Bexarotene

What is Bexarotene?

• Bexarotene (Targretin) is a retinoid used to treat skin problems caused by cutaneous T-cell lymphoma that have not gotten better after other treatment.

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What are the uses of this medicine?

Bexarotene (Targretin) is a prescription medicine used to treat the skin problems that happen with a type of cancer called cutaneous T-cell lymphoma (CTCL) after treatment with at least one other type of medicine by mouth or injection, did not work or has stopped working.

How does this medicine work?

• Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRß, RXRγ).
• RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs).
• Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation.
• Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin.
• It also induces tumor regression in vivo in some animal models.
• The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are pregnant or plan to become pregnant.
• are allergic to bexarotene or any of the ingredients in Targretin.

What drug interactions can this medicine cause?

• Using Targretin with certain other medicines can affect each other.
• Concomitant administration of gemfibrozil with Targretin is not recommended.
• CA125 assay values in patients with ovarian cancer may be increased by Targretin therapy.
• Treatment with Targretin is intended for a female with reproductive potential, it is strongly recommended that a non-hormonal contraception be considered.

Is this medicine FDA approved?

• It was approved by the U.S. Food and Drug Administration (FDA) in December 1999, and the European Medicines Agency (EMA) in March 2001.

How should this medicine be used?

Recommended dosage:

• Recommended initial dose is 300 mg/m2/day.

• Dose Adjustment: May be adjusted to 200 mg/m2/day then to 100 mg/m2/day

Administration:

• Your healthcare provider will tell you how many Targretin capsules to take each day.
• Your healthcare provider may change your daily dose of Targretin as needed to treat your CTCL or if you get certain side effects.
• You should not change your dose unless your healthcare provider tells you to.
• Take your dose of Targretin one time a day with a meal.
• Your healthcare provider will do blood tests before you start Targretin and during treatment to check for side effects.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 75 mg

This medicine is available in fallowing brand namesː

• Targretin

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• asthenia
• rash
• nausea
• infection
• stomach-area (abdomen) pain
• swelling of your hands, arms, feet or legs
• dry skin

Targretin can cause serious side effects, including:

• major birth defects to an unborn baby
• Increased levels of fats (lipids) called cholesterol or triglycerides, in your blood
• acute pancreatitis
• Liver problems, including liver failure
• hypothyroidism
• Low white blood cell count
• New or worse cataracts
• Risk of low blood sugar in people who have diabetes

What special precautions should I follow?

• Targretin induces substantial elevations in lipids in most patients. Obtain baseline values, monitor, and manage elevations during therapy by dose reduction, interruption, discontinuation and/or lipid lowering therapy.
• Acute pancreatitis, including a fatal case, has been reported in four patients with CTCL and in six patients with non-CTCL cancers treated with Targretin. Interrupt Targretin and evaluate if pancreatitis is suspected.
• Targretin caused elevations in liver chemistry tests in patients with CTCL receiving an initial dose of Targretin. Interrupt or discontinue Targretin if test results exceed three times the upper limit of normal values for AST, ALT, or bilirubin.
• Targretin induces hypothyroidism in about half of all patients treated by causing a reversible reduction in levels of thyroid hormone (total thyroxine [total T4]) and thyroid-stimulating hormone (TSH). Obtain baseline thyroid function tests and patients monitor during treatment.
• Monitor for neutropenia. Obtain complete blood counts (CBC) at baseline and periodically during treatment.
• Posterior subcapsular cataracts have occurred. Patients treated with Targretin who experience visual difficulties should have an appropriate ophthalmologic evaluation.
• Because of the relationship of bexarotene to vitamin A, patients should be advised to limit vitamin A supplements to avoid potential additive toxic effects.
• In patients using insulin, agents enhancing insulin secretion (e.g., sulfonylureas), or insulin sensitizers (e.g., thiazolidinedione class), based on the mechanism of action, Targretin could enhance the action of these agents, resulting in hypoglycemia.
• Advise patients to minimize exposure to sunlight and artificial ultraviolet light while receiving Targretin.
• Before initiating Targretin therapy, obtain a CBC, fasting lipid profile, liver function tests, and a thyroid profile. Fasting triglycerides should be normal or normalized with appropriate intervention prior to therapy. Monitor lab tests during Targretin therapy as described above.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Targretin, a retinoid, can cause fetal harm based on findings from animal studies when administered to a pregnant female and is contraindicated during pregnancy.

Can this medicine be used in children?

• Safety and effectiveness of Targretin in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: bexarotene

• Inactive ingredients: butylated hydroxyanisole, polyethylene glycol 400, polysorbate 20, and povidone. The capsule shell contains gelatin, sorbitol special-glycerin blend, and titanium dioxide.

Who manufactures and distributes this medicine?

• Distributed by: Bausch Health US, LLC, Bridgewater, NJ USA
• Manufactured by: Catalent Pharma Solutions LLC, St. Petersburg, FL USA
• Targretin is a trademark of Bausch Health Companies Inc. or its affiliates.

What should I know about storage and disposal of this medication?

• Store Targretin between 36° to 77°F (2° to 25°C).
• Store the Targretin bottle away from light, heat, and humidity.
• The capsules should not be taken after the expiration date printed on the bottle.

• Dailymed label info on Bexarotene
• FDA Bexarotene

Bexarotene Resources
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