Osimertinib

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Generic Name: Osimertinib Brand Name(s): Generics only. No brands available. Avability: Rx Pregnancy Category: N

Uses

What is Osimertinib used for?

Osimertinib is used to treat lung cancer. Osimertinib belongs to a class of drugs known as kinase inhibitors. It works by slowing or stopping the growth of cancer cells. It binds to a certain protein (epidermal growth factor receptor-EGFR) in some tumors.

How should I take Osimertinib?

Take this medication by mouth with or without food as directed by your doctor, usually once daily.

If you have trouble swallowing the tablet whole, place the tablet into a container with a small amount of non-carbonated water (2 ounces/60 milliliters). Stir well until the tablet breaks into small pieces. The tablet will not completely dissolve. Do not crush the tablet or heat the mixture. Drink all of the mixture right away. Add at least another half a glass of water (4 ounces/120 milliliters) to the container and drink all of the mixture to make sure you are getting all of the drug. Use only non-carbonated water for mixing, and do not prepare a supply in advance. The mixture may also be given through a tube into the stomach (nasogastric tube). If you are giving this medication through a nasogastric tube, ask your health care professional for detailed instructions on how to give it.

The dosage is based on your medical condition and response to treatment.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.

How do I store Osimertinib?

Osimertinib is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Osimertinib in the bathroom or the freezer. There may be different brands of Osimertinib that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Osimertinib down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Osimertinib?

Before taking osimertinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history.

Osimertinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using osimertinib, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using osimertinib safely.

This drug may cause blurred vision. Do not drive, use machinery, or do any activity that requires clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.

Osimertinib can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.

Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).

To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the side effects of this drug, especially QT prolongation.

This medication is not recommended for use during pregnancy. It may harm an unborn baby. It is important to prevent pregnancy while taking this medication and after treatment. Females should use reliable forms of birth control (such as condoms, birth control pills) during treatment and for 6 weeks after the end of treatment. Males with female partners should use reliable forms of birth control (such as condoms) during treatment and for 4 months after the end of treatment. If you become pregnant or think you may be pregnant or may have caused pregnancy, tell your doctor right away.

It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding is not recommended while using this drug and for 2 weeks after the end of treatment. Consult your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Osimertinib during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Osimertinib. Osimertinib is pregnancy risk category N according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Osimertinib?

Diarrhea, nausea, mouth sores, dry/itchy skin, tiredness, back pain, headache, or loss of appetite may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, such as: easy bruising/bleeding, changes in your nails (such as nail tenderness/irritation/redness, change in nail color), signs of eye disease (such as vision changes, eye redness/pain, light sensitivity, eye discharge), signs of low level of sodium in the blood (such as nausea, extreme drowsiness, mental/mood changes, seizures).

Get medical help right away if you have any very serious side effects, such as: slow/fast/irregular heartbeat, severe dizziness, fainting, slow/shallow breathing, symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain), new or worsening symptoms of lung disease (such as trouble breathing, chest pain, cough, fever), signs of blood clots (such as pain/swelling/warmth in the groin/calf).

This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you have any signs of infections (such as sore throat that doesn’t go away, fever, chills).

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, such as: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Osimertinib?

Osimertinib may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Osimertinib?

Osimertinib may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with Osimertinib?

Osimertinib may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Osimertinib.

What is the dose of Osimertinib for an adult?

Usual Adult Dose for Non-Small Cell Lung Cancer

80 mg orally once a day

Duration of therapy: Until disease progression or unacceptable toxicity

Comments: The presence of a T790M epidermal growth factor receptor (EGFR) mutation in tumor specimens should be confirmed with an FDA-approved test prior to treatment initiation.

Use: Treatment for patients with metastatic EGFR T790M mutation-positive non-small cell lung cancer (NSCLC) who have progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.

Renal Dose Adjustments

-Mild (CrCl 60 to 89 mL/min) or Moderate (CrCl 30 to 59 mL/min) Renal Impairment: No adjustment recommended.

-Severe (CrCl less than 30 mL/min) Renal Impairment or End-Stage Renal Disease: Data not available; no recommended dose.

Liver Dose Adjustments

-Mild Hepatic Impairment (Total bilirubin less than upper limit of normal [ULN] and AST between 1 to 1.5 x ULN OR total bilirubin between 1 and 1.5 x ULN and any AST): No adjustment recommended.

-Moderate (Total bilirubin between 1.5 to 3 x ULN and any AST) or Severe Hepatic Impairment (Total bilirubin between 3 to 10 x ULN and any AST): Data not available; no recommended dose.

Dose Adjustments

Strong CYP450 3A Inhibitors:

-Avoid concomitant use if possible.

-If no alternative exists, monitor patients closely for adverse reactions.

Strong CYP450 3A Inducers:

-Avoid concomitant use if possible.

Interstitial Lung Disease (ILD)/Pneumonitis:

-Permanently discontinue treatment.

QTc Interval Greater Than 500 msec On At Least 2 Separate ECGs:

-Withhold treatment; resume at 40 mg dose once QTc interval less than 481 msec OR recovery to baseline (if baseline is 481 msec or greater).

QTc Interval Prolongation with Signs/Symptoms of Life-Threatening Arrhythmia:

-Permanently discontinue treatment.

Asymptomatic, Absolute Decrease in Left Ventricular Ejection Fraction (LVEF) of 10% From Baseline and Below 50%:

-Withhold treatment for up to 4 weeks.

-If improved to baseline LVEF, resume treatment.

-If not improved to baseline LVEF, permanently discontinue treatment.

Symptomatic Congestive Heart Failure:

-Permanently discontinue treatment.

Grade 3 or Higher Adverse Reaction:

-Withhold treatment for up to 3 weeks.

-If improvement to Grade 0 to 2 within 3 weeks, resume treatment at 40 to 80 mg once a day.

-If no improvement within 3 weeks, permanently discontinue treatment.

Other Comments

Reconstitution/Preparation Techniques:

-Patients with difficulty swallowing solids can disperse this drug tablet in non-carbonated water in order to drink the mixture or receive it through a naso-gastric tube; the manufacturer product information should be consulted for preparation instructions.

-The drug tablet should not be crushed, heated, or ultrasonicated.

General:

-This drug is under accelerated approval based on tumor response rate and response duration; continued approval may be contingent upon verification and description of clinical benefit in confirmatory trials.

-In 2 blinded independent central review (BICR) clinical trials of patients with metastatic EGFR T790M mutation-positive NSCLC who have progressed on prior systemic therapy including an EGFR TKI, the objective response rate was 59% (complete response 0.5%, partial response 59%); the majority (96%) of patients had ongoing responses ranging from 1.1 to 5.6 months after a median follow up duration of 4 to 4.2 months.

Monitoring:

-Cardiovascular: LVEF by ECG or MUGA scan (before treatment initiation and 3-month intervals during treatment); QTc interval with ECG and electrolytes (periodically during treatment in patients with risk factors)

-Respiratory: Worsening respiratory symptoms (e.g., dyspnea, cough, fever; confirm whether ILD)

What is the dose of Osimertinib for a child?

The dosage has not been established in pediatric patients. It may be unsafe for your child. It is always important to fully understand the safety of the drug before using. Please consult with your doctor or pharmacist for more information.

How is Osimertinib available?

Osimertinib is available in the following dosage forms and strengths:

  • Oral tablet.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Osimertinib, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.

Sources

Review Date: August 10, 2018 | Last Modified: August 10, 2018

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