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Mekinist Information

Mekinist (Trametinib) is a targeted therapy that belongs to the group of medications called MEK inhibitors. It is primarily used to treat certain cancers, particularly those caused by mutations in the BRAF V600E or V600K gene. It is used alone or in combination with other medications such as dabrafenib in the management of unresectable or metastatic melanoma, a serious skin cancer. It’s also used as an adjuvant treatment after surgery to help prevent the cancer from returning if it has reached the lymph nodes. It is also used in combination with dabrafenib for treating metastatic or unresectable non-small cell lung cancer.

Additionally, it is used for the treatment of locally advanced or metastatic anaplastic thyroid cancer in patients who have no other good treatment options. Furthermore, it is also used for treating both adults and children (1 year and older) with metastatic solid tumors that have progressed despite other treatments and have no other good treatment options. It is also used specifically for children aged 1 year and above with low-grade glioma who require systemic therapy. These cancerous conditions occur when a mutation in the cellular signaling pathway causes cells to multiply uncontrollably, forming tumors that can spread to distant organs.

Trametinib specifically inhibits MEK1 and MEK2 in the MAPK/ERK pathway. In a healthy cell, this pathway acts like a relay race, passing signals from the cell surface to the nucleus to regulate growth. In mutated cancer cells, the relay is stuck in the on position. By inhibiting MEK, this drug disrupts this signaling cascade, effectively starving the tumor of the signals it needs to proliferate and survive. This targeted approach helps to shrink existing tumors and delay disease progression, especially when used in combination with BRAF inhibitors like dabrafenib to prevent the cancer from developing resistance. Mekinist can be an essential part of a targeted cancer therapy regimen, improving survival rates and progression-free survival for patients with these specific mutations.

Mekinist Side Effects

Like other medications, trametinib can cause some side effects. Common side effects of this medication include fever, nausea, rash, chills, diarrhea, vomiting, swelling of the face, arms, or legs, dry skin, cough, constipation, and increased sensitivity of the skin to light. Contact your doctor if these mild side effects persist or worsen.

Stop taking this medicine and contact your doctor immediately if you experience any serious side effects, including the following:
• Allergic reactions such as breathing difficulties, body itching, body rash, skin blistering, swelling of the face, mouth, tongue, lips, or throat;
• Bleeding problems such as headaches, dizziness, or feeling weak, cough up blood or blood clots, vomit blood or your vomit looks like coffee grounds, red or black stools that look like tar;
• Blood clot problems with symptoms such as chest pain, sudden shortness of breath or trouble breathing, pain in your legs with or without swelling, swelling in your arms or legs, a cool, pale arm or leg;
• Breathing problems such as cough, shortness of breath, and fever;
• Eye problems such as blurred vision, loss of vision, or other vision changes, haloes around light, eye pain, swelling, or redness;
• Gastrointestinal problems such as severe diarrhea or more bowel movements than usual, stomach-area (abdominal) pain or tenderness, fever, nausea, blood in stools;
• Heart problems such as feeling your heart pound, race, or beat irregularly; shortness of breath; swelling in your ankles and feet; and feeling lightheaded;
• High blood pressure;
• High blood sugar

Inform your doctor about any other side effects you notice that are not listed here.

Mekinist Precautions

Do not take this medication if you are allergic to trametinib, other ingredients in Mekinist, or any other medicines. Before you start taking this medication, ensure that you inform your doctor about any prior or current medical conditions, including the following:
• Active infection;
• Bleeding disorders;
• Blood clot disorders;
• Diabetes;
• Eye problems;
• Gastrointestinal problems such as inflammatory bowel diseases;
• Heart disease;
• High blood pressure;
• Kidney disease;
• Liver disease;
• Lung problems

Pregnant women should not use this medication due to the risk to the fetus. Pregnant women (or those trying to conceive) should avoid handling the tablets or breathing in any dust from broken tablets, as the drug can be absorbed through the skin or lungs. Breastfeeding is not recommended while using Mekinist due to the potential for serious adverse effects in a nursing infant. Women of reproductive age group taking this medication must use effective contraception during treatment and for at least 4 months after the final dose. If used in combination with dabrafenib, non-hormonal contraception (like condoms) is required, as dabrafenib can render hormonal birth control less effective. Men taking this medication should use condoms during sexual intercourse during treatment with this Mekinist and for at least 4 months after their last dose of Mekinist. This medication is not recommended for use in children younger than 1 year or weighing less than 8 kg. Your doctor will request blood tests before and during treatment to monitor your blood cell counts and detect possible adverse effects.

Live vaccines (such as Measles, Mumps, Rubella, and Yellow Fever) should be avoided while taking this medication, as it can alter the immune response, increasing your risk of infection. Mekinist can interact with other medications, especially those that affect liver enzymes (CYP3A). Strong CYP3A inhibitors (such as ketoconazole and clarithromycin) can increase Mekinist levels in the body, increasing the risk of side effects. Therefore, before using this medication, inform your doctor about any other medications you are taking, including herbal medicines and supplements, to determine whether it is safe to use with Mekinist. Take Mekinist (Trametinib) once daily, at the same time each day. Swallow the tablet whole with or without food. Do not crush or chew the tablet. The recommended dose is typically 2 mg per day, but the doctor may adjust the dose based on side effects or response. Ensure your stomach is empty by taking the dose at least one hour before eating or two hours after a meal. Unopened bottles of Mekinist should be refrigerated (between 2°C and 8°C or 36°F to 46°F). Once opened, the bottle can be kept at room temperature for up to 30 days, but it must be kept in the original bottle with the desiccant.

Do I need a prescription to order Mekinist?

Yes, a prescription is required from your physician to order Mekinist.