Bexarotene (Targretin) is an oral retinoid medication used to treat a rare skin cancer called cutaneous T-cell lymphoma (CTCL) in adults. It’s a type of chemotherapy, usually prescribed when other treatments have stopped working. You take the dose once a day with food, and you’ll need regular blood tests to check for side effects. Common side effects include headache, feeling very tired or low on energy, and high cholesterol levels in the blood.
Cutaneous T-cell lymphoma (CTCL), after at least one other treatment has stopped working
Bexarotene (Targretin) is a retinoid. It activates certain proteins in your body called retinoid X receptors (RXRs). These receptors help control how cells grow and divide.
Though the exact way bexarotene (Targretin) works to treat cutaneous T-cell lymphoma is not fully known, it’s thought to slow down or stop the growth of tumor cells.
Source: DailyMed
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Since this medication is given in varying doses, the actual frequency of side effects may vary. In general, side effects are less common with lower doses than with higher doses.
Check with your doctor as soon as possible if any of the following side effects occur:
More common
Unusual tiredness or weakness
skin rash or other skin and mucous membrane lesions
increase in lipid or cholesterol levels
coldness, dry, puffy skin or weight gain
chills, cough, hoarseness, lower back or side pain or painful or difficult urination
swelling of the arms, feet, hands, or legs
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
Pills taken by mouth once a day
Recommended option when previous treatment no longer work
Can be used alone or with other treatments
Typically requires taking multiple capsules for each daily dose
Commonly causes higher cholesterol levels in the blood
Not safe during pregnancy
Bexarotene (Targretin) comes in 75 mg capsules, and you’ll likely need to take multiple capsules to make up your daily dose. Take your full dose at the same time each day with food.
Bexarotene (Targretin) isn’t safe in pregnancy. If you’re able to get pregnant, use two forms of birth control starting 1 month before, during treatment, and 1 month after stopping the medication.
You’ll need regular pregnancy tests while taking bexarotene (Targretin). If you become pregnant during treatment, stop the medication and tell your care team right away.
If you can become pregnant, start taking bexarotene (Targretin) on the second or third day of your period. This helps to make sure you're not pregnant before beginning treatment.
If you’re a male taking bexarotene (Targretin) and have a partner who can become pregnant, use a condom during sex and continue to do so for at least 1 month after your last dose.
Bexarotene (Targretin) can interact with other medications, herbals, and supplements. Share a list of everything you take with your care team before starting treatment.
If you take vitamin A supplements, tell your oncology care team before starting bexarotene (Targretin). Taking too much vitamin A can raise the risk for side effects from this medication.
Bexarotene (Targretin) can make some blood-sugar lowering medications (like insulin or sulfonylureas) work stronger. If you have diabetes, tell your care team if you notice symptoms of low blood sugar like shakiness, sweating, or dizziness.
Get your lab tests done as scheduled during treatment with bexarotene (Targretin). The medication can cause side effects that don’t have symptoms right away, like changes in cholesterol, thyroid levels, liver function, or white blood cells.
Bexarotene (Targretin) can make your skin more sensitive to the sun, so you might get sunburns more easily. Limit sun exposure and don’t use tanning beds or lamps while taking the medication.
Let your oncologist know if you experience any vision changes while taking bexarotene (Targretin). You might need an eye exam since eye problems like cataracts have occurred in some people taking this medication.
Bexarotene (Targretin) 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.
Bexarotene (Targretin) can cause harm to an unborn baby, so it’s not safe during pregnancy. If you’re able to get pregnant, you’ll need to take a pregnancy test within 1 week before starting the medication and then once a month during treatment. It’s recommended to use two forms of birth control starting 1 month before, during treatment, and for 1 more month after stopping bexarotene (Targretin). One of these should be non-hormonal because hormonal birth control might not work as well with this medication. Let your care team know right away if you become pregnant while taking this medication.
If you're a male taking bexarotene (Targretin) and your partner can become pregnant, you must use a condom during sex and continue to do so for at least 1 month after your last dose.
Bexarotene (Targretin) can cause high levels of cholesterol and triglycerides (fat) in most people who take it. These changes can raise your risk for serious health problems, so it’s important for your care team to monitor your levels closely. Before you start treatment with bexarotene (Targretin), you will do a fasting blood test to check your cholesterol and triglyceride levels. These will be checked weekly at first, then every 2 months once your levels are stable. If your levels get too high during treatment, your oncologist might lower your dose, pause treatment, or give you medication to help manage cholesterol. One commonly used option is atorvastatin.
Risk factors: History of pancreatitis | Uncontrolled high fat levels | Uncontrolled diabetes | Gallbladder problems | Drinking a lot of alcohol | Taking medications that raise fat levels | Taking medications that harm the pancreas
Bexarotene (Targretin) can cause pancreatitis (inflammation of the pancreas), which can be life-threatening. Your risk is higher if you’ve had pancreatitis before, drink a lot of alcohol, or take medications that raise fat levels or affect the pancreas. Tell your care team right away if you have nausea, vomiting, stomach pain, or back pain.
Risk factors: High doses of bexarotene (Targretin)
Bexarotene (Targretin) can cause liver problems, especially if you’re taking a higher dose. You’ll have regular blood tests to check your liver before starting treatment, and again at 1, 2, and 4 weeks. If your liver tests stay stable, your care team will continue to check them at least every 2 months during treatment. Talk to your oncologist immediately if you notice yellowing of your eyes or skin, reduced appetite, unusual bleeding, or bruising.
Bexarotene (Targretin) can cause hypothyroidism (low thyroid hormone levels). Your care team will check your thyroid function before and during treatment. If your levels drop, your oncologist might have you start thyroid hormone replacement therapy. In studies, about one-third of people taking bexarotene (Targretin) needed these replacement medications. Tell your care team if you feel more tired than usual, cold, or gain weight since these could be signs of low thyroid hormone levels.
Bexarotene (Targretin) can lower your white blood cell count, which might make it harder for your body to fight infections. In studies, this usually happened within 4 to 8 weeks of starting treatment, and got better within about 30 days after lowering the dose or stopping the medication. Your care team will check your blood counts before starting treatment and regularly during treatment to monitor for these changes. Let them know if you have symptoms like frequent infections, fever, or feeling more tired than usual.
In studies, some people had new or worsening cataracts after taking bexarotene (Targretin). If you notice vision changes or problems seeing, tell your oncologist. They might refer you for an eye exam to check for cataracts or other eye problems.
If you're taking insulin or other diabetes medications like sulfonylureas or thiazolidinediones, bexarotene (Targretin) can make them work more strongly and raise your risk of low blood sugar (hypoglycemia). This hasn’t been seen when bexarotene (Targretin) is used by itself, but it’s important to watch for symptoms like shakiness, sweating, or dizziness. Talk to your care team before starting this medication if you're taking anything to manage your blood sugar.
bexarotene (Targretin), like other retinoids, can make your skin more sensitive to sunlight. Some people have had sunburns or skin irritation after being in the sun while taking this medication. To help prevent this, limit direct sunlight and tanning beds during treatment. If you go outside, wear sunscreen, protective clothing, and a hat.
The dose depends on your body surface area (BSA), which your care team will calculate using your height and weight.
The typical starting dose is 300 mg/m² of BSA by mouth once a day with a meal. Your oncologist will tell you how many capsules to take each day based on your BSA.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Currently pregnant
Cutaneous T-cell lymphoma (CTCL), after at least one other treatment has stopped working
Advanced cutaneous T-cell lymphoma (CTCL), after least two prior therapies
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