Trametinib

What is Trametinib?

• Trametinib (Mekinist) is a kinase inhibitor used alone or in combination with a medicine called dabrafenib to treat a type of skin cancer called melanoma.

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What are the uses of this medicine?

This medicine is used: alone or in combination with a medicine called dabrafenib to treat a type of skin cancer called melanoma:

• that has spread to other parts of the body or cannot be removed by surgery, and
• that has a certain type of abnormal “BRAF” gene.

In combination with dabrafenib, to help prevent melanoma that has a certain type of abnormal “BRAF” gene from coming back after the cancer has been removed by surgery. Mekinist should not be used to treat people who already have received a BRAF inhibitor for treatment of their melanoma, and it did not work or is no longer working.

In combination with dabrafenib to treat a type of lung cancer called non-small cell lung cancer (NSCLC)

• that has spread to other parts of the body, and
• that has a certain type of abnormal “BRAF” gene.

in combination with dabrafenib to treat a type of thyroid cancer called anaplastic thyroid cancer (ATC)

• that has spread to other parts of the body and you have no satisfactory treatment options, and
• that has a certain type of abnormal “BRAF” gene.

How does this medicine work?

• Trametinib (tra me’ ti nib) is an orally available, small molecule inhibitor of the mitogen activated extracellular signal regulated kinases 1 and 2 (MEK1 and MEK2), which are important components of the kinase cascade in the mitogen activated protein kinase (MAPK) pathway (RAS-RAF-MEK-ERK).
• Components of the MAPK pathway are frequently mutated in patients with malignant melanoma, particular the RAF isoform BRAF.
• These mutations cause a constitutive activation of the MAPK pathway, resulting in unregulated cell growth and proliferation.
• Clinical trials of trametinib in patients with metastatic malignant melanoma have shown that it prolongs progression free and overall survival, but the effect seemed to be limited to patients with the BRAF mutations.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Mekinist is indicated for use in combination with dabrafenib.
• Refer to the dabrafenib labeling for additional risk information that applies to combination use treatment.

Is this medicine FDA approved?

• It was approved for use in the United States in 2014.

How should this medicine be used?

• Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to initiation of treatment with Mekinist as a single agent or in combination with dabrafenib.

Recommended Dosage: Recommended Dosage for Unresectable or Metastatic Melanoma

• The recommended dosage of Mekinist is 2 mg orally taken once daily, as a single agent or in combination with dabrafenib, until disease progression or unacceptable toxicity.

Recommended Dosage for the Adjuvant Treatment of Melanoma

• The recommended dosage of Mekinist is 2 mg orally taken once daily in combination with dabrafenib until disease recurrence or unacceptable toxicity for up to 1 year.

Recommended Dosage for NSCLC

• The recommended dosage of Mekinist is 2 mg orally taken once daily in combination with dabrafenib until disease recurrence or unacceptable toxicity.

Recommended Dosage for ATC

• The recommended dosage of Mekinist is 2 mg orally taken once daily in combination with dabrafenib until disease recurrence or unacceptable toxicity.

Administration

• Take Mekinist exactly as your healthcare provider tells you to take it. Do not change your dose or stop Mekinist unless your healthcare provider tells you.
• Your healthcare provider may change your dose of Mekinist, temporarily stop, or completely stop your treatment with Mekinist if you develop certain side effects.
• Take Mekinist one time a day, about every 24 hours.
• Take Mekinist at least 1 hour before or 2 hours after a meal.
• If you miss a dose, take it as soon as you remember. If it is less than 12 hours before your next scheduled dose, skip the missed dose. Just take the next dose at your regular time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 0.5 mg, 2 mg

This medicine is available in fallowing brand namesː

• Mekinist

What side effects can this medication cause?

