Rozlytrek (entrectinib)

Rozlytrek^TM (entrectinib) is a drug used to treat adults with non-small cell lung cancer (NSCLC). Specifically, entrectinib is for the treatment of metastatic (has spread to other parts of the body) non-small cell lung cancer (NSCLC) that has an abnormal ROS1 gene. It can also be used in both adults and children (of at least 12 years of age) with solid tumor cancers that test positive for certain neurotrophic tyrosine receptor kinase (NTRK) genes, have also metastasized (spread to other parts of the body) or if surgery to treat the cancer is probable to cause serious problems, and have gotten worse during other types of treatment or there are no other available treatment options.

How does entrectinib work?

As mentioned, entrectinib 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, entrectinib can slow or stop the growth of the cancer cells, while also potentially having less impact on normal, healthy cells in the body.

Entrectinib 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 entrectinib can find these cancer cells whether they are in the lungs, breast, or anywhere else. For solid tumor cancers with certain NTRK genes, as well as other specific characteristics, entrectinib may be used to treat these cancers throughout the body. In terms of cancer that has a certain ROS1 gene, use is currently limited to metastatic NSCLC.

What are the possible side effects of entrectinib?

The most common side effects of entrectinib include, but are not limited to:

• 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

Things to know about entrectinib

As with any medication, there are additional serious side effects that may occur. Your doctor will help you determine if the benefits of taking entrectinib outweigh the risks.

Entrectinib may lead to the development or worsening of heart failure. If you experience any of the following symptoms, let your doctor know as soon as possible:

• Trouble breathing when lying down
• Sudden increase in weight
• Worsening shortness of breath, coughing, or wheezing
• Swelling in your ankles, legs, or feet
• Worsening tiredness, fatigue, or weakness

Entrectinib may impact liver functioning. Your doctor will monitor your liver while you are taking entrectinib. Signs of liver issues to tell your doctor about include:

• Pain on the upper right side of your abdomen
• Nausea, vomiting, or changes in appetite

Entrectinib may increase the risk of bone fractures and vision problems. Vision changes include experiencing light sensitivity, double vision, blurry vision, or seeing flashes of light or new floaters. Tell your doctor as soon as possible if you notice any changes in your vision while taking entrectinib. Entrectinib may also cause cognitive issues, like mood, memory, or sleep changes.

Entrectinib may increase the amount of uric acid in your blood. Uric acid is a natural waste product that gets removed from the body through the urine. Your doctor will monitor you regularly for any changes in uric acid levels. Entrectinib may also interfere with the way your heart is beating, called QT prolongation. Your doctor will also monitor your heart for any changes in its rhythm while taking entrectinib.

This is not an exhaustive list of all potential side effects of entrectinib. Talk to your healthcare provider or pharmacist for further information.

Talk to your doctor

Before starting entrectinib tell your doctor if you:

• Have liver, kidney, or nervous system problems
• Have problems with your vision
• Have any heart problems including heart failure or a condition called long QT syndrome
• Are taking any other medications, including prescription and over-the-counter medicines, vitamins, or supplements
• Are pregnant or planning to become pregnant
• Are sexually active with a partner who may become pregnant
• Are breastfeeding or planning to breastfeed

If you are pregnant, plan to become pregnant, or are breastfeeding or plan to breastfeed, talk with your doctor. Entrectinib can cause harm to a developing fetus and should not be taken by women who are pregnant. While taking entrectinib, males with female partners who can become pregnant, and females who can become pregnant, should both use contraceptives during treatment and for a period of time after completing treatment (patients should discuss appropriate birth control methods, and how long they need to use them, with their doctor). Females should not breastfeed during entrectinib treatment and for a period of time following the final dose (patients should discuss breastfeeding considerations with their doctor).

Receiving entrectinib

Entrectinib comes in oral capsule form. Follow your doctor’s instructions on how and when to take entrectinib, and what to do if you miss a dose or vomit after a dose. Do not change your dose or stop taking entrectinib without talking to your doctor first.

Patients should take their medication as prescribed by their doctor. Patients should talk to their doctor if they have any questions, or if they have questions regarding their entrectinib regimen.

For more information, read the full prescribing information of entrectinib.¹