Binimetinib

What is Binimetinib?[edit | edit source]

Binimetinib (Mektovi) is a kinase inhibitor used in combination with a medicine called encorafenib to treat people with a type of skin cancer called melanoma.

Binimetinib

Binimetinib Structural Formula V1

What are the uses of this medicine?[edit | edit source]

This medicine is used in combination with a medicine called encorafenib to treat people with a type of skin cancer called melanoma:

that has spread to other parts of the body or cannot be removed by surgery, and
that has a certain type of abnormal "BRAF" gene

How does this medicine work?[edit | edit source]

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.

Who Should Not Use this medicine ?[edit | edit source]

This medicine have no usage limittations.

What drug interactions can this medicine cause?[edit | edit source]

No clinically important drug interactions have been observed with Mektovi.

Is this medicine FDA approved?[edit | edit source]

It was approved for use in the United States in 2018.

How should this medicine be used?[edit | edit source]

Confirm the presence of a BRAF V600E or V600K mutation in tumor specimens prior to initiating Mektovi.

Recommended Dosage

The recommended dosage of Mektovi is 45 mg orally taken twice daily, approximately 12 hours apart, in combination with encorafenib until disease progression or unacceptable toxicity.

Dosage Modifications for Moderate or Severe Hepatic Impairment

For patients with moderate or severe hepatic impairment the recommended dose is 30 mg orally twice daily.

Administration

Take Mektovi exactly as your healthcare provider tells you to take it. Do not change your dose or stop taking Mektovi unless your healthcare provider tells you to.
Your healthcare provider may change your dose of Mektovi, temporarily stop, or completely stop your treatment with Mektovi if you develop certain side effects.
Take Mektovi in combination with encorafenib by mouth 2 times a day, about 12 hours apart.
Mektovi may be taken with or without food.
If you miss a dose of Mektovi, take it as soon as you remember. If it is within 6 hours of your next scheduled dose, take your next dose at your regular time. Do not make up for the missed dose.
Do not take an extra dose if you vomit after taking your scheduled dose. Take your next dose at your regular time.
If you stop treatment with encorafenib, talk to your healthcare provider about whether your Mektovi treatment may need to be stopped.

What are the dosage forms and brand names of this medicine?[edit | edit source]

This medicine is available in fallowing doasage form:

As Tablets: 15 mg

This medicine is available in fallowing brand namesː

Mektovi

What side effects can this medication cause?[edit | edit source]

The most common side effects of this medicine include:

fatigue
nausea
diarrhea
vomiting
abdominal pain

Mektovi may cause serious side effects, including:

Heart problems, including heart failure
Blood clots
Eye problems
Lung or breathing problems
Liver problems
Muscle problems (rhabdomyolysis)
Bleeding problems

What special precautions should I follow?[edit | edit source]

Assess left ventricular ejection fraction (LVEF) before initiating treatment, after one month of treatment, then every 2 to 3 months thereafter. The safety of Mektovi has not been established in patients with LVEF below 50%.
Deep vein thrombosis and pulmonary embolism can occur with Mektovi.
Serous retinopathy, retinal vein occlusion (RVO) and uveitis have occurred. Perform an ophthalmologic evaluation at regular intervals and for any visual disturbances.
Assess new or progressive unexplained pulmonary symptoms or findings for possible Interstitial Lung Disease (ILD).
This medicine may cause hepatotoxicity. Monitor liver function tests before and during treatment and as clinically indicated.
Rhabdomyolysis may occur. Monitor creatine phosphokinase and creatinine periodically and as clinically indicated.
Major hemorrhagic events can occur with Mektovi.
Mektovi Can cause fetal harm. Advise females with reproductive potential of potential risk to the fetus and to use effective contraception.

What to do in case of emergency/overdose?[edit | edit source]

Management for overdosage:

Since binimetinib is 97% bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with Mektovi.

Can this medicine be used in pregnancy?[edit | edit source]

Based on findings from animal reproduction studies and its mechanism of action, Mektovi can cause fetal harm when administered to a pregnant woman.
There are no available clinical data on the use of Mektovi during pregnancy.

Can this medicine be used in children?[edit | edit source]

The safety and effectiveness of Mektovi have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?[edit | edit source]

Active ingredient: binimetinib
Inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate (vegetable source), and colloidal silicon dioxide
Tablet coating: polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, ferric oxide yellow, ferrosoferric oxide

Who manufactures and distributes this medicine?[edit | edit source]

Distributed by: Array BioPharma Inc., a wholly owned subsidiary of Pfizer Inc., Boulder, Colorado 80301.
Mektovi® is a registered trademark of Array BioPharma Inc. in the United States and various other countries.

What should I know about storage and disposal of this medication?[edit | edit source]

Store Mektovi at room temperature between 68°F to 77°F (20°C to 25°C).
Keep Mektovi and all medicines out of the reach of children.

Binimetinib Resources
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