Mektovi (Binimetinib) – Melanoma | HongKong DengYue Medicine

Binimetinib Application Scope

• Used in combination with encorafenib (a BRAF inhibitor).
• Treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test.
• Treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation, as detected by an FDA-approved test.

Binimetinib Characteristics

• Ingredients: Binimetinib

• Properties:​ A kinase inhibitor, specifically a reversible inhibitor of mitogen-activated extracellular signal-related kinase 1 ($\text{MEK}1$) and $\text{MEK}2$ activity (antineoplastic/cancer medicine).

• Packaging Specification: ​15 mg × 84 tablets

• Storage:​ Store at room temperature, typically 20∘C to 25∘C (68∘F to 77∘F); excursions permitted between 15∘C and 30∘C (59∘F and 86∘F). Keep in a closed container, away from heat, moisture, and direct light. Keep from freezing.

• Expiry Date: Varies by batch and packaging.

• Executive Standard: ​ Varies by country’s regulatory authority. (e.g., FDA-approved label for MEKTOVI)

• Approval Number: Varies by country. (e.g., NDA 210498 in the US for MEKTOVI)

• Date of Revision: Varies by regulatory authority updates.

• Manufacturer: Array BioPharma Inc. (US Approval), now part of Pfizer.

Guidelines for the Use of Binimetinib

• Dosage and Administration:

  • Recommended Dose: $45\text{ mg}$ orally two times a day (twice daily), taken approximately $12$ hours apart. For patients with moderate or severe hepatic impairment, the recommended dose is $30\text{ mg}$ orally twice daily.

  • Administration: Take with or without food.

  • Missed Dose:​ If a dose is missed, do not take it if it is within $6$ hours of the next scheduled dose. Continue with the regular dosing schedule.

• Adverse Reactions:

  • Common Adverse Reactions: Fatigue, nausea, diarrhea, vomiting, abdominal pain, musculoskeletal pain, visual impairment (including serous retinopathy), constipation, dyspnea, rash, and cough (profile may vary slightly by indication).

  • Serious Adverse Reactions:​

    • Cardiomyopathy (Left Ventricular Dysfunction)
    • Venous Thromboembolism (Deep Vein Thrombosis and Pulmonary Embolism)
    • Ocular Toxicities (Serous Retinopathy/Retinal Pigment Epithelial Detachment, Retinal Vein Occlusion ($\text{RVO}$), Uveitis)
    • Pulmonary Effects (Interstitial Lung Disease/Pneumonitis)
    • Hepatotoxicity ($\text{AST}/\text{ALT}$ elevation)
    • Rhabdomyolysis ($\text{CPK}$ elevation)
    • New Primary Malignancies (cutaneous and non-cutaneous)
    • Hemorrhage (including major hemorrhagic events)

• Contraindications:

  • Known hypersensitivity to binimetinib or excipients.

  • Not recommended in pregnancy or breastfeeding.

• Precautions:

  • Assess Left Ventricular Ejection Fraction ($\text{LVEF}$) prior to initiation and monitor during treatment.
  • Monitor for New Primary Malignancies (cutaneous and non-cutaneous) before, during, and after treatment.
  • Monitor for signs of Hemorrhage and Venous Thromboembolism.
  • Perform Ophthalmologic Evaluation at regular intervals and for any visual disturbances.
  • Monitor Liver Function Tests ($\text{AST}/\text{ALT}$) monthly and as clinically indicated.
  • Monitor Creatine Phosphokinase ($\text{CPK}$) and Creatinine levels periodically.
  • Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for $30$ days after the final dose.
  • Lactation: Advise women not to breastfeed during treatment and for $3$ days after the final dose

Binimetinib Interactions

• Refer to the full prescribing information for a complete list. Binimetinib is primarily metabolized by glucuronidation ($\text{UGT}1\text{A}1$) and has minor metabolic pathways involving $\text{CYP}1\text{A}2$ and $\text{CYP}2\text{C}19$.
• Dose modification of binimetinib is not generally recommended when used with moderate $\text{UGT}1\text{A}1$ inhibitors (e.g., atazanavir) or gastric acid reducing agents (e.g., rabeprazole), as simulations suggest no clinically important effect on exposure.
• The manufacturer’s label does not list severe or serious drug interactions for binimetinib itself. However, the combination therapy with encorafenib (Braftovi) has significant drug-drug interactions involving $\text{CYP}3\text{A}4$ and $\text{CYP}2\text{C}8$ that must be considered and managed.

Note:

• If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
•  This content is for reference only. Prescription drugs must be used under a doctor’s guidance and purchased from authorized sources.