Mekinist

Generic name: trametinib
Drug class: Multikinase inhibitors

Medically reviewed by A Ras MD.

What is Mekinist used for?

Mekinist is used to treat skin cancer. It is used to treat lung cancer. Mekinist is also used to treat thyroid cancer.

Description

Trametinib dimethyl sulfoxide is a kinase inhibitor. The chemical name is acetamide, N-[3-[3-cyclopropyl-5-[(2-fluoro-4- iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl- 2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-, compound with 1,1’-sulfinylbis[methane] (1:1). It has a molecular formula C26H23FIN5O4•C2H6OS with a molecular mass of 693.53 g/mol. Trametinib dimethyl sulfoxide has the following chemical structure:

Trametinib dimethyl sulfoxide is a white to almost white powder. It is practically insoluble in the pH range of 2 to 8 in aqueous media.

MEKINIST (trametinib) tablets for oral use are supplied as 0.5 mg and 2 mg tablets for oral administration. Each 0.5 mg tablet contains 0.5635 mg trametinib dimethyl sulfoxide equivalent to 0.5 mg of trametinib non-solvated parent. Each 2 mg tablet contains 2.254 mg trametinib dimethyl sulfoxide equivalent to 2 mg of trametinib non-solvated parent.

The inactive ingredients of MEKINIST tablets are: Tablet Core: colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate (vegetable source), mannitol, microcrystalline cellulose, and sodium lauryl sulfate. Coating: hypromellose, iron oxide red (2 mg tablets), iron oxide yellow (0.5 mg tablets), polyethylene glycol, polysorbate 80 (2 mg tablets), and titanium dioxide.

Mechanism of Action

Trametinib is a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2. Trametinib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

Trametinib and dabrafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Use of trametinib and dabrafenib in combination resulted in greater growth inhibition of BRAF V600 mutation-positive tumor cell lines in vitro and prolonged inhibition of tumor growth in BRAF V600 mutation positive tumor xenografts compared with either drug alone.

Before taking Mekinist, tell your doctor:

If you are allergic to Mekinist; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
If you are breast-feeding. Do not breast-feed while you take Mekinist or for 4 months after your last dose.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take Mekinist with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take Mekinist?

Tell all of your health care providers that you take Mekinist. This includes your doctors, nurses, pharmacists, and dentists.
Sometimes, dabrafenib is taken with trametinib. If you are taking dabrafenib with trametinib, be sure you know the side effects that can happen with each drug. When these drugs are taken together, the chance of certain side effects may be raised. These side effects can be very bad and sometimes deadly. This includes bleeding, bleeding in the brain, blood clots, eye problems, fever, heart problems (like heart failure), high blood sugar, other cancers, and skin problems. Talk with your doctor about the chance of side effects with your drugs.
High blood pressure has happened with Mekinist. Have your blood pressure checked as you have been told by your doctor.
Have your eye pressure and eyesight checked as you have been told by the doctor.
Blood clots have happened with Mekinist. Tell your doctor if you have ever had a blood clot. Talk with your doctor.
Call your doctor right away if you have signs of a blood clot like chest pain or pressure; coughing up blood; shortness of breath; swelling, warmth, numbness, change of color, or pain in a leg or arm; or trouble speaking or swallowing.
It is common to get a rash with Mekinist but other skin reactions may also happen. Sometimes, these rashes and skin reactions can be very bad and may need treatment in the hospital. Call your doctor right away if you have acne, skin redness, or a skin rash that bothers you or does not go away. Call your doctor right away if you have redness or irritation of the palms of hands or soles of feet.
Very bad eye problems have happened with Mekinist. Sometimes, this has led to loss of eyesight. Call your doctor right away if you have blurred eyesight, loss of eyesight, or other changes in eyesight. Call your doctor right away if you see color dots or halos or if bright lights bother you.
A bowel problem (colitis) and holes in the bowel have happened with Mekinist. Sometimes, these have been deadly. Call your doctor right away if you have diarrhea, stomach pain or cramps, fever, or very upset stomach.
If you are 65 or older, use Mekinist with care. You could have more side effects.
This medicine may cause fertility problems. This may affect being able to have children. Talk with the doctor.
This medicine may cause harm to an unborn baby. A pregnancy test will be done before you start Mekinist to show that you are NOT pregnant.
Women must use birth control while taking Mekinist and for some time after the last dose. Ask your doctor how long to use birth control. If you get pregnant, call your doctor right away.
Men with a partner who is pregnant or may get pregnant must use a condom while taking Mekinist and for some time after the last dose. Use a condom even if you have had a vasectomy. Ask your doctor how long to use a condom. If your partner is pregnant or gets pregnant, call the doctor right away.

How is Mekinist best taken?

Use Mekinist as ordered by your doctor. Read all information given to you. Follow all instructions closely.

Take Mekinist at the same time of day.
Take on an empty stomach. Take 1 hour before or 2 hours after meals.
Keep taking Mekinist as you have been told by your doctor or other health care provider, even if you feel well.
Have blood work checked as you have been told by the doctor. Talk with the doctor.

What do I do if I miss a dose?

Take a missed dose as soon as you think about it.
If it is less than 12 hours until the next dose, skip the missed dose and go back to your normal time.
Do not take 2 doses at the same time or extra doses.

What are the side effects of Mekinist that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Signs of bleeding like throwing up or coughing up blood; vomit that looks like coffee grounds; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a cause or that get bigger; or bleeding you cannot stop.
Signs of lung or breathing problems like shortness of breath or other trouble breathing, cough, or fever.
Signs of fluid and electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, very bad dizziness or passing out, fast heartbeat, more thirst, seizures, feeling very tired or weak, not hungry, unable to pass urine or change in the amount of urine produced, dry mouth, dry eyes, or very bad upset stomach or throwing up.
Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.
Fever or chills.
Feeling very tired or weak.
This medicine may cause heart failure. You will need to have your heart function checked while taking Mekinist. Call your doctor right away if you have signs of heart problems like a cough or shortness of breath that is new or worse, swelling of the ankles or legs, a heartbeat that does not feel normal, weight gain of more than 5 pounds in 24 hours, dizziness, or passing out.

What are some other side effects of Mekinist?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

Dry skin.
Change in nails.
Mouth irritation or mouth sores.
Upset stomach or throwing up.
Feeling tired or weak.
Not hungry.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out Mekinist?

Store in a refrigerator. Do not freeze.
Keep tablets in the bottle they come in and do not move to a pill holder.
Store in the original container. Do not take out the antimoisture cube or packet.
Protect from light.
Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.