Pronunciation: tuh-GRISS-oh
Generic name: osimertinib
Dosage form: oral tablet
Drug class: EGFR inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on Feb 22, 2024.

What is Tagrisso?

Tagrisso (osimertinib) is an oral (taken by mouth) kinase inhibitor that may be used to treat adults with non-small cell lung cancer (NSCLC) whose tumors have certain abnormal epidermal growth factor receptor (EGFR) gene(s). It may be used:

• as adjuvant therapy to help prevent your lung cancer from coming back after your tumor(s) has been removed by surgery
• as your first treatment when your lung cancer has spread to other parts of the body (metastasized)
• when your lung cancer has spread to other parts of the body ((metastasized) and you have had previous treatment with an EGFR tyrosine kinase inhibitor (TKI) medicine that did not work or is no longer working
• in combination with pemetrexed and platinum-based chemotherapy, as your first treatment when your lung cancer has spread to nearby tissues (locally advanced) or to other parts of the body (metastasized).

Your healthcare provider will perform a test to make sure that Tagrisso is right for you.

Tagrisso and its active metabolites work by targeting the EGFR receptor which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) at 9-fold lower concentrations than wild-type EGFR. Research has shown anti-tumor activity against NSCLC lines that harbor these EGFR-mutations, leading to tumor regression and increased survival.

Tagrisso was first approved on November 13, 2015.

Warnings

Tagrisso may cause lung problems that may lead to death. Symptoms may be similar to those symptoms from lung cancer. Tell your doctor right away if you have any new or worsening lung symptoms, including trouble breathing, shortness of breath, cough, or fever.

Tagrisso may cause heart problems including affecting the hearts electrical system that may lead to death. Your doctor should check your heart function before you start taking this medicine and during treatment. Call your doctor right away if you have any of the following signs and symptoms of a heart problem: feeling like your heart is pounding or racing, shortness of breath, swelling of your ankles and feet, feeling lightheaded.

Tagrisso may cause eye problems. Tell your healthcare provider right away if you have symptoms of eye problems which may include watery eyes, sensitivity to light, eye pain, eye redness, or vision changes. Your healthcare provider may send you to see an eye specialist (ophthalmologist).

Tagrisso may cause skin problems. Tell your healthcare provider right away if you develop skin reactions that look like rings (target lesions), severe blistering or peeling of the skin.

Tagrisso may cause blood vessel problems in your skin. Tell your healthcare provider right away if you develop purple spots or redness of the skin that does not fade in color when pressed (non-blanching) on your lower arms, lower legs, or buttocks or large hives on the main part of your body (trunk) that do not go away within 24 hours and look bruised.

Tagrisso may cause a condition where your bone marrow cannot make enough new blood cells (aplastic anemia), and which may lead to death. Your healthcare provider will monitor your blood cell counts before you start and during treatment. Tell your healthcare provider right away if you develop any signs or symptoms of blood and bone marrow problems, including:

• a new fever or fever (temperature 100.4°F or higher)
• easy bruising or
•  infection that does not go away bleeding that will not stop
•  tiredness
• weakness
• unusually pale skin.

May cause fetal harm.

It is not known if Tagrisso is safe and effective in children.

Before taking this medicine

You should not use Tagrisso if you are allergic to Tagrisso, osimertinib, or any of the inactive ingredients in the tablets.

To make sure Tagrisso is safe for you, tell your doctor if you have ever had:

• lung or breathing problems
• an electrolyte imbalance (such as high or low blood levels of sodium, calcium, potassium, or magnesium)
• eye problems or
• heart problems, including long QT syndrome (in you or a family member)
• are pregnant or intend to become pregnant
• are breastfeeding or plan to breastfeed.

Pregnancy

Osimertinib can harm an unborn baby if the mother or the father is using this medicine.

If you are a woman, you may need a pregnancy test to make sure you are not pregnant. Use birth control while using this medicine and for at least 6 weeks after your last dose.

If you are a man, use birth control if your sex partner is able to get pregnant. Keep using birth control for at least 4 months after your last dose.

