Bexarotene
Bexarotene is a retinoid X receptor (RXR) agonist used primarily to treat skin lesions associated with cutaneous T-cell lymphoma (CTCL) in patients who have not responded to prior therapies. It works by selectively activating RXR subtypes, which regulate genes involved in cell differentiation, proliferation, and apoptosis.
Bexarotene is an RXR agonist used to treat skin manifestations of cutaneous T-cell lymphoma.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- L01XF03
- RxNorm
- 233272
- Generic
- Bexarotene
- Class
- atc-l01
- Brands
- Targretin
- Availability
- rx
- Lactation
- unknown
- Routes
- topical, oral
- Forms
- gel, capsule
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
8 groupspregnancy
first trimesteravoid use
do not use during pregnancy as bexarotene is a known teratogen causing fetal harm
fetal monitoring required if pregnancy occurs during treatment
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid use
discontinue therapy if pregnancy occurs
continuous fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid use
avoid use near term due to risk of prolonged gestation and labor
fetal and uterine monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingdo not breastfeed
bexarotene should not be administered to nursing mothers due to potential severe adverse reactions in infants
monitor infant for signs of toxicity if exposure occurs
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderlystart at lower end of dosing range
use caution when initiating therapy and monitor closely for adverse effects including hyperlipidemia and hypothyroidism
regular monitoring of lipids and thyroid function
Use with caution and monitor for adverse effects.
pediatric_age
children under 18not recommended
safety and efficacy not established in pediatric patients; avoid use in children
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
renal_impairment
severe renal impairmentreduce dose and monitor closely
use with caution in patients with severe renal impairment; limited pharmacokinetic data available
monitor renal function and adjust dose based on clinical response
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate to severedo not use
bexarotene is metabolized hepatically and should not be used in patients with moderate or severe hepatic impairment due to increased risk of toxicity
liver function tests required before and during treatment
Use of this medication in this population requires careful consideration of risks and benefits.
Statistics and clinical data
FDA approval year
FDA approval date for Bexarotene
Drug class
Retinoid X receptor (RXR) agonist
Primary indication
Primary FDA-approved therapeutic use
Mechanism of action
Molecular mechanism of action
Bexarotene is indicated for the treatment of skin lesions in patients with cutaneous T-cell lymphoma (mycosis fungoides or Sézary syndrome) who are refractory to at least one prior systemic therapy.
Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ). Activated RXRs form heterodimers with various partners including retinoic acid receptors, vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors, modulating gene expression involved in cell differentiation, proliferation, and apoptosis.
Bexarotene is highly teratogenic and contraindicated in pregnancy. Common adverse effects include hyperlipidemia (requiring lipid monitoring), hypothyroidism, leukopenia, and skin toxicity. It is typically reserved for patients who have failed at least one prior systemic therapy and requires regular laboratory monitoring during treatment.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
WellAlly may earn a referral fee from linked resources at no extra cost to you. Editorial content is never influenced by commercial relationships.
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy