Entrectinib

What is Entrectinib?

• Entrectinib (Rozlytrek) is a kinase inhibitor.

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Entrectinib

What are the uses of this medicine?

This medicine is used to treat:

• Adults with non-small cell lung cancer (NSCLC) that has spread to other parts of the body and is caused by an abnormal ROS1 gene.

Adults and children 12 years and older with solid tumors (cancer) that:

• are caused by certain abnormal NTRK genes and
• have spread or if surgery to remove their cancer is likely to cause severe complications, and
• there is no satisfactory alternative treatment option or the cancer grew or spread on other treatment.

How does this medicine work?

• (en-TREK-tih-nib) A substance that blocks certain proteins involved in cell signaling and growth.
• These proteins may be found in a mutated (changed) form or at high levels in some types of cancer cells.
• Blocking these proteins may help keep cancer cells from growing and may kill them.
• Entrectinib is being studied in the treatment of some types of cancer.
• It is a type of tyrosine kinase inhibitor and a type of targeted therapy.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Coadministration of Rozlytrek with a strong or moderate CYP3A inhibitor increases entrectinib plasma concentrations.
• Avoid grapefruit products during treatment with Rozlytrek, as they contain inhibitors of CYP3A.
• Avoid coadministration of strong and moderate CYP3A inducers with Rozlytrek.
• Avoid coadministration of Rozlytrek with other products with a known potential to prolong QT/QTc interval.

Is this medicine FDA approved?

• It was approved for use in the United States in 2019.

How should this medicine be used?

• Select patients for the treatment of metastatic NSCLC with Rozlytrek based on the presence of ROS1 rearrangement(s) in tumor specimens.
• Select patients for treatment of locally advanced or metastatic solid tumors with Rozlytrek based on the presence of a NTRK gene fusion.

Recommended Dosage for ROS1-Positive Non-Small Cell Lung Cancer

• The recommended dosage of Rozlytrek is 600 mg orally once daily with or without food until disease progression or unacceptable toxicity.

Recommended Dosage for NTRK Gene Fusion-Positive Solid Tumors

Adults

• The recommended dosage of Rozlytrek in adults is 600 mg orally once daily with or without food until disease progression or unacceptable toxicity.

Pediatric Patients 12 Years and Older: Recommended dosage is based on body surface area (BSA) as shown below

• BSA greater than 1.50 m2: 600 mg once daily
• BSA 1.11 to 1.50 m2: 500 mg once daily
• BSA 0.91 to 1.10 m2: 400 mg once daily

Administration

• Take Rozlytrek exactly as your healthcare provider tells you to take it. Do not change your dose or stop taking Rozlytrek unless your healthcare provider tells you to.
• Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Rozlytrek if you develop side effects.
• Take Rozlytrek 1 time each day with or without food.
• Swallow whole Rozlytrek capsules. Do not open, crush, chew or dissolve the capsule contents.
• If you miss a dose of Rozlytrek, take it as soon as you remember. If your next dose is due within 12 hours, skip the missed dose and take your next dose at your regular time.
• If you vomit right after taking a dose of Rozlytrek, you may take the dose again.

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

This medicine is available in fallowing doasage form:

• As Capsules: 100 mg and 200 mg

This medicine is available in fallowing brand namesː

• Rozlytrek

What side effects can this medication cause?

The most common side effects of this medicine include:

• tiredness
• constipation
• change in taste
• swelling
• dizziness
• diarrhea
• nausea
• abnormal touch sensation
• shortness of breath
• muscle pain
• confusion, mental status changes, memory problems, and hallucinations
• weight gain
• cough
• vomiting
• fever
• joint pain
• vision changes

Rozlytrek may cause serious side effects, including:

• Congestive heart failure
• Central nervous system (CNS) effects
• Bone fractures
• Liver problems (hepatotoxicity)
• Increased uric acid level in your blood (hyperuricemia)
• Changes in the electrical activity of your heart called QT prolongation
• Vision problems

What special precautions should I follow?

• You should not drink grapefruit juice or eat grapefruit during your treatment with Rozlytrek. It may increase the amount of entrectinib in your blood to a harmful level.
• Do not drive or operate heavy machinery until you know how Rozlytrek affects you. If you experience dizziness, fainting, tiredness, blurred vision, memory loss, changes in mental status, confusion, or hallucinations, do not drive or operate heavy machines until your symptoms resolve.
• Monitor patients for clinical signs and symptoms of congestive heart failure (CHF). For patients with myocarditis, with or without a decreased ejection fraction, MRI or cardiac biopsy may be required to make the diagnosis.
• CNS adverse reactions including cognitive impairment, mood disorders, dizziness, and sleep disturbances can occur with Rozlytrek. Withhold and then resume at same or reduced dose upon improvement or permanently discontinue Rozlytrek based on severity.
• Rozlytrek increases the risk of fractures. Promptly evaluate patients with signs or symptoms of fractures.
• Monitor liver tests, including ALT and AST, every 2 weeks during the first month of treatment, then monthly thereafter, and as clinically indicated.
• This medicine may cause hyperuricemia. Monitor patients for signs and symptoms of hyperuricemia. Initiate treatment with urate-lowering medications as clinically indicated and withhold Rozlytrek for signs and symptoms of hyperuricemia.
• Assess QT interval and electrolytes at baseline and periodically during treatment. Withhold and then resume at same or reduced dose, or permanently discontinue Rozlytrek based on severity.
• This medicine Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and use of effective contraception.

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?

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

Can this medicine be used in children?

• The safety and effectiveness of Rozlytrek in pediatric patients less than 12 years of age with solid tumors who have an NTRK gene fusion have not been established.
• The safety and effectiveness of Rozlytrek in pediatric patients with ROS1-positive NSCLC have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: entrectinib
• Inactive ingredients: tartaric acid, lactose anhydrous, hypromellose, crospovidone, microcrystalline cellulose, colloidal silicon dioxide, and magnesium stearate. Yellow opaque capsule shell contains: hypromellose, titanium dioxide, and yellow iron oxide. Orange opaque capsule shell contains: hypromellose, titanium dioxide, and FD&C Yellow No. 6. Printing ink contains: shellac, propylene glycol, strong ammonia solution, and FD&C Blue No. 2 aluminum lake.

Who manufactures and distributes this medicine?

• Distributed by: Genentech, Inc., A Member of the Roche Group, 1 DNA Way, South San Francisco, CA 94080-4990

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

• Store Rozlytrek below 86°F (30°C).

• Dailymed label info on Entrectinib
• FDA Entrectinib

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