What is Mektovi used for?
Mektovi is a prescription medicine that is used to treat a type of skin cancer (melanoma).
Binimetinib is a kinase inhibitor. The chemical name is 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide. The molecular formula is C17H15BrF2N4O3 and the molecular weight is 441.2 daltons. The chemical structure of binimetinib is shown below:
Binimetinib is a white to slightly yellow powder. In aqueous media, binimetinib is slightly soluble at pH 1, very slightly soluble at pH 2, and practically insoluble at pH 4.5 and higher.
MEKTOVI (binimetinib) tablets for oral use contain 15 mg of binimetinib with the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate (vegetable source), and colloidal silicon dioxide. The coating contains polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, ferric oxide yellow, and ferrosoferric oxide.
Mechanism of Action
Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cell-free assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models.
Binimetinib and encorafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Compared to either drug alone, coadministration of encorafenib and binimetinib resulted in greater anti-proliferative activity in vitro in BRAF mutation-positive cell lines and greater anti-tumor activity with respect to tumor growth inhibition in BRAF V600E mutant human melanoma xenograft studies in mice. Additionally, the combination of binimetinib and encorafenib delayed the emergence of resistance in BRAF V600E mutant human melanoma xenografts in mice compared to either drug alone.
Before taking Mektovi, tell your doctor:
- If you are allergic to Mektovi; 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 Mektovi and for at least 3 days 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 Mektovi 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 Mektovi?
- Tell all of your health care providers that you take Mektovi. This includes your doctors, nurses, pharmacists, and dentists.
- Encorafenib is taken with binimetinib. Be sure you know about the warnings, benefits, and risks of each drug. Talk with your doctor if you have questions or concerns about these drugs.
- Very bad bleeding problems have happened when encorafenib was taken with binimetinib. This includes bleeding in the stomach or brain. Sometimes, these bleeding problems have been deadly. If you have any questions, talk with your doctor.
- High blood pressure has happened with Mektovi. Have your blood pressure checked as you have been told by your doctor.
- Have blood work checked as you have been told by the doctor. Talk with the doctor.
- Blood clots have happened with Mektovi. 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.
- Very bad eye problems have happened with Mektovi. 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.
- Have an eye exam as you have been told by your doctor.
- This medicine may cause harm to the unborn baby if you take it while you are pregnant.
- If you are able to get pregnant, a pregnancy test will be done to show that you are NOT pregnant before starting Mektovi. Talk with your doctor.
- Use birth control that you can trust to prevent pregnancy while taking Mektovi and for at least 1 month after stopping Mektovi.
- If you get pregnant while taking Mektovi or within 1 month after your last dose, call your doctor right away.
How is Mektovi best taken?
Use Mektovi as ordered by your doctor. Read all information given to you. Follow all instructions closely.
- Take with or without food.
- Keep taking Mektovi as you have been told by your doctor or other health care provider, even if you feel well.
- If you throw up after taking a dose, do not repeat the dose. Take your next dose at your normal time.
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 6 hours until the next dose, skip the missed dose and go back to the normal time.
- Do not take 2 doses at the same time or extra doses.
What are the side effects of Mektovi 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 high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
- Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
- Signs of low sodium levels like headache, trouble focusing, memory problems, feeling confused, weakness, seizures, or change in balance.
- Fever or chills.
- Feeling very tired or weak.
- Muscle pain or weakness.
- Dark urine.
- Eye pain, swelling, or redness.
- Very bad headache.
- This medicine may cause heart failure. You will need to have your heart function checked while taking Mektovi. 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 Mektovi?
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:
- Feeling tired or weak.
- Belly pain.
- Constipation, diarrhea, throwing up, and upset stomach are common with Mektovi. If these happen, talk with your doctor about ways to lower these side effects. Call your doctor right away if any of these effects bother you, do not go away, or get very bad.
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 Mektovi?
- Store at room temperature.
- Store in a dry place. Do not store in a bathroom.
- 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.
PRINCIPAL DISPLAY PANEL – 15 MG TABLET BOTTLE LABEL
- NDC 70255-010-02
- 15 mg
- Rx only
- 180 Tablets
PRINCIPAL DISPLAY PANEL – 15 MG TABLET BOTTLE CARTON
- NDC 70255-010-02
- 15 mg
- Rx only
- 180 Tablets
SRC: NLM .