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Bexarotene (Topical)

Medically reviewed by Drugs.com. Last updated on Aug 21, 2020.

Pronunciation

(beks AIR oh teen)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Gel, External:

Targretin: 1% (60 g) [contains alcohol, usp]

Brand Names: U.S.

  • Targretin

Pharmacologic Category

  • Antineoplastic Agent, Retinoic Acid Derivative

Pharmacology

Bexarotene binds to and activates retinoid X receptor subtypes. Once activated, these receptors function as transcription factors that regulate the expression of genes which control cellular differentiation and proliferation, resulting in decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression.

Absorption

Systemically absorbed following topical application (1% gel: generally less than 5 ng/mL and did not exceed 55 ng/mL)

Metabolism

Oral bexarotene metabolism is primarily hepatic via CYP450 3A4 to form oxidative metabolites, which may then be glucuronidated.

Onset of Action

Response may be seen at 4 weeks, although longer application may be required for response (range: up to 56 weeks).

Protein Binding

>99% to plasma proteins

Use: Labeled Indications

Cutaneous T-cell lymphoma (refractory or persistent): Topical treatment of cutaneous lesions in patients with refractory or persistent cutaneous T-cell lymphoma (stage 1A and 1B) or who have not tolerated other therapies

Contraindications

Known hypersensitivity to bexarotene or any component of the formulation; pregnancy

Documentation of allergenic cross-reactivity for drugs in this class is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Dosing: Adult

Cutaneous T-cell lymphoma (refractory or persistent; early stage): Topical: Apply to lesions once every other day for first week, then increase on a weekly basis to once daily, 2 times daily, 3 times daily, and finally 4 times daily, according to individual lesion tolerance (Breneman 2002; Heald 2003). Continue as long as deriving benefit. Response is usually observed with application at 2 to 4 times daily. May decrease frequency if local toxicity occurs; for severe irritation, temporarily withhold for a few days until symptoms subside.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Administration

Topical: Using a clean, dry finger, apply a sufficient amount to cover lesion with a generous coating. Allow gel to dry (for 5 to 10 minutes) before covering with clothing. Avoid application to normal (healthy) skin; do not apply near mucosal surfaces. Use of occlusive dressings is not recommended. Avoid scratching the treated area(s). If applying after bathing/showering, wait 20 minutes prior to application. Avoid bathing/showering/swimming for at least 3 hours following application (if possible). Following application, wipe excess gel from finger with a disposable tissue and wash hands with soap and water.

Storage

Store at 25°C (77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F). Avoid exposure to high temperatures and humidity after the tube is opened. Protect from light. Keep away from open flame.

Drug Interactions

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Avoid combination

Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Monitor therapy

Multivitamins/Fluoride (with ADE): May enhance the adverse/toxic effect of Bexarotene (Topical). Management: Limit doses of vitamin A to 5,000 units per day if combined with topical bexarotene. Consider therapy modification

Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the adverse/toxic effect of Bexarotene (Topical). Management: Limit doses of vitamin A to 5,000 units per day if combined with topical bexarotene. Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): May enhance the adverse/toxic effect of Bexarotene (Topical). Management: Limit doses of vitamin A to 5,000 units per day if combined with topical bexarotene. Consider therapy modification

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Vitamin A: May enhance the adverse/toxic effect of Bexarotene (Topical). Management: Limit doses of vitamin A to 5,000 units per day if combined with topical bexarotene. Consider therapy modification

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Central nervous system: Pain (30%), headache (14%)

Dermatologic: Skin rash (14% to 72%), pruritus (6% to 40%), contact dermatitis (14%)

Infection: Infection (18%)

1% to 10%:

Cardiovascular: Edema (10%)

Central nervous system: Paresthesia (6%)

Dermatologic: Diaphoresis (6%), exfoliative dermatitis (6%)

Endocrine & metabolic: Hyperlipidemia (10%)

Hematologic & oncologic: Leukopenia (6%), lymphadenopathy (6%)

Neuromuscular & skeletal: Weakness (6%)

Respiratory: Cough (6%), pharyngitis (6%)

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: Use with caution in patients with known hypersensitivity to other retinoids.

• Photosensitivity: Retinoids may cause photosensitization; minimize sunlight and artificial UV light exposure during bexarotene treatment.

Concurrent drug therapy issues:

• Vitamin A supplements: Due to the potential for additive toxicities, patients should be advised to limit additional vitamin A intake to ≤15,000 units/day.

Other warnings/precautions:

• Insect repellents: Avoid insect repellents containing N,N-diethyl-meta-toluamide (DEET) while using topical bexarotene (animal studies demonstrated increased DEET toxicity).

Monitoring Parameters

In females of reproductive potential, obtain a pregnancy test 1 week before initiation, then monthly while on bexarotene; monitor for signs/symptoms of hypersensitivity.

Reproductive Considerations

Evaluate pregnancy status prior to use in females of reproductive potential. Effective contraception should be used for 1 month prior to initiating treatment, during therapy, and for at least 1 month after bexarotene is discontinued. Either abstinence or two forms of reliable contraception (one should be nonhormonal) are recommended. A negative pregnancy test (sensitivity of at least 50 mIU/mL) within 1 week prior to beginning therapy, and monthly, thereafter, is required for women of childbearing potential. A maximum 1-month supply is recommended so that pregnancy tests may be evaluated.

Male patients must use a condom during sexual intercourse with females who are pregnant, possibly pregnant, or who may become pregnant during therapy and for at least 1 month following discontinuation of bexarotene.

Pregnancy Considerations

Bexarotene use is contraindicated in pregnancy. Bexarotene is a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene also caused birth defects when administered orally to pregnant rats. Bexarotene must not be administered to a pregnant woman. If a woman becomes pregnant while taking the drug, it must be stopped immediately and appropriate counseling be given.

Patient Education

What is this drug used for?

• It is used to treat a type of lymphoma that affects the skin.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Burning

• Itching

• Redness

• Peeling

• Loss of strength and energy

• Sweating a lot

• Headache

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Infection

• Burning or numbness feeling

• Swelling

• Swollen glands

• Severe skin irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.