Adult: For the treatment of cutaneous T-cell lymphoma (CTCL) skin manifestations in patients who are refractory to at least 1 prior systemic therapy: As cap: Initially, 300 mg/m2 once daily. Dose may be reduced to 200 mg/m2 daily, then to 100 mg/m2 daily, or temporarily interrupted if intolerable toxicity occurs. Once toxicity is controlled, the dose may be cautiously re-escalated. If the initial 300 mg/m2 daily dose is well tolerated but no tumour response is observed after 8 weeks of therapy, the dose may be increased to 400 mg/m2 once daily with careful monitoring. All doses are given as a single daily dose. Continue treatment as long as clinical benefit is demonstrated.
Topical/Cutaneous Cutaneous T-cell lymphoma
Adult: For the treatment of cutaneous lesions in patients with refractory or persistent stage IA and IB CTCL or who are intolerant to other therapies: As 1% gel: Apply a sufficient amount to affected areas once every other day during the 1st week. Increase the frequency of application at weekly intervals to once daily, bid, tid, and then to 4 times daily depending on individual lesion tolerance. If local toxicity occurs, application frequency may be decreased. May temporarily discontinue for a few days until symptoms resolve if severe irritation occurs. Continue treatment as long as clinical benefit is demonstrated.
Administration
Bexarotene Should be taken with food.
Contraindications
Pregnancy.
Special Precautions
Patient with risk factors for pancreatitis (e.g. previous pancreatitis, uncontrolled hyperlipidaemia, biliary tract disease, excessive alcohol intake, receiving drugs known to cause hyperlipidaemia or drugs associated with pancreatic toxicity); diabetes mellitus, uncontrolled hypothyroidism, hypervitaminosis A; history of depression; known hypersensitivity to retinoids. Hepatic impairment. Lactation. Concomitant vitamin A supplementation should be limited to ≤15,000 international units/day due to potential additive toxicity. Concurrent use of bexarotene gel with products containing N,N-diethyl-m-toluamide (DEET) should be avoided due to possible increased DEET toxicity.
Adverse Reactions
Significant: Hypothyroidism, reversible reduction in total thyroxine (T4) and TSH levels; increased serum AST, ALT and bilirubin; leucopenia, neutropenia; lipid abnormalities (e.g. hyperlipidaemia, hypercholesterolaemia); photosensitivity, visual disturbances (e.g. new or worsening of cataract), psychiatric disorders (e.g. depression, anxiety, mood changes). Blood and lymphatic system disorders: Lymphoma-like reaction, lymphadenopathy, hypochromic anaemia. Cardiac disorders: Tachycardia. Ear and labyrinth disorders: Deafness, otalgia, otitis externa. Endocrine disorders: Thyroid disorder. Eye disorders: Dry eyes, eye disorder, blepharitis, conjunctivitis. Gastrointestinal disorders: Vomiting, diarrhoea, nausea, cheilitis, dry mouth, constipation, flatulence, abdominal pain. General disorders and administration site conditions: Chills, pain, asthenia. Immune system disorders: Allergic reaction. Infections and infestations: Infection. Investigations: Increased lactic dehydrogenase and creatinine; weight gain. Metabolism and nutrition disorders: Hypoproteinaemia, peripheral oedema. Musculoskeletal and connective tissue disorders: Bone pain, arthralgia, myalgia. Nervous system disorders: Dizziness, headache, hyperaesthesia, insomnia. Renal and urinary disorders: Albuminuria. Skin and subcutaneous tissue disorders: Pruritus, rash, exfoliative dermatitis, skin