Mektovi (Tablets) Instructions for Use

Marketing Authorization Holder

Pierre Fabre Medicament (France)

Manufactured By

Almac Pharma Services, Limited (United Kingdom)

ATC Code

L01EE03 (Binimetinib)

Active Substance

Binimetinib (Prop.INN)

Dosage Form

Mektovi

Film-coated tablets 15 mg: 84 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets

12 pcs. – blisters (7 pcs.) – cardboard packs (84 pcs.) – By prescription

Pharmacotherapeutic Group

Antineoplastic agents, protein kinase inhibitors, mitogen-activated protein kinase (MEK) inhibitors

Pharmacological Action

Antineoplastic agent, protein kinase inhibitor, mitogen-activated protein kinase (MEK) inhibitor. Defects (mutations) in the BRAF gene can lead to the production of specific proteins that stimulate melanoma growth.

Binimetinib targets another protein – MEK, which also stimulates the growth of tumor cells. When Binimetinib is used in combination with encorafenib (which targets the mutated BRAF protein), this combination slows or stops the growth of tumor cells.

Indications

Treatment of melanoma in adult patients over 18 years of age with a mutation in the gene responsible for the production of the BRAF protein, with involvement of other organs and systems or when the tumor cannot be removed surgically.

ICD codes

Dosage Regimen

Take orally.

The recommended dose is 45 mg twice daily at approximately 12-hour intervals.

Administer in combination with encorafenib.

Take with or without food. Swallow tablets whole with water; do not chew or crush.

If a dose is vomited, do not take an additional dose; resume the next scheduled dose.

If a dose is missed by more than 6 hours, skip the dose and resume the next scheduled dose.

Perform dose modifications for adverse reactions based on severity.

For specific adverse reactions, the first dose reduction is to 30 mg twice daily.

The second dose reduction is to 15 mg twice daily.

Permanently discontinue therapy if unable to tolerate 15 mg twice daily.

Withhold, dose reduce, or permanently discontinue based on clinical assessment of severity.

Monitor patients closely for new primary malignancies, hemorrhage, cardiomyopathy, ocular toxicities, and rhabdomyolysis.

Adverse Reactions

From the cardiovascular system very common – increased blood pressure; common – decreased left ventricular ejection fraction (possible symptoms – feeling of dizziness, fatigue or unsteadiness, shortness of breath, palpitations, arrhythmia, swelling of the legs), venous thromboembolism, including pulmonary embolism (symptoms – chest pain, sudden shortness of breath or difficulty breathing, leg pain with or without swelling, swelling in the arms and legs, decreased temperature of the skin of the hands and feet).

From the organ of vision very common – retinal pigment epithelial detachment, blurred vision, vision loss.

From the blood coagulation system very common – bleeding of various locations (symptoms – headaches, dizziness or weakness, coughing up blood or blood clots, vomiting blood or resembling “coffee grounds”, red or black stools, blood in the urine, abdominal pain (in the stomach area), abnormal vaginal bleeding).

From the skin and subcutaneous tissues common – cutaneous squamous cell carcinoma.

From the musculoskeletal system uncommon – rhabdomyolysis (symptoms – muscle pain, cramps, stiffness or spasms, dark urine), which can lead to kidney damage and cause serious complications.

Adverse reactions that may occur when used in combination with encorafenib should be taken into account.

Contraindications

Hypersensitivity to binimetinib, pregnancy, breastfeeding period.

With caution

Heart disease, blood clotting disorders, eye diseases (including glaucoma, increased intraocular pressure), muscle pain, arterial hypotension, tendency to thrombosis, respiratory system disorders, liver function disorders, while taking drugs that can cause bleeding, history of retinal vein occlusion (use is not recommended), history of other malignant neoplasms.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Special Precautions

Before starting treatment and during binimetinib administration, the function of the cardiovascular system should be monitored, regular ophthalmological examination should be performed, indicators of the blood coagulation system, biochemical blood parameters for the timely detection of rhabdomyolysis development, lung condition; liver function status should be monitored.

Binimetinib in combination with encorafenib can cause the development of other malignant skin neoplasms, including cutaneous squamous cell carcinoma. New melanomas may also occur while taking binimetinib. The skin condition should be examined before treatment and then monitored every 2 months during and for 6 months after completion of treatment. The development of squamous cell carcinoma on the head, neck, in the mouth and in the lymph nodes should be excluded, so patients should regularly undergo computed tomography. Before and after completion of treatment, it is also recommended to examine the external genitalia (in women) and the anus.

Use in pediatrics

Should not be used in children and adolescents under 18 years of age, as the efficacy and safety of binimetinib have not been established in this category of patients.

Effect on the ability to drive vehicles and mechanisms

During treatment, the patient should avoid driving or working with machinery if any visual disturbances or other side effects occur that may affect the ability to drive a car or operate technical devices.

Drug Interactions

Adverse reactions may develop with simultaneous use with the following medications: rifampicin, ciprofloxacin; phenobarbital, phenytoin, carbamazepine; indinavir, atazanavir; sorafenib; St. John’s wort preparations; duloxetine; pravastatin; theophylline.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.