Mekinist (Trametinib) – Melanoma | DengYue Medicine

Mekinist Application Scope

Mekinist is a once-daily oral MEK inhibitor used to treat various BRAF V600E/K-positive cancers.

Characteristics

• Ingredients: Trametinib

• Properties:

  • A kinase inhibitor that disrupts the MAPK/ERK pathway

  • Oral bioavailability is approximately 72%

  • Time to peak ~1.5 hours; half-life ~3.9–4.8 days

• Packaging Specification:

  • Tablets: 30-count bottles of 0.5 mg, 1 mg, or 2 mg

  • Pediatric solution: single-use 4.7 mg vials (powder to reconstitute)

• Storage: Store tablets below 25 °C; keep solution under 25 °C once reconstituted; do not freeze

• Expiry Date: As per package/bottle; typically 2 years from manufacture—check carton.

• Executive Standard:

  • U.S. FDA approved (first approved in 2013 with updates through 2025)

  • complies with EMA and TGA product standards.

• Approval Number: U.S. NDA 204114, sNDA updates (e.g., s-001, s-031)

• Date of Revision:

  • U.S. prescribing info revised April 2025

  • Oral solution guide revised March 2025

• Manufacturer: Novartis Pharmaceuticals.

Guidelines for the Use of Mekinist

• Dosage and Administration:

  • Adults: 2 mg once daily orally (tablets or solution) until progression or intolerance

  • Pediatrics (≥1 year and ≥26 kg): weight-based tablet/solution dosing

  • With dabrafenib, the usual dose is 150 mg BID

  • Dose modifications:

    • hold or reduce based on the severity of side effects, such as fever

    • skin toxicity, cardiomyopathy, ocular events, ILD

    • permanently discontinue for life-threatening reactions

 

• Adverse Reactions:

  • Common (≥20%):

    • rash, diarrhea, edema, fever (especially with dabrafenib)

    • nausea, chills, hypertension, vomiting, fatigue, headache.

  • Serious:

    • skin toxicities including SCARs/SJS/DRESS; ILD/pneumonitis; cardiomyopathy

    • ocular events (RPED, RVO); febrile reactions; hemorrhage;

    • GI perforation, thromboembolism, pancreatitis, hepatic events, HLH.

• Contraindications: Known hypersensitivity to trametinib or any component.

• Precautions:

  • Monitor cardiac function (LVEF), liver enzymes, and blood pressure

  • Glucose in diabetics, eye exam for ocular symptoms, pulmonary (ILD), and skin.

  • Avoid in pregnancy (teratogenic); counsel on contraception and reproductive toxicity.

  • Caution with hepatic impairment; insufficient data in severe renal impairment.

Mekinist Interactions

• Drug Interactions:

  • Use with dabrafenib: increased risk of fever, hemorrhage, etc.

  • Adjust both drugs per the guidelines.

  • Metabolism via hepatic/biliary route; caution with CYP inhibitors/inducers.

  • Possible interactions affecting warfarin, hormone contraceptives

  • Corticosteroids, hypoglycemics—monitor accordingly.

Note:

• If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
• It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.