Osimertinib (Tagrisso)

What Is Osimertinib?

Osimertinib (pronounced [oh si mer ti nib]) is also known by the brand name, Tagrisso. It is a targeted anticancer therapy (an antineoplastic drug) that belongs to a class called epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). EGFR TKIs work by blocking EGFR signaling pathways that can drive cancer cell growth and survival. Follow your clinic/pharmacy’s handling instructions for antineoplastic medications. Wash hands after handling tablets and keep them out of reach of children and pets.

What Is Targeted Therapy?

Targeted therapy is a cancer treatment that blocks specific molecules or signals that help cancer cells grow and survive. Unlike traditional chemotherapy, many targeted therapies are not broadly cytotoxic to rapidly dividing cells, though they can still cause significant side effects.

How Is Tagrisso Used?

Tagrisso is FDA-approved to treat certain types of non-small cell lung cancer (NSCLC), including use as a first-line treatment in appropriate patients.

Available Formulations

Tagrisso is only available in the form of tablets and must be administered orally. The tablets are only available in two strengths: 40 mg and 80 mg. The 40 mg tablets are round and imprinted with “AZ 40.” The 80 mg tablets are oval and imprinted with “AZ 80.” Tagrisso is typically dosed once a day, and the dose is dependent on the cancer type or severity and other factors. Verify the correct dose and frequency with your provider.

Directions for Use

Tagrisso may be taken with or without food. When taking the tablet, swallow it whole; do not break, crush, chew, or allow it to dissolve in your mouth. 

For patients with difficulty swallowing solids, this medication can be dispersed in 2 ounces (60 ml) of noncarbonated water. Stir until dispersed into small pieces (it will not completely dissolve) and immediately drink. Rinse the container with another 4 to 8 ounces (120-240 mL) of water and immediately drink again. Do not crush or heat the tablet.

Missed Dose

If you accidentally miss a dose, skip the missed dose and continue with the next scheduled dose. Do not take extra doses to make up for a missed dose.

Storage

Store tablets in a cool, dry place at room temperature and ensure the bottle is tightly closed.

What To Avoid While Taking Tagrisso

While on Tagrisso therapy, you must follow some precautions. Always tell your physician about any medications you are already taking. Do not take any drug or medicine (even herbals or over-the-counter medications) without prior consent from your physician or pharmacist, as they may have some significant interactions with Tagrisso.

Avoid taking this medication with any other drugs that may prolong cardiac QTc intervals, such as ziprasidone, dronedarone, and posaconazole. QTc prolongation is when the heart’s electrical system takes longer than normal to recharge between beats, which may be detected through a periodic ECG.

Do not receive any vaccinations (especially live vaccines) without first discussing it with your oncology team. They can advise you on timing and which vaccines are appropriate during treatment. Avoid driving or operating machinery if you have blurred vision or other vision changes.

Pregnancy and Tagrisso

Pregnancy status must be checked prior to starting treatment in women of childbearing age. Females of childbearing age must use effective contraception during treatment and for 6 weeks after the last dose. Male patients with partners who can become pregnant should use effective contraception during treatment and for 4 months after the last dose. Tagrisso may cause fetal harm and is therefore not recommended for women who are breastfeeding during therapy. Breastfeeding should also be avoided for at least 2 weeks after the last dose.

Side Effects

As with any other medication, you may encounter many side effects while taking Tagrisso. A few things to keep in mind are:

• You may not have all the side effects listed below. Many people may experience little to no side effects.
• The severity of side effects may vary from person to person, so don’t compare your side effects with other people’s experiences.
• Most of the side effects will improve when therapy is discontinued.
• These side effects are easily manageable most of the time, either by readjusting the dose of Tagrisso or using additional medications to treat the symptoms. Consult with your physician or pharmacist to explore available options.
• Do not hide any symptoms; when you feel any discomfort, do not hesitate to tell your physician or pharmacist about it. 

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Some of the most common side effects of Tagrisso are: 

Diarrhea or Abdominal Pain

If you have watery stools more than four times a day or frequent loose, watery stools, you may have diarrhea. This is one of the most common side effects of Tagrisso. Abdominal pain may be associated with diarrhea. Stay hydrated and take plenty of fluids to maintain the water balance of your body. If you have diarrhea, choose bland, low-fiber foods and avoid foods that commonly worsen diarrhea (such as greasy/fried foods, spicy foods, high-fiber foods, and dairy if it bothers you). As symptoms improve, gradually return to your usual diet based on your tolerance. Examples of foods that are often easier to tolerate include bananas, rice, applesauce, toast, plain pasta, and baked/boiled lean proteins. In rare cases, diarrhea may get severe. If this happens, consult your doctor immediately. Patients 65 years and older may experience a greater incidence of these side effects.

Cardiac Complications

There is a risk that Tagrisso may cause cardiac complications, especially in patients with pre-existing heart problems such as high blood pressure or a history of arrhythmias. Serious symptoms that require medical attention include severe palpitations, swelling of feet, and lightheadedness. Tagrisso should be discontinued immediately and indefinitely if there is QTc prolongation along with a very high heart rate or signs of heart failure. QTc prolongation is when the heart’s electrical system takes longer than normal to recharge between beats, and this can be detected through a periodic ECG.

Lung Complications

Lung problems can include difficulty breathing, coughing, and wheezing. These problems may progress to pneumonitis or interstitial lung disease (ILD) and can be fatal. If ILD develops, permanent discontinuation of Tagrisso may be warranted. Therefore, it is essential to inform your physician immediately if any of these symptoms are present. 

Skin Rash

Tagrisso can cause skin problems that can vary from a minor rash to major skin problems like peeling skin or raised spots on the hands and feet. On rare occasions, it may cause a severe skin reaction called Stevens-Johnson syndrome (SJS) or erythema multiforme. Red, swollen, itching, blistered, or peeling skin (with or without fever) may occur, along with hives, red or irritated eyes, or sores in the mouth, throat, nose, or eyes. Notify your physician or pharmacist immediately of any signs of a rash or allergic reaction, including wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat. Changes in nails, including redness, pain, brittleness, separation from the nail bed, and shedding of the nail, may also occur with Tagrisso use.

Vision Problems

Vision problems can include eye pain, vision changes, light sensitivity, and eye discharge. Tagrisso can cause blurring of vision. Driving and other activities that require clear vision must be avoided while taking this drug. If the symptoms are severe, contact your physician or ophthalmologist immediately. 

Blood Count Changes

Your care team may monitor your blood counts with periodic labs (such as a complete blood count/CBC). Tagrisso can sometimes cause decreases in blood cells, including leukopenia (low white blood cells), neutropenia (a type of low white blood cells), thrombocytopenia (low platelets), and anemia (low red blood cells).

Less severe side effects can include:

• Muscle, bone, or joint pain
• Tiredness
• Oral ulcers
• Cough

Precautions

Unless approved by your physician, Tagrisso is generally not recommended for: 

• Patients who have an allergy to Tagrisso. Allergic reactions can cause a rash over the whole body, shortness of breath, wheezing, dizziness, swelling around your mouth or eyes, fast heart rate, trouble breathing, and sweating. If you have any of these symptoms, stop using Tagrisso and call your doctor or get emergency help right away.
• Patients with history of heart rhythm abnormalities. Periodic ECGs should be used to monitor QTc Prolongation.
• Patients with a history of lung disease. Lung diseases like interstitial lung disease (ILD) or similar lung problems can worsen if you take Tagrisso.
• Patients undergoing elective surgery. Tagrisso may need to be discontinued 3 to 7 days before and after scheduled surgeries.

FAQs

Is Tagrisso a chemo agent?

Tagrisso (osimertinib) is generally considered a targeted therapy (an EGFR tyrosine kinase inhibitor), not traditional chemotherapy. It works by blocking EGFR signals that help certain lung cancer cells grow.

How should Tagrisso be taken?

Tagrisso may be taken with or without food. While taking the tablet, swallow it whole; do not break, crush, chew, or allow it to dissolve in your mouth. For patients with difficulty swallowing solids, this medication can be dispersed in noncarbonated water.

Is Osimertinib available as a generic?

Currently, osimertinib is not available as a generic. It is only available as the brand, Tagrisso.