your health care provider
within 24 hours
of noticing any of the following:
- Diarrhea (4-6 episodes in a 24-hour period)
- Nausea (interferes with ability to eat and unrelieved with prescribed medication)
- Vomiting (vomiting more than 4-5 times in a 24 hour period)
- Unable to eat or drink for 24 hours or have signs of dehydration: tiredness, thirst, dry mouth, dark and decrease amount of urine, or dizziness
- Skin wound that will not heal
- Change in eyesight (blurred vision, loss of vision, seeing colored dots/halos, or other visual changes)
- Onset of shortness of breath
- Fast heartbeat
- Very bad headache
- Very bad dizziness or passing out
- Cough with or without mucus
- Swelling or pain of hands or feet
- Change in color or size of a mole
- Any skin change, irritation, itching or rash
- Any bruising or bleeding
Always inform your health care provider if you experience any unusual symptoms.
- Before starting trametinib treatment, make sure you tell your doctor about any other medications you are taking (including prescription,
over-the-counter, vitamins, herbal remedies, etc.).
- Do not receive any kind of immunization or vaccination without your doctor's approval while taking trametinib.
- Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. trametinib is pregnancy category D, should
not be taken during pregnancy and may be hazardous to the fetus. Women who are pregnant or become pregnant must be advised of the potential hazard to the
- For both men and women: Do not conceive a child (get pregnant) while taking trametinib. Barrier methods of contraception, such as condoms, are
recommended during therapy and for 4 months after treatment is complete. Discuss with your doctor when you may safely become pregnant or conceive a child
- Do not breast feed while taking this medication.
- Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.
- If you should experience nausea, take anti-nausea medications as prescribed by your doctor, and eat small frequent meals. Sucking on lozenges and chewing
gum may also help.
- Avoid sun exposure. Wear SPF 15 (or higher) sun block and protective clothing.
- In general, drinking alcoholic beverages should be kept to a minimum or avoided completely. You should discuss this with your doctor.
- Get plenty of rest.
- Maintain good nutrition.
- If you have any changes, dizziness and tiredness use caution when driving a car, using machinery, or anything that requires you to be alert.
- If you experience symptoms or side effects, be sure to discuss them with your health care team. They can prescribe medications and/or offer other
suggestions that are effective in managing such problems.
Monitoring and testing:
You will be checked regularly by your health care professional with blood work, cardiac evaluations and skin examinations while you are taking trametinib
to monitor side effects and check your response to therapy.
How this drug works:
Targeted therapy is the result of about 100 years of research dedicated to understanding the differences between cancer cells and normal cells. To date,
cancer treatment has focused primarily on killing rapidly dividing cells because one feature of cancer cells is that they divide rapidly. Unfortunately,
some of our normal cells divide rapidly too, causing multiple side effects.
Targeted therapy is about identifying other features of cancer cells. Scientists look for specific differences in the cancer cells and the normal cells.
This information is used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects.
Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or
communicate with other cells.
There are different types of targeted therapies, defined in three broad categories. Some targeted therapies focus on the internal components and function
of the cancer cell. The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die. There
are several types of targeted therapy that focus on the inner parts of the cells. Other targeted therapies target receptors that are on the outside of the
cell. Therapies that target receptors are also known as monoclonal antibodies. Antiangiogenesis inhibitors target the blood vessels that supply oxygen to
the cells, ultimately causing the cells to starve.
Trametinib is a targeted therapy that targets the MEK 1 and MEK 2 protein (kinase) within the cancer cell. It is usually given in combination with a BRAF kinase inhibitor.
The BRAF gene plays an important role in both normal and cancer cells. This gene leads to the production of BRAF protein. This protein is normally part of a chain of molecules that relay a signal that tells cells how to grow and divide. A change in the BRAF gene (called a mutation) can alter the way that the BRAF protein works. Instead of waiting for its turn to signal a cell to divide or grow, the BRAF protein is out of control and signals all of the time, this out of control BRAF signaling may drive the uncontrolled growth of cancer cells. MEK1-2 are proteins further down the chain of molecules in this pathway. Trametinib interferes with the signal at the MEK 1-2 part of the chain, this interference may cause a slowdown in the growth of cancer.
We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in
this website is meant to be helpful and educational, but is not a substitute for medical advice