Trametinib

Non-Small-Cell Lung Carcinoma, Melanoma

Drug Status

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Government Approvals

US(FDA), UK(BNF)

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WHO Essential Medicine

NO

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Known Teratogen

Definite

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Pharmaceutical Class

Kinase Inhibitor

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Controlled Drug Substance

NO

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Drug Ingredient

Trametinib

Summary

  • Trametinib is used to treat certain types of skin melanoma and lung cancer that have a specific genetic mutation (BRAF V600E or V600K). It can also be used for thyroid cancer in some cases, usually in combination with another drug called dabrafenib.

  • Trametinib works by blocking proteins called MEK1 and MEK2. These proteins play a role in cell growth and division. By inhibiting these proteins, Trametinib helps to slow down the growth and spread of cancer cells.

  • The usual dose for adults is 2 mg once daily, taken on an empty stomach. The tablet should be swallowed whole with water, without crushing, chewing, or breaking it. Always follow your doctor's instructions for the correct dosage.

  • Common side effects of Trametinib include rash, diarrhea, fatigue, high blood pressure, and fever. Serious risks include heart failure, vision loss, lung inflammation, and severe skin reactions.

  • Trametinib should be avoided by people allergic to it, those with severe heart or lung disease, pregnant women, and those with active bleeding disorders due to potential risks and side effects. Always consult your doctor before starting this medication.

Indications and Purpose

How does Trametinib work?

Trametinib is a MEK inhibitor that blocks the MEK1 and MEK2 proteins, preventing cancer cells from growing and spreading. This helps slow down tumor progression in BRAF-mutant cancers. It is particularly effective when combined with dabrafenib, which targets the BRAF protein.

Is Trametinib effective?

Yes, clinical trials show that trametinib, especially when combined with dabrafenib, significantly improves progression-free survival in patients with BRAF-mutant melanoma and lung cancer. Studies indicate that it reduces tumor growth and extends patient survival compared to chemotherapy alone.

What is Trametinib?

Trametinib is a targeted therapy used to treat certain types of skin (melanoma) and lung cancer. It works by inhibiting the MEK1 and MEK2 proteins, which are involved in cell growth and division. This helps slow the spread of cancer cells. It is often used in combination with dabrafenib for better effectiveness.

Directions for Use

For how long do I take Trametinib?

The duration of treatment depends on your condition and response to therapy. Trametinib is usually taken as long as it remains effective or until side effects become too severe. Your doctor will monitor your progress with regular blood tests and imaging scans to decide how long you should continue treatment.

How do I take Trametinib?

Take trametinib once daily on an empty stomach, at least 1 hour before or 2 hours after a meal. Swallow the tablet whole with water. Do not crush, chew, or break the tablet. Avoid grapefruit or grapefruit juice, as it may interfere with the drug’s effectiveness.

How long does it take for Trametinib to start working?

Trametinib starts working within a few days to weeks, but noticeable improvements in cancer symptoms may take a few months. The effectiveness is assessed through regular scans and blood tests. Some patients experience relief from symptoms like tumor-related pain and fatigue within a few weeks.

How should I store Trametinib?

Store trametinib in the refrigerator (2°C - 8°C / 36°F - 46°F). Do not freeze. Keep it in the original packaging to protect it from light and moisture. Do not use expired tablets.

What is the usual dose of Trametinib?

The usual dose for adults is 2 mg once daily, taken on an empty stomach. For children, its use is not common, and dosing is determined by the doctor. The dose may be adjusted based on side effects, body weight, or other medications being used. Always follow your doctor’s instructions for the correct dosage.

Warnings and Precautions

Can I take Trametinib with other prescription drugs?

Trametinib may interact with:

  • Blood thinners (warfarin, aspirin) – increased bleeding risk
  • CYP3A4 inhibitors (ketoconazole, clarithromycin) – increased trametinib levels
  • Immunosuppressants (tacrolimus, cyclosporine) – unpredictable effects

Tell your doctor about all medications you are taking before starting trametinib.

Can Trametinib be taken safely while breastfeeding?

No. Trametinib can pass into breast milk and may harm the baby. Women should not breastfeed while taking this medicine and for at least 4 months after stopping treatment.

Can Trametinib be taken safely while pregnant?

No. Trametinib can cause severe birth defects or fetal harm. Women must use effective birth control during treatment and for 4 months after stopping the medication. If pregnancy occurs, contact your doctor immediately.

Is it safe to drink alcohol while taking Trametinib?

It is not recommended to drink alcohol while taking trametinib. Alcohol may increase dizziness, fatigue, and liver toxicity. Since trametinib can already cause liver issues, drinking alcohol may worsen these effects. If you consume alcohol, do so in moderation and consult your doctor about possible risks.

Is it safe to exercise while taking Trametinib?

Yes, light to moderate exercise is safe and even beneficial while taking trametinib. However, intense workouts may be too exhausting, especially if you experience fatigue, dizziness, or weakness. Gentle activities like walking, yoga, or stretching can help maintain muscle strength and overall well-being. Always listen to your body and consult your doctor before starting a new exercise routine.

Is Trametinib safe for the elderly?

Elderly patients may experience increased side effects, such as high blood pressure, fatigue, and swelling. Dose adjustments may be needed, and kidney or liver function monitoring is recommended.

Who should avoid taking Trametinib?

People who should avoid trametinib include:

  • Those allergic to trametinib
  • Patients with severe heart or lung disease
  • Pregnant women (due to risk of birth defects)
  • Those with active bleeding disorders

Your doctor will assess your medical history before prescribing trametinib.