MEKINIST 0.5 MG 30 TB

MEKINIST (Trametinib) is a targeted cancer therapy used primarily for the treatment of certain types of melanoma, non-small cell lung cancer (NSCLC), and anaplastic thyroid cancer. It is specifically indicated for cancers that have mutations in the BRAF gene, which lead to uncontrolled cell growth. MEKINIST is often used in combination with another targeted therapy, dabrafenib (Tafinlar), to enhance its effectiveness. MEKINIST is classified as a MEK inhibitor, which blocks specific proteins involved in the MAPK/ERK signaling pathway, critical for the proliferation and survival of cancer cells.

How MEKINIST Works

Mechanism of Action

1. Inhibition of MEK1 and MEK2:
   • MEKINIST is a selective inhibitor of mitogen-activated extracellular signal-regulated kinase (MEK) 1 and MEK 2, which are key components of the MAPK/ERK pathway. This pathway is often abnormally activated in cancers with BRAF mutations, driving tumor growth and survival.
2. Blocking Abnormal Cell Growth:
   • By inhibiting MEK1 and MEK2, MEKINIST prevents the phosphorylation and activation of ERK proteins, which in turn stops the transmission of growth signals within cancer cells. This inhibition leads to reduced tumor cell proliferation and can trigger cell death.
3. Targeting BRAF-Mutant Tumors:
   • MEKINIST is particularly effective against tumors harboring the BRAF V600E or V600K mutations. These mutations result in continuous activation of the MAPK/ERK pathway, making MEK inhibition an effective strategy to curb cancer progression.
4. Combination Therapy:
   • When used in combination with dabrafenib, a BRAF inhibitor, MEKINIST provides a more comprehensive blockade of the MAPK/ERK pathway, leading to improved treatment outcomes compared to using either drug alone.

Side Effects

Common Side Effects

• Rash:
  • Skin rashes are common, often appearing as acneiform eruptions, and can be mild to severe.
• Diarrhea:
  • Frequent loose stools, which may require dose adjustments or supportive care.
• Fatigue:
  • Patients often experience tiredness and lack of energy during treatment.
• Edema:
  • Swelling, especially in the legs, ankles, and feet, due to fluid retention.
• Nausea and Vomiting:
  • Gastrointestinal disturbances, which can often be managed with antiemetic medications.
• Hypertension:
  • Elevated blood pressure is a potential side effect that needs regular monitoring.
• Dry Skin and Pruritus:
  • Skin dryness and itching are commonly reported, requiring topical treatments.
• Fever:
  • Fever is more common when MEKINIST is used in combination with dabrafenib.

Serious Side Effects

• Cardiomyopathy:
  • MEKINIST can cause heart problems, including decreased heart function, necessitating regular cardiac monitoring.
• Retinal Vein Occlusion (RVO) and Retinal Pigment Epithelial Detachment (RPED):
  • Serious eye problems that can lead to visual disturbances or loss of vision.
• Interstitial Lung Disease (ILD):
  • Inflammation of lung tissue can cause cough, shortness of breath, and other respiratory symptoms.
• Hemorrhage:
  • Severe bleeding events, including gastrointestinal and intracranial hemorrhages.
• Serious Skin Reactions:
  • Severe skin reactions, including Stevens-Johnson syndrome, which can be life-threatening.
• Secondary Cancers:
  • Rarely, MEKINIST may be associated with the development of other types of cancers, such as cutaneous squamous cell carcinoma.

Indications

MEKINIST is indicated for:

• Unresectable or Metastatic Melanoma:
  • For the treatment of patients with BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma, used as monotherapy or in combination with dabrafenib.
• Non-Small Cell Lung Cancer (NSCLC):
  • In combination with dabrafenib, MEKINIST is indicated for patients with BRAF V600E mutation-positive metastatic NSCLC.
• Anaplastic Thyroid Cancer:
  • For the treatment of patients with locally advanced or metastatic anaplastic thyroid cancer with BRAF V600E mutations and who have no satisfactory locoregional treatment options.

Contraindications

MEKINIST is contraindicated in the following situations:

• Hypersensitivity:
  • Patients with known hypersensitivity to trametinib or any component of the formulation.
• Concurrent Use with Other MEK Inhibitors:
  • MEKINIST should not be used with other MEK inhibitors, except in specifically approved combinations like with dabrafenib.
• Severe Cardiovascular Disease:
  • Patients with severe or uncontrolled heart conditions, such as recent heart attack or severe heart failure.
• Severe Ocular Conditions:
  • Not recommended in patients with significant eye disorders, particularly those affecting the retina.
• Pregnancy and Breastfeeding:
  • MEKINIST can cause fetal harm and is contraindicated during pregnancy. It should not be used during breastfeeding due to potential risks to the infant.

Price in Different Countries

The cost of MEKINIST varies across countries, influenced by healthcare systems, local regulations, and insurance coverage. Below is an approximate price list for MEKINIST 2 mg 30 TB in various countries.

Country	Price (Per 2 mg Tablet)	Reference
United States	$8,000 – $10,000	GoodRx
United Kingdom	£6,500 – £8,500	NHS UK
Canada	CAD $10,000 – $12,000	Canada Drugs
Australia	AUD $12,000 – $14,000	PBS Australia
India	₹550,000 – ₹700,000	1mg

Top 5 Global Brands

1. MEKINIST – Novartis:
   • The original and most widely recognized brand, MEKINIST by Novartis is extensively used for treating BRAF-mutant cancers, especially melanoma.
2. Tafinlar + Mekinist Combination – Novartis:
   • This combination of dabrafenib (Tafinlar) and trametinib (Mekinist) is marketed together by Novartis for enhanced efficacy in BRAF V600 mutation-positive cancers.
3. Trametinib – Generic Versions:
   • Several generic versions are becoming available as patents expire, offering more affordable options for patients worldwide.
4. GSK Mekinist – GlaxoSmithKline:
   • Initially developed by GlaxoSmithKline, MEKINIST was later acquired by Novartis, but GSK continues to be a key player in the drug’s development history.
5. Other Biosimilars:
   • As MEKINIST’s exclusivity expires, biosimilar versions are being developed by pharmaceutical companies globally, making the drug more accessible.