Rozlytrek

Generic name: Entrectinib
Dosage form: oral capsules, oral pellets
Drug class: Multikinase inhibitors

Usage of Rozlytrek

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

Adults with confirmed ROS1-positive non-small cell lung cancer (NSCLC) that has spread to other parts of the body (metastasized)

Adults and children 1 month and older with solid tumors that have spread or cannot be safely removed with surgery, or when other treatments have failed or are not safe options. The tumor must have a confirmed neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation. This indication is authorized under the accelerated approval criteria.

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 side effects

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:

Congestive heart failure. Tell your healthcare provider right away if you develop:

persistent coughing or wheezing

increasing shortness of breath

trouble breathing when lying down

tiredness, weakness, or fatigue

sudden weight gain

swelling in the ankles, feet, or legs.

Central nervous system (CNS) effects. Tell your doctor if you experience dizziness, or changes in your mood, or may affect how you think and cause confusion, hallucinations, and problems with concentration, attention, memory, speaking, understanding what you hear or read, and sleep.

Bone fractures. Tell your healthcare provider if you develop pain, changes in movement, or bone abnormalities.

Liver problems (hepatotoxicity). Your healthcare provider will do blood tests to check your liver function during treatment. Tell your healthcare provider right away if you develop any of these symptoms:

loss of appetite

nausea or vomiting

pain in your upper right stomach area

yellowing of your skin or the white part of your

eyes

dark urine.

Increased uric acid levels in your blood (hyperuricemia). Tell your healthcare provider if you develop any of the following symptoms:

red, hot, tender, or swollen joints, especially in your big toe

pain in your stomach area or sides

nausea or vomiting

pink or brown urine.

Changes in the electrical activity of your heart (QT prolongation). Tell your healthcare provider right away if you feel faint, lightheaded, dizzy, or feel your heart beating irregularly or fast during your treatment

Vision problems. Tell your healthcare provider right away if you have any loss of vision or any vision change, including:

double vision o seeing flashes of light

blurry vision or light hurting your eyes

new or increased floaters.

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

tiredness

constipation

change in taste

swelling and water retention

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.

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.

Before taking Rozlytrek

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

gout

heart problems

long QT syndrome (in you or a family member)

liver or kidney disease

a nervous system disorder or

problems with your eyes or vision.

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

Pregnancy

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.

Breastfeeding

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

Relate drugs

How to use Rozlytrek

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.

Use capsules prepared as suspension for enteral tube administration. Do not use pellets for enteral tube administration.

Administer the dose once daily, with or without food.

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

600 mg orally once daily.

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

Adults: 600 mg orally once daily.

Pediatric Patients: Recommended dosage is based on age and body surface area (BSA) as described in the prescribing information.

Warnings

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.

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:

Strong or moderate CYP3A4 inhibitors, such as clarithromycin, nefazodone, itraconazole, ketoconazole, atazanavir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, or saquinavir. Avoid coadministration, but if unavoidable, reduce the dosage of Braftovi

Strong or moderate CYP3A4 inducers, such as phenobarbital, phenytoin, rifampicin, St. John's Wort, or glucocorticoids. Avoid coadministration.

Drugs that prolong the QTc interval, such as haloperidol, ondansetron, or clarithromycin.

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.

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