What is Rozlytrek, and how does it work?
Rozlytrek is a prescription medicine 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:
- It is not known if Rozlytrek is safe and effective for use in children less than 12 years of age.
What are the side effects of Rozlytrek?
The most common side effects of Rozlytrek 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
These are not all the possible side effects of Rozlytrek. For more information, ask your healthcare provider or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What is the dosage for Rozlytrek?
Patient Selection
- Select patients for the treatment of metastatic NSCLC with Rozlytrek based on the presence of ROS1 rearrangement(s) in tumor specimens. An FDA-approved test for detection of ROS1 rearrangement(s) in NSCLC for selecting patients for treatment with Rozlytrek is not available.
- Select patients for treatment of locally advanced or metastatic solid tumors with Rozlytrek based on the presence of a NTRK gene fusion. An FDA-approved test for the detection of NTRK gene fusion in solid tumors is not available.
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 (Adolescents)
- The recommended dosage of Rozlytrek is based on body surface area (BSA) as shown in Table 1 below.
- Take Rozlytrek orally once daily with or without food until disease progression or unacceptable toxicity.
Table 1: Dosing in Pediatric Patients 12 Years and Older (Adolescents)
Body Surface Area (BSA) | Recommended Dosage (Orally once daily) |
Greater than 1.50 m² | 600 mg |
1.11 to 1.50 m² | 500 mg |
0.91 to 1.10 m² | 400 mg |
Dosage Modifications For Adverse Reactions
The recommended dosage reductions for adverse reactions are provided in Table 2.
Table 2: Recommended Dose Reductions for Rozlytrek Adverse Reactions
Action | Adults and Pediatric Patients 12 Years and Older with BSA Greater than 1.50 m² (Orally once daily) | Pediatric Patients 12 Years and Older with BSA of 1.11 to 1.50 m² (Orally once daily) | Pediatric Patients 12 Years and Older with BSA of 0.91 to 1.10 m² (Orally once daily) |
First dose reduction | 400 mg | 400 mg | 300 mg |
Second dose reduction* | 200 mg | 200 mg | 200 mg |
*For a subsequent modification, permanently discontinue Rozlytrek in patients who are unable to tolerate Rozlytrek after two dose reductions. |
Table 3 describes dosage modifications for specific adverse reactions.
Table 3: Recommended Dosage Modifications for Rozlytrek for Adverse Reactions
Adverse Reaction | Severity* | Dosage Modification |
Congestive Heart Failure | Grade 2 or 3 |
|
Grade 4 |
| |
Central Nervous System Effects | Intolerable Grade 2 |
|
Grade 3 |
| |
Grade 4 |
| |
Hepatotoxicity | Grade 3 |
|
| ||
Grade 4 |
| |
ALT or AST greater than 3 times ULN with concurrent total bilirubin greater than 1.5 times ULN (in the absence of cholestasis or hemolysis). |
| |
Hyperuricemia | Symptomatic or Grade 4 |
|
QT Interval Prolongation | QTc greater than 500 ms |
|
Torsade de pointes; polymorphic ventricular tachycardia; signs/symptoms of serious arrhythmia |
| |
Vision Disorders | Grade 2 or above |
|
Anemia or Neutropenia | Grade 3 or 4 |
|
Other Clinically Relevant Adverse Reactions | Grade 3 or 4 |
|
*Severity as defined by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4.0. |
Dosage Modifications For Drug Interactions
Moderate And Strong CYP3A Inhibitors
Adults And Pediatric Patients 12 Years And Older With BSA Greater Than 1.50 m²
Avoid coadministration of Rozlytrek with moderate or strong CYP3A inhibitors. If coadministration cannot be avoided, reduce the Rozlytrek dose as follows:
- Moderate CYP3A Inhibitors: 200 mg orally once daily
- Strong CYP3A Inhibitors: 100 mg orally once daily
After discontinuation of a strong or moderate CYP3A inhibitor for 3 to 5 elimination half-lives, resume the Rozlytrek dose that was taken prior to initiating the CYP3A inhibitor.
Administration
- Swallow capsules whole. Do not open, crush, chew, or dissolve the contents of the capsule.
- If a patient misses a dose, patients should make up that dose unless the next dose is due within 12 hours.
- If a patient vomits immediately after taking a dose, they should repeat that dose.

