Osimertinib

What is Osimertinib?

• Osimertinib (Tagrisso) is a kinase inhibitor used to treat certain patients with non-small cell lung cancer.

What are the uses of this medicine?

This medicine is used to treat adults with non-small cell lung cancer (NSCLC) that has certain abnormal epidermal growth factor receptor (EGFR) gene(s):

• to help prevent your lung cancer from coming back after your tumor(s) has been removed by surgery, or
• as your first treatment when your lung cancer has spread to other parts of the body (metastatic), or
• when your lung cancer has spread to other parts of the body (metastatic) and you have had previous treatment with an EGFR tyrosine kinase inhibitor (TKI) medicine that did not work or is no longer working.

How does this medicine work?

• Osimertinib (oh" sim er' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against the epidermal growth factor receptor (EGFR) that is rearranged and mutated in selected cancers including approximately 5% of non-small cell lung cancer (NSCLC).
• The mutated, rearranged EGFR promotes unregulated cell growth and proliferation, and inhibition of its activity can result in death of cells that overexpress the receptor.
• Osimertinib has been found to inhibit mutated EGFR in cell culture and, in several clinical trials, was found to induce objective responses in a proportion of patients with advanced EGFR mutated (T790M) NSCLC.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid co-administering Tagrisso with strong CYP3A inducers. Increase the Tagrisso dosage when co-administering with a strong CYP3A4 inducer if concurrent use is unavoidable.
• Monitor for adverse reactions of the BCRP or P-gp substrate, unless otherwise instructed in its approved labeling, when co-administered with Tagrisso.
• The effect of co-administering medicinal products known to prolong the QTc interval with Tagrisso is unknown. When feasible, avoid concomitant administration of drugs known to prolong the QTc interval with known risk of Torsades de pointes.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

• Select patients with resectable tumors for the adjuvant treatment of NSCLC with Tagrisso based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in tumor specimens.
• Select patients for the first-line treatment of metastatic EGFR-positive NSCLC with Tagrisso based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in tumor or plasma specimens.
• Select patients for the treatment of metastatic EGFR T790M mutation-positive NSCLC with Tagrisso following progression on or after EGFR TKI therapy based on the presence of an EGFR T790M mutation in tumor or plasma specimens.

Recommended Dosage:

• Adjuvant treatment of early stage NSCLC: 80 mg orally once daily, with or without food, until disease recurrence, or unacceptable toxicity, or for up to 3 years.
• Metastatic NSCLC: 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity.

Administration

• Take Tagrisso exactly as your healthcare provider tells you to take it.
• Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Tagrisso if you have side effects.
• Take Tagrisso 1 time each day.
• You can take Tagrisso with or without food.
• If you miss a dose of Tagrisso, do not make up for the missed dose. Take your next dose at your regular time.

If you cannot swallow Tagrisso tablets whole:

• place your dose of Tagrisso in a container that contains 60 mL (2 ounces) of water. Do not use carbonated water or any other liquids.
• stir the Tagrisso tablet and water until the Tagrisso tablet is in small pieces (the tablet will not completely dissolve). Do not crush, heat, or use ultrasound to prepare the mixture.
• drink the Tagrisso and water mixture right away.
• add 120 mL to 240 mL (4 to 8 ounces) of water into the container and drink to make sure that you take your full dose of Tagrisso.

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

This medicine is available in fallowing doasage form:

• As Tablets: 80 mg and 40 mg

This medicine is available in fallowing brand namesː

• Tagrisso

What side effects can this medication cause?

The most common side effects of this medicine include:

• low white blood cell counts
• low platelet counts
• diarrhea
• low red blood cell counts (anemia)
• rash
• muscle, bone, or joint pain
• changes in your nails, including: redness, tenderness, pain, inflammation, brittleness, separation from the nailbed, and shedding of nail
• dry skin
• mouth sores
• tiredness
• cough

Tagrisso may cause serious side effects, including:

• lung problems
• heart problems, including heart failure
• eye problems
• skin problems
• inflammation

of the blood vessels in your skin

What special precautions should I follow?

• Interstitial lung disease (ILD)/pneumonitis occurred in 3.7% of the 1479 Tagrisso-treated patients; 0.3% of cases were fatal. Permanently discontinue Tagrisso in patients diagnosed with ILD/Pneumonitis.
• Heart rate-corrected QT (QTc) interval prolongation occurs in patients treated with Tagrisso. Monitor electrocardiograms and electrolytes in patients who have a history or predisposition for QTc prolongation, or those who are taking medications that are known to prolong the QTc interval. Withhold then restart at a reduced dose or permanently discontinue Tagrisso.
• Across clinical trials, cardiomyopathy (defined as cardiac failure, chronic cardiac failure, congestive heart failure, pulmonary edema or decreased ejection fraction) occurred. Occurred in 3% of patients. Conduct cardiac monitoring, including left ventricular ejection fraction (LVEF) assessment in patients with cardiac risk factors.
• Keratitis was reported in 0.7% of 1479 patients treated with Tagrisso in clinical trials. Promptly refer patients with signs and symptoms of keratitis to an ophthalmologist for evaluation.
• Stevens-Johnson syndrome (SJS) and erythema multiforme major (EMM) have been reported in patients receiving Tagrisso. Withhold Tagrisso if erythema multiforme major (EMM) or Stevens-Johnson syndrome (SJS) is suspected and permanently discontinue if confirmed.
• cutaneous vasculitis including leukocytoclastic vasculitis, urticarial vasculitis, and IgA vasculitis have been reported in patients receiving Tagrisso. Withhold Tagrisso if cutaneous vasculitis is suspected, evaluate for systemic involvement, and consider dermatology consultation. If no other etiology can be identified, consider permanent discontinuation based on severity.
• Tagrisso can cause fetal harm. Advise females of potential risk to the fetus and to use effective contraception during treatment with Tagrisso and for 6 weeks after final dose. Advise males to use effective contraception for 4 months, after the last dose of Tagrisso.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Tagrisso can cause fetal harm when administered to a pregnant woman.
• There are no available data on Tagrisso use in pregnant women.

Can this medicine be used in children?

• The safety and effectiveness of Tagrisso in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: osimertinib
• Inactive ingredients: mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and sodium stearyl fumarate. Tablet coating contains: polyvinyl alcohol, titanium dioxide, macrogol 3350, talc, ferric oxide yellow, ferric oxide red and ferric oxide black.

Who manufactures and distributes this medicine?

• Distributed by: AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850

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

• 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.

• Dailymed label info on Osimertinib
• FDA Osimertinib

Osimertinib Resources
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