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Bexarotene (Topical)

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

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.

Absorption

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

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: 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: 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. 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.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied); however, although renal elimination is a minor excretion pathway, renal insufficiency may result in significant protein binding changes and altered pharmacokinetics of bexarotene.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied); however, hepatic impairment would be expected to result in decreased clearance of bexarotene due to the extensive hepatic contribution to elimination.

Administration

Using a clean, dry finger, apply a sufficient amount to cover lesion with a generous coating. Allow gel to dry before covering with clothing. Avoid application to normal skin; do not apply near mucosal surfaces. Use of occlusive dressings is not recommended. 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. Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).

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: Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid. 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

>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 treatment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

• 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.

Special populations:

• Pregnancy: Bexarotene is a retinoid, a drug class associated with birth defects in humans; do not administer during pregnancy. Pregnancy test needed 1 week before initiation and every month thereafter. Effective contraception must be in place 1 month before initiation, during therapy, and for at least 1 month after discontinuation. Male patients with sexual partners who are pregnant, possibly pregnant, or who could become pregnant, must use condoms during sexual intercourse during treatment and for 1 month after last dose.

Special handling:

• Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).

Other warnings/precautions:

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

Monitoring Parameters

If female, pregnancy test 1 week before initiation then monthly while on bexarotene

Pregnancy Risk Factor

X

Pregnancy Considerations

Bexarotene is a retinoid, a drug class associated with birth defects in humans; do not administer during pregnancy. Bexarotene caused birth defects when administered orally to pregnant rats. It must not be given to a pregnant woman or a woman who intends to become pregnant. If a woman becomes pregnant while using the gel, it must be stopped immediately and appropriate counseling be given. In women of childbearing potential, therapy should be started on the second or third day of a normal menstrual period. Either abstinence or two forms of reliable contraception (one should be nonhormonal) must be used for at least 1 month before initiating therapy, during therapy, and for 1 month following discontinuation of bexarotene. A negative pregnancy test (sensitivity of at least 50 milliunits/mL) within 1 week prior to beginning therapy, and monthly thereafter is required for women of childbearing potential. Males patients must use a condom during any sexual contact with women of childbearing age during therapy, and for 1 month following discontinuation of bexarotene

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience burning, itching, redness, peeling, or headache. Have patient report immediately to prescriber signs of infection, burning or numbness feeling, edema, or severe skin irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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