Rozlytrek (entrectinib)

Reviewed by: HU Medical Review Board | Last reviewed: August 2023

Rozlytrek® (entrectinib) is a targeted therapy that is used to treat:1

  • Adults with non-small cell lung cancer (NSCLC) that has spread to other parts of the body (metastatic) and is caused by an abnormal ROS1 gene
  • Adults and children ages 1 month and older with solid tumors that:
    • Are caused by certain abnormal NTRK genes, and
    • Have spread (metastatic) or if surgery to remove the cancer is likely to cause severe complications, and
    • There is no alternative treatment option or the cancer grew or spread on other treatment

Your doctor will perform a genetic test to find out whether your cancer is positive for ROS1 or NTRK genes.1

What are the ingredients in Rozlytrek?

The active ingredient in Rozlytrek is entrectinib.1

How does Rozlytrek work?

Rozlytrek is a kinase inhibitor. This means it blocks the action of proteins called kinases made by certain mutated genes, like the ROS1 and NTRK genes. These kinases help the cancer cells continue to grow and spread. By blocking these cancer-specific kinases, Rozlytrek can slow or stop the growth of the cancer cells while also potentially having less impact on normal, healthy cells in the body.1

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Rozlytrek is a targeted tissue agnostic therapy. This means it is designed to target specific aspects of cancer cells, no matter where they are. Drugs like Rozlytrek can find these cancer cells whether they are in the lungs, breast, or anywhere else.1

What are the possible side effects?

The most common side effects of Rozlytrek include:1

  • Nausea
  • Vomiting
  • Swelling
  • Cough
  • Fatigue
  • Constipation
  • Fever
  • Changes in sense of taste
  • Changes in sense of touch (burning, pain, prickling)
  • Dizziness
  • Joint or muscle pain
  • Vision changes
  • Cognitive issues, including confusion, dizziness, memory problems, or hallucinations
  • Weight gain
  • Shortness of breath
  • Diarrhea

These are not all the possible side effects of Rozlytrek. Talk to your doctor about what to expect when taking Rozlytrek. You also should call your doctor if you have any changes that concern you when taking Rozlytrek.

Other things to know

Do not drive a car or operate heavy machinery until you know how Rozlytrek affects you.1

Avoid eating grapefruit or drinking grapefruit juice during treatment with Rozlytrek. Grapefruit may increase the amount of Rozlytrek in your blood.1

Before starting treatment with Rozlytrek, tell your doctor if you have:1

  • Liver or kidney problems
  • Any heart problems, including a condition called long QT syndrome
  • Nervous system (neurological) problems
  • Current or previous eye or vision problems

Rozlytrek can harm an unborn baby. If you can become pregnant, you should use birth control during treatment and for some time after the last dose of Rozlytrek. You should also not breastfeed during treatment with Rozlytrek and for some time after the last dose. Talk to your doctor about your options for birth control and breastfeeding while taking Rozlytrek.1

Before beginning treatment for lung cancer, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you are taking. This includes over-the-counter drugs.

For more information, read the full prescribing information of Rozlytrek.