QUESTION
Lung cancer is a disease in which lung cells grow abnormally in an uncontrolled way. See AnswerWhat drugs interact with Rozlytrek?
Effect Of Other Drugs On Rozlytrek
Moderate And Strong CYP3A Inhibitors
Adults And Pediatric Patients 12 Years And Older With BSA Greater Than 1.50 m²
- Coadministration of Rozlytrek with a strong or moderate CYP3A inhibitor increases entrectinib plasma concentrations, which could increase the frequency or severity of adverse reactions. Avoid coadministration of strong or moderate CYP3A inhibitors with Rozlytrek.
- If coadministration is unavoidable, reduce the Rozlytrek dose.
Pediatric Patients 12 Years And Older With BSA Less Than Or Equal To 1.50 m²
- Avoid coadministration of Rozlytrek with moderate or strong CYP3A inhibitors.
- Avoid grapefruit products during treatment with Rozlytrek, as they contain inhibitors of CYP3A.
Moderate And Strong CYP3A Inducers
- Coadministration of Rozlytrek with a strong or moderate CYP3A inducer decreases entrectinib plasma concentrations, which may reduce Rozlytrek efficacy. Avoid coadministration of strong and moderate CYP3A inducers with Rozlytrek.
Drugs That Prolong QT Interval
- QTc interval prolongation can occur with Rozlytrek. Avoid coadministration of Rozlytrek with other products with a known potential to prolong QT/QTc interval.
Is Rozlytrek safe to use while pregnant or breastfeeding?
- Based on literature reports in humans with congenital mutations leading to changes in TRK signaling, findings from animal studies, and its mechanism of action, Rozlytrek can cause fetal harm when administered to a pregnant woman.
- There are no available data on Rozlytrek use in pregnant women.
- There are no data on the presence of entrectinib or its metabolites in human milk or their effects on either the breastfed child or on milk production.
- Because of the potential adverse reactions in breastfed children from Rozlytrek, advise a lactating woman to discontinue breastfeeding during treatment with Rozlytrek and for 7 days after the final dose.
Health News
Summary
Rozlytrek is a prescription medicine 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; and adults and children with solid tumors. The most common side effects of Rozlytrek 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 hallucination, weight gain, and others.
Multimedia: Slideshows, Images & Quizzes
-
Lung Cancer: Early Signs, Symptoms, Stages
Learn about lung cancer early warning signs, symptoms and treatments. What causes stage IV lung cancer? Get more information on...
-
Lung Cancer Quiz: Signs and Symptoms
Lung cancer is the number one cause of cancer deaths in both men and women in the U.S. and worldwide. Get the facts about lung...
-
Picture of Lung Cancer
Cancer of the lung, like all cancers, results from an abnormality in the body's basic unit of life, the cell. See a picture of...
-
Lung Cancer Risks: Myths and Facts
Learn about lung cancer myths and facts. Explore how cigar smoke, menthol, and pollution can increase your risk of lung cancer...
Related Disease Conditions
-
Lung Cancer
Lung cancer kills more men and women than any other form of cancer. Eight out of 10 lung cancers are due to tobacco smoke. Lung cancers are classified as either small-cell or non-small-cell lung cancers.
-
What Should I Do After an Unwanted Pregnancy?
There are a variety of options that may help you handle your situation. It might help you to visualize each option and decide how you feel about it. Consider reaching out to trained professionals or close friends if you get overwhelmed.
-
Small Cell Lung Cancer vs. Non-Small Cell Lung Cancer
Non-small cell lung cancers (NSCLC) consist of large cell carcinomas, adenocarcinomas, and squamous cell carcinomas. Small cell lung cancer (SCLC) usually starts in the bronchi and typically appears in those who smoke. SCLC and NSCLC are staged in different manners, and SCLC tends to metastasize more quickly than NSCLC. Signs and symptoms of NSCLC and SCLC include shortness of breath, coughing up blood, recurring lung infections, and chest pain. Treatment may involve radiation therapy, chemotherapy, and surgery.
-
What Are the Four Types of Lung Cancer?
The four types of lung cancer are classified by what kind of cells the cancer affects and what the tumor cells look like under a microscope. Lung cancers can be small-cell or non-small cell, further classified as squamous cell carcinoma or adenocarcinoma.
Treatment & Diagnosis
- Lung Cancer FAQs
- Sensitive to Smoke, Lung Cancer Gene
- Lung Cancer and Chemotherapy
- Lung Cancer Signs and Symptoms
- 5 Causes of Lung Cancer in Non-Smokers
- Dana Reeve Dies of Lung Cancer by Dr. Stoppler
- What Is the Survival Rate for Lung Cancer Nodules?
- Why Does Lung Cancer Spread So Fast?
- Can You Get Lung Cancer After Quitting Smoking?
- Stage IV Lung Cancer With ALK (Anaplastic Lymphoma Kinase) Rearrangement
Medications & Supplements

SLIDESHOW
Lung Cancer: Early Signs, Symptoms, Stages See SlideshowHealth Solutions From Our Sponsors

Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.