The most common side effects of Mekinist when taken alone include:

• rash
• diarrhea
• swelling of the face, arms, or legs

The most common side effects of Mekinist when taken with dabrafenib in people with melanoma that has spread to other parts of the body or cannot be removed by surgery include:

• fever
• diarrhea
• rash
• vomiting
• nausea
• high blood pressure (hypertension)
• chills
• swelling of the face, arms, or legs

The most common side effects of Mekinist when taken with dabrafenib to help prevent melanoma from coming back after the cancer has been removed by surgery include:

• fever
• chills
• fatigue
• diarrhea
• nausea
• vomiting
• headache
• joint aches
• rash
• muscle aches

The most common side effects of Mekinist when taken with dabrafenib in people with NSCLC include:

• fever
• rash
• fatigue
• swelling of face, arms, and legs
• nausea
• chills
• vomiting
• bleeding
• diarrhea
• cough
• dry skin
• shortness of breath
• decreased appetite

What special precautions should I follow?

• New Primary Malignancies, Cutaneous, and Non-cutaneous, can occur when Mekinist is used with dabrafenib. Monitor patients for new malignancies prior to initiation of therapy, while on therapy, and following discontinuation of treatment.
• Major hemorrhagic events can occur. Monitor for signs and symptoms of bleeding.
• Colitis and gastrointestinal perforation can occur in patients receiving Mekinist. Monitor patients closely for colitis and gastrointestinal perforations.
• Deep vein thrombosis and pulmonary embolism (PE) can occur in patients receiving Mekinist. Advise patients to immediately seek medical care if they develop symptoms of DVT or PE, such as shortness of breath, chest pain, or arm or leg swelling. Permanently discontinue Mekinist for life-threatening PE.
• Cardiomyopathy, including cardiac failure, can occur with Mekinist. Assess left ventricular ejection fraction (LVEF) before treatment, after one month of treatment, then every 2 to 3 months thereafter.
• Perform ophthalmologic evaluation for any visual disturbances. For Retinal Vein Occlusion (RVO), permanently discontinue Mekinist.
• Across clinical trials of Mekinist monotherapy, interstitial lung disease or pneumonitis occurred in 2% of patients. Withhold Mekinist for new or progressive unexplained pulmonary symptoms. Permanently discontinue Mekinist for treatment-related ILD or pneumonitis.
• Serious febrile reactions, can occur when Mekinist is used with dabrafenib.
• Monitor for skin toxicities and for secondary infections. Permanently discontinue Mekinist for intolerable Grade 2, or Grade 3 or 4 rash not improving within 3 weeks despite interruption of Mekinist. Permanently discontinue for severe cutaneous adverse reactions (SCARs).
• Monitor serum glucose levels in patients with preexisting diabetes or hyperglycemia.
• Mekinist Can cause fetal harm. Advise females of reproductive potential of potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

Management of overdosage: Since trametinib is highly bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with Mekinist.

Can this medicine be used in pregnancy?

• Based on its mechanism of action and findings from animal reproduction studies, Mekinist can cause fetal harm when administered to a pregnant woman.

Can this medicine be used in children?

• The safety and effectiveness of Mekinist as a single agent or in combination with dabrafenib have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: trametinib
• Inactive ingredients:
• Tablet Core: colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate (vegetable source), mannitol, microcrystalline cellulose, sodium lauryl sulfate.
• Tablet Coating: hypromellose, iron oxide red (2 mg tablets), iron oxide yellow (0.5 mg tablets), polyethylene glycol, polysorbate 80 (2 mg tablets), titanium dioxide.

Who manufactures and distributes this medicine?

• Packager: Novartis Pharmaceuticals Corporation

What should I know about storage and disposal of this medication?

• Store Mekinist in the refrigerator between 36°F to 46°F (2°C to 8°C).
• Keep Mekinist dry and away from moisture and light.
• The bottle of Mekinist contains a desiccant packet to help keep your medicine dry. Do not throw away the desiccant packet.
• Keep Mekinist in its original bottle. Do not place tablets in a pill box.
• Safely throw away Mekinist that is out of date or no longer needed.
• Keep Mekinist and all medicine out of the reach of children.

• Dailymed label info on Trametinib
• FDA Trametinib

Trametinib Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Trametinib Resources
Latest articles Most recent articles Ongoing trials	Wikipedia