Version May 2024
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 (Ref). 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.
There are no dosage adjustments provided in the manufacturer's labeling; however, although renal elimination is a minor excretion pathway, renal insufficiency may result in significant protein binding changes and altered pharmacokinetics of bexarotene.
There are no dosage adjustments provided in the manufacturer's labeling; however, hepatic impairment would be expected to result in decreased clearance of bexarotene due to the extensive hepatic contribution to elimination.
Refer to adult dosing.
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%)
Known hypersensitivity to bexarotene or any component of the formulation; pregnancy
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).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gel, External:
Targretin: 1% (60 g) [contains alcohol, usp]
Generic: 1% (60 g)
Yes
Gel (Bexarotene External)
1% (per gram): $524.28 - $554.02
Gel (Targretin External)
1% (per gram): $583.18
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
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.
Hazardous agent (NIOSH 2016 [group 1]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
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
Substrate of CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Risk X: Avoid combination
Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Risk C: Monitor therapy
Methoxsalen (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Methoxsalen (Systemic). Risk C: 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. Risk D: 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. Risk D: 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. Risk D: Consider therapy modification
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy
Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Risk C: 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. Risk D: Consider therapy modification
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.
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.
It is not known if bexarotene is present in breast milk.
Due to the potential for serious adverse reactions in a breastfeeding infant, a decision should be made to discontinue bexarotene gel or to discontinue breastfeeding during therapy, considering the importance of treatment to the mother.
In females of reproductive potential, obtain a pregnancy test 1 week before initiation, then monthly while on bexarotene; monitor for signs/symptoms of hypersensitivity.
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.
Onset: Response may be seen at 4 weeks, although longer application may be required for response (range: up to 56 weeks).
Absorption: Systemically absorbed following topical application (1% gel: generally less than 5 ng/mL and did not exceed 55 ng/mL).
Protein binding: >99% to plasma proteins.
Metabolism: Oral bexarotene metabolism is primarily hepatic via CYP450 3A4 to form oxidative metabolites, which may then be glucuronidated.
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