Tell your doctor right away if a pregnancy occurs.

Pregnancy may be less likely to occur while the mother or the father is using this medicine. Both men and women should still use birth control to prevent pregnancy because the medicine can harm an unborn baby.

Breastfeeding

It is not known if Tagrisso passes into your breast milk. Do not breastfeed while using Tagrisso, and for at least 2 weeks after your last dose.

How should I take Tagrisso?

Take Tagrisso exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Tagrisso is usually taken once per day.

• The usual dosage is 80mg once daily, for all indications.
• It may be taken with or without food.
• To make swallowing easier or if you cannot swallow Tagrisso whole, place your tablet in a glass with about 2 ounces (60mL) of water. Do not use carbonated water or any other liquids.
• Stir until the tablet is in small pieces (it will not completely dissolve). Do not crush, heat, or use a microwave to prepare the mixture.
• Drink the mixture right away.
• Add 4 to 8 ounces (120 to 240 mL) more water to the glass, swirl gently and drink right away to make sure you take your full dose of Tagrisso.

If you have a nasogastric (NG) tube:

• Follow the same instructions for mixing Tagrisso tablets in a container but only use 0.5 ounce (15 mL)of water. Do not use carbonated water or any other liquids.
• Stir until the tablet is in small pieces (it will not completely dissolve). Do not crush, heat, or use a microwave to prepare the mixture.
• Add another 15 mL of water into the container to make sure no pieces of Tagrisso tablet remain.
• Administer the Tagrisso tablet and water mixture using the NG tube manufacturer instructions within 30 minutes.
• Add another 30 mL of water into the syringe and give the water and any remaining Tagrisso through the NG tube to make sure that all of the medicine is given. Repeat this step until no pieces remain in the syringe. This will help to ensure that the full prescribed dose is given.

What happens if I miss a dose?

Skip the missed dose and use your next dose at the regular time. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking Tagrisso?

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

What are the side effects of Tagrisso?

Get emergency medical help if you have signs of an allergic reaction to Tagrisso (hives, difficulty breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).

Call your doctor at once if you have:

• skin redness or purple spots that don't turn pale when pressed, and that still look red or bruised after 24 hours (may appear on your arms, legs, buttocks, or midsection)
• redness, rash, or blisters on the palms of your hands or the soles of your feet
• new or worsening cough or trouble breathing
• fast or pounding heartbeats
• swelling in your lower legs, weight gain, feeling short of breath
• a light-headed feeling, like you might pass out
• low blood cell counts - fever, chills, tiredness, mouth sores, skin sores, easy bruising, unusual bleeding, pale skin, cold hands and feet or
• eye problems - vision changes, watery eyes, increased sensitivity to light, eye pain or redness.

Common Tagrisso side effects affecting 20% or more people taking Tagrisso include:

• low blood cell counts
• muscle, bone, or joint pain
• diarrhea
• tiredness
• cough, mouth sores
• dry skin, rash or
• redness, tenderness, pain, or other problems with your fingernails or toenails.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Tagrisso?

Other drugs may interact with Tagrisso, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all other medicines you use.

Tagrisso can cause serious heart problems. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Avoid concomitant use with strong CYP3A inducers, such as rifampicin, phenytoin, or St. John’s Wort. Increase Tagrisso to 160 mg daily in patients receiving a strong CYP3A4 inducer if not possible to avoid these drugs.

See the Product Information for a full list of interactions.

Storage

Store Tagrisso at room temperature between 68°F to 77°F (20°C to 25°C).

Safely throw away medicine that is out of date or that you no longer need.

Keep Tagrisso and all medicines out of the reach of children.

Ingredients

Active: osimertinib

Inactive: mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and sodium stearyl fumarate.

Tablet coating: polyvinyl alcohol, titanium dioxide, macrogol 3350, talc, ferric oxide yellow, ferric oxide red, and ferric oxide black.

Available as 40mg and 80mg tablets.

Manufacturer

AstraZeneca Pharmaceuticals LP.

Frequently asked questions

• What is Tagrisso used for?

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer