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Pronunciation: Roz-lye-trek
Generic name: entrectinib
Dosage form: oral capsules, oral pellets
Drug class: Multikinase inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on Oct 26, 2023.

What is Rozlytrek?

Rozlytrek (entrectinib) is an oral kinase inhibitor that may be used to treat:

Rozlytrek works by targeting ROS1 fusion proteins. Normally, the ROS1 gene makes a protein that can send signals to your cells, telling them to grow. When a normal ROS1 gene breaks apart and attaches to another part of a gene, it can create a ROS1 gene fusion which results in a ROS1 fusion protein. ROS1 fusion proteins continuously send signals that can cause cancer cells to develop, grow, and spread. When Rozlytrek finds ROS1 fusion proteins, it binds to them inside cancer cells, blocking their action and slowing or stopping the cancer from growing. About 2% of people with metastatic NSCLC have abnormal ROS1 genes. Roxlytrek also has activity against NTRK and ALK fusion genes.

Available as oral capsules and oral pellets, and the capsules can be made into an oral suspension.

Rozlytrek was FDA-approved on August 15, 2019.


Rozlytrek may cause new or worsened symptoms of congestive heart failure. Your healthcare provider may need to conduct further tests before starting treatment if you have any preexisting heart problems. Call your doctor at once if you have swelling in your lower legs, rapid weight gain, cough, wheezing, shortness of breath, or trouble breathing while lying down.

May cause Central Nervous System (CNS) side effects, such as cognitive impairment, mood disorders, dizziness, and sleep disturbances. Your healthcare provider may withhold treatment temporarily or discontinue it permanently.

May cause liver toxicity. Your healthcare provider will monitor your liver function every 2 weeks during the first month of treatment, then monthly thereafter, and as clinically indicated.

May also cause high levels of uric acid, QT interval prolongation, and increase your risk for fractures (broken bones).

Rozlytrek may affect your vision. Report any changes in vision to your healthcare provider and they may conduct an ophthalmological evaluation as appropriate.

Can harm an unborn baby. Do not use it if you are pregnant. Your doctor may conduct a pregnancy test before you start treatment if you are a woman of childbearing age. Use a non-hormonal form of birth control to prevent pregnancy while using Rozlytrek and for at least 2 weeks after your last dose.

Before taking this medicine

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

You may need to have a negative pregnancy test before starting this treatment.


Rozlytrek can harm an unborn baby or cause birth defects if the mother or the father is using this medicine. If you are a woman, do not use it if you are pregnant. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 5 weeks after your last dose.

If you are a man, use effective birth control if your sex partner can get pregnant. Keep using birth control for at least 3 months after your last dose.

Tell your doctor right away if a pregnancy inadvertently occurs while either the mother or the father is using Rozlytrek.


Do not breastfeed while using this medicine, and for at least 7 days after your last dose.

How should I take Rozlytrek?

Use Rozlytrek exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose. Use the medicine exactly as directed.

If you vomit shortly after taking Rozlytrek, take another dose. Do not change your dose or stop taking Rozlytrek without your doctor's advice.

Rozlytrek capsules

Rozlytrek capsules prepared as a suspension

Carefully open the prescribed number of capsules and pour the contents into room-temperature drinking water or milk. Your healthcare provider will tell you how much water or milk to use, how much suspension to take or give, and provide you with a measuring device like an oral syringe or measuring cup.

Rozlytrek oral pellets

Sprinkle the prescribed number of packets of pellets on 1 or more spoonfuls of soft food like applesauce, yogurt, or pudding, and take within 20 minutes of sprinkling the pellets on the soft food.

Dosing information

Your doctor should select the appropriate dosage form for your age and ability to swallow: oral capsules, capsules prepared as an oral suspension, or oral pellets.

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

Adult and Pediatric Dosage for NTRK Gene Fusion-Positive Solid Tumors

What happens if I miss a dose?

Use the medicine as soon as you can, but skip the missed dose if your next dose is due in less than 12 hours. Do not use two doses at one time. the missed dose and take your next dose at your regular time.

If you vomit shortly after taking Rozlytrek, take another dose.

What happens if I overdose?

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

What to avoid

Avoid driving or hazardous activity until you know how this medicine will affect you. Your reactions could be impaired.

Grapefruit may interact with Rozlytrek and lead to unwanted side effects. Avoid the use of grapefruit products.

What are the side effects of Rozlytrek?

Get emergency medical help if you have signs of an allergic reaction to Rozlytrek: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Rozlytrek may cause serious side effects, including:

The most common side effects occurring in 20% or more people are:

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 the FDA at 1-800-FDA-1088.

What other drugs will affect Rozlytrek?

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements, including:

Know the medicines you take. Keep a list of them to show to your healthcare provider and pharmacist when you get a new medicine. See the prescribing information for a full list of interactions.


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

Keep the bottle tightly closed to protect it from moisture.

Keep all medicines out of the reach of children.


Active: entrectinib

Inactive ingredients

Capsules: tartaric acid, lactose anhydrous, hypromellose, crospovidone, microcrystalline cellulose, colloidal silicon dioxide, and magnesium stearate.

Pellets: tartaric acid, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium, sodium stearyl fumarate, mannitol, and magnesium stearate.


Genentech, Inc.


  1. Rozlytrek

Further information

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