Rozlytrek
Rozlytrek (entrectinib) is a targeted therapy that treats metastatic non-small cell lung cancer (NSCLC) and many other advanced cancers that have specific mutations. It’s a pill taken by mouth once a day, so it’s a convenient treatment option. But it commonly causes tiredness, changes in taste, and constipation that can be bothersome.
What is Rozlytrek (entrectinib)?
What is Rozlytrek (entrectinib) used for?
- Metastatic non-small cell lung cancer (NSCLC) with ROS1 gene changes
- Advanced and metastatic cancers with NTRK gene changes, when prior treatment hasn’t worked and no other treatment is available
How Rozlytrek (entrectinib) works
Healthy cells can turn into cancer cells when there are changes (mutations) in their genetic material. These gene changes produce abnormal proteins that can then cause tumors to form and spread.
Certain types of cancer have changes in the NTRK and ROS1 genes. These changes result in abnormal proteins called NTRK fusions and ROS1 fusions that can send signals for tumors to grow. Rozlytrek (entrectinib) works by attaching to these abnormal proteins and blocking the tumors from growing and spreading.
Drug facts
Side effects of Rozlytrek (entrectinib)
The following side effects may get better over time as your body gets used to the medication. Let your healthcare provider know immediately if you continue to experience these symptoms or if they worsen over time.
Common Side Effects
- Lower blood cell counts (up to 57%)
- Feeling very tired (48%)
- Constipation (46%)
- Changes in taste (44%)
- Swelling (40%)
- Dizziness (38%)
- Diarrhea (35%)
- Nausea (34%)
- Feeling numbness, pain, or tingling (34%)
- Trouble catching your breath (30%)
Less Common Side Effects
- Brain fog, confusion, mood, and sleep problems
- Muscle, bone, and joint pain
- Weight gain
- Vomiting
- Cough
- Fever
- Eye problems
Rozlytrek (entrectinib) serious side effects
Contact your healthcare provider immediately if you experience any of the following.
- Hallucinations and confusion
- Depression and thoughts of self-harm
- Serious eye problems: changes in vision, blurry vision
- Heart problems: feeling lightheaded, trouble catching your breath, racing heartbeat, swelling in the legs
- Broken bones: muscle or bone pain, changes in mobility
- Serious liver injury: pain in the right side of the stomach, yellowing of the eyes or skin, dark or brown urine
The following Rozlytrek (entrectinib) side effects have also been reported
Side effects that you should report to your care team as soon as possible:
- Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or throat
- Change in vision
- Heart failure—shortness of breath, swelling of the ankles, feet, or hands, sudden weight gain, unusual weakness or fatigue
- Heart rhythm changes—fast or irregular heartbeat, dizziness, feeling faint or lightheaded, chest pain, trouble breathing
- High uric acid level—severe pain, redness, warmth, or swelling in joints, pain or trouble passing urine, pain in the lower back or sides
- Infection—fever, chills, cough, or sore throat
- Liver injury—right upper belly pain, loss of appetite, nausea, light-colored stool, dark yellow or brown urine, yellowing skin or eyes, unusual weakness or fatigue
- Mood and behavior changes—anxiety, nervousness, confusion, hallucinations, irritability, hostility, thoughts of suicide or self-harm, worsening mood, feelings of depression
Side effects that usually do not require medical attention (report these to your care team if they continue or are bothersome):
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Pros and cons of Rozlytrek (entrectinib)
Pros
- Taken by mouth once a day
- Can be taken with or without food
- Targeted therapy option for people with cancers with an NTRK mutation, or NSCLC with a ROS1 mutation
- Can be used to treat NSCLC that has spread to the brain (brain metastases)
Cons
- Commonly causes tiredness, changes in taste, and constipation
- Can cause dizziness, confusion, and changes in mood, attention, and memory
- Can cause rare but serious heart problems
- Interacts with many other medications, including common antibiotics (e.g., levofloxacin)) and anti-nausea medications (e.g., ondansetron (Zofran))
Pharmacist tips for Rozlytrek (entrectinib)
- Rozlytrek (entrectinib) is available as 100 mg and 200 mg capsules, so you’ll need to take 3 of the 200 mg capsules, or 6 of the 100 mg capsules to make a 600 mg dose. Store the Rozlytrek (entrectinib) capsules in the original container.
- Take the entire Rozlytrek (entrectinib) dose around the same time each day, with or without food. You can set an alarm as a reminder to take Rozlytrek (entrectinib) each day, or incorporate taking it into your daily routine (for example, taking it right before going to bed). Taking Rozlytrek (entrectinib) regularly as instructed by your healthcare team will help you get the most benefit from the medication.
- If you miss a Rozlytrek (entrectinib) dose and it’s within 12 hours of the usual time you take your medication, take your dose as soon as you remember. If there’s less than 12 hours until your next dose, just skip the missed dose and wait to take your medication at the next scheduled time. If you vomit after taking a Rozlytrek (entrectinib) dose, take a make-up dose as soon as you can.
- Rozlytrek (entrectinib) interacts with many drugs, supplements, and other food products. For example, you should avoid grapefruit and grapefruit juice while taking this medication, because substances in grapefruit can raise Rozlytrek (entrectinib) levels in the body and put you at higher risk for side effects. Make sure to share a complete list of medications, herbals, and supplements you’re taking with your healthcare team so they can make sure what you’re taking is safe to take with Rozlytrek (entrectinib).
- Taking Rozlytrek (entrectinib) can make you feel tired, dizzy, and have memory problems. Avoid activities that require you to be alert, such as driving or operating machinery, until you know how the medication affects you.
- Rozlytrek (entrectinib) is likely to cause harm to the unborn baby. If you’re able to become pregnant, use effective birth control while taking Rozlytrek (entrectinib) and for 5 weeks after your last dose. If you’re taking Rozlytrek (entrectinib) and your partner is pregnant or able to become pregnant, make sure to use effective birth control while taking this medication and for 3 months after your last dose.
- Since Rozlytrek (entrectinib) hasn’t been studied in people who are breastfeeding, avoid breastfeeding while taking this medication and for a week after stopping treatment.
Common questions about Rozlytrek (entrectinib)
No, Rozlytrek (entrectinib) isn’t chemotherapy. It’s a targeted therapy that works against certain proteins in the body involved in cancer growth. Targeted therapy is different from chemotherapy, which works against all fast-growing cells in the body, including cancer cells.
Rozlytrek (entrectinib) is currently approved for treating cancers that have a change (mutation) in a gene called NTRK. It’s also used to treat NSCLC that has changes in the ROS1 gene. Your provider will collect a sample of the tumor (biopsy) to check if your cancer has gene changes that can be targeted with specific medications. If your cancer has changes in the ROS1 or NTRK genes, Rozlytrek (entrectinib) might be a treatment option for you.
Typically, you’ll continue taking Rozlytrek (entrectinib) for as long as it’s working to treat your cancer. Your provider will do scans periodically during treatment to make sure the medication is still working. If you’re having more symptoms of your cancer coming back, or if your provider sees the cancer spreading on scans, then they’ll likely ask you to stop taking Rozlytrek (entrectinib) and potentially switch you to a different treatment. Throughout treatment, your provider will monitor you for side effects of Rozlytrek (entrectinib) with physical check ups and blood draws. Talk with your healthcare team if you’re having bothersome side effects, like mood changes or extreme tiredness, while taking Rozlytrek (entrectinib). They can give tips or recommend medications to help manage side effects. They might ask you to stop Rozlytrek (entrectinib) (either for a short while or permanently) or adjust the dose of your medication, depending on how severe your symptoms are.
Constipation is a common side effect of Rozlytrek (entrectinib). You can ease constipation by staying hydrated throughout the day. Try your best to include high-fiber foods in your diet, like whole grains, fruits, and vegetables. You can also improve bowel movements by moving around and engaging in physical activity. If constipation becomes bothersome while taking Rozlytrek (entrectinib), check in with your provider. They might recommend medications to help keep your bowel movements regular.
You might notice that food tastes different, or feel a metallic taste in your mouth after starting Rozlytrek (entrectinib). If you experience this common side effect, try brushing your teeth, flossing, and using salt and baking soda rinses to help keep bad tastes out. You can also use sugar-free gum or hard candies to hide any bad tastes in your mouth. If you’re having trouble eating because of changes in taste, let your provider know. They can give tips on eating well during treatment, or refer you to a nutrition expert who can help find a meal plan that works for you.
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Risks and warnings for Rozlytrek (entrectinib)
Rozlytrek (entrectinib) can cause some serious health issues. This risk may be even higher for certain groups. If this worries you, talk to your doctor or pharmacist about other options.
Heart failure and heart rhythm problems
- Risk factors: Long QT syndrome | History of heart rhythm problems | Heart failure | Taking other medications that can cause heart rhythm problems
Though rare, some people developed heart failure, typically within 2 months after starting Rozlytrek (entrectinib). Your provider will do an ultrasound of your heart before starting treatment, and they’ll also check you for heart failure symptoms regularly throughout treatment. If you develop heart failure, your provider might have you take a break from Rozlytrek (entrectinib). They also might recommend medications to help your heart pump better and have you restart Rozlytrek (entrectinib) at a lower dose. Let your provider know if you have symptoms of heart failure, such as trouble breathing (especially when lying down), coughing or wheezing, or swelling in the legs.
In addition, some people taking Rozlytrek (entrectinib) developed a rare and potentially life-threatening heart rhythm problem. Your provider will do an electrocardiogram (EKG) to check on your heart rhythm (the QT interval) before your start Rozlytrek (entrectinib) and regularly throughout treatment. If you develop heart rhythm problems, your provider might ask you to stop this medication or lower your dose. Let a provider know if you feel a fast heartbeat or are feeling lightheaded or dizzy. Those could be signs of abnormal heart rhythms.
Central nervous system side effects
- Risk factors: Having received radiation for cancer that has spread to the brain
In studies, people treated with Rozlytrek (entrectinib) experienced a variety of side effects in the central nervous system, including confusion, mood changes, dizziness, and changes in sleeping patterns. The majority of people noticed these side effects within 1-3 months of starting the medication (sometimes, as early as a day after starting treatment). If you have these side effects, avoid driving or doing anything that needs concentration until you’ve been checked out by a healthcare provider. They might have you take a break from Rozlytrek (entrectinib) to allow time for you to recover. Let your healthcare team know if you have any new or worsening dizziness, mood changes, hallucinations, sleep disturbances, or problems with memory and concentration.
Risk of broken bones
- Risk factors: Children and adolescents
Taking Rozlytrek (entrectinib) can put people at higher risk for broken bones (fractures), most commonly in the hip or leg. The risk is higher for children. About half of people who had fractures while taking Rozlytrek (entrectinib) experienced the fracture within 4 months after starting the medication. If you fall down, have new muscle or bone pain, or are having more trouble moving around than usual, contact your provider. They can do scans to check for fractures and recommend strategies to manage pain.
Serious eye problems
Rozlytrek (entrectinib) can cause eye problems, including blurry vision, sensitivity to light, and double vision. If you notice changes in your eyesight, let your provider know. They might have you temporarily stop taking Rozlytrek (entrectinib) and refer you to an eye specialist. Once your symptoms have lessened or stopped getting worse, your provider might have you restart Rozlytrek (entrectinib) at a lower dose, depending on your symptoms.
Harm to the unborn baby
Let your provider know if you are pregnant or plan to become pregnant. Rozlytrek (entrectinib) hasn’t been studied in human pregnancy , but it’s likely to cause harm to the unborn baby based on animal studies. If you’re able to become pregnant, your provider will have you do a pregnancy test before starting treatment. They’ll also ask you to use effective birth control while taking this medication and for at least 5 weeks after your last dose. If you’re male and have a partner who’s able to become pregnant, continue using effective birth control while taking Rozlytrek (entrectinib) and for at least 4 months after your last dose.
Liver injury
In studies, signs of liver injury on lab tests were a common, mild side effect of Rozlytrek (entrectinib) that typically appeared within the first few weeks of treatment. But in rare situations, these lab tests indicated serious liver injury. Your provider will do blood tests before starting treatment, every 2 weeks for the first month, and then monthly afterward to check your liver. If you notice signs of liver injury, such as pain in the upper right side of the stomach, yellowing of the eyes or skin, or dark or brown urine, let your healthcare team know. They’ll have you take a break from Rozlytrek (entrectinib) and potentially adjust the dose once your liver labs return to normal.
High uric acid levels
Rozlytrek (entrectinib) can cause high levels of uric acid (a waste product of cells) in the blood. High amounts of uric acid can form crystals that cause pain, swelling, and warmth in joints, similar to gout. Your provider will check on your uric acid levels as part of your blood tests prior to starting and while you’re taking Rozlytrek (entrectinib). If your uric acid levels are high, your provider will have you temporarily stop taking Rozlytrek (entrectinib) and start taking uric acid-lowering medications. Once your uric acid level has returned to normal, it’s likely your provider will restart Rozlytrek (entrectinib) for you, but possibly at a lower dose.
Rozlytrek (entrectinib) dosage
Carton| Dosage | Quantity | Price as low as | Price per unit |
|---|---|---|---|
| 42 packets of 50mg | 2 cartons | $10,158.37 | $5,079.19 |
Typical dosage for Rozlytrek (entrectinib)
- NSCLC with ROS1 mutations
- Adults: The typical dose is 600 mg by mouth once a day.
- Cancers with NTRK gene changes
- Adults: The typical dose is 600 mg by mouth once a day.
- Children (ages 12 years and older): Your child’s provider will calculate the dose based on your child’s body surface area (BSA), which takes into account their height and weight. The typical dose ranges between 400 mg to 600 mg by mouth once a day.
How much does Rozlytrek (entrectinib) cost?
$10,158.37
What are alternatives to Rozlytrek (entrectinib)?
Rozlytrek (entrectinib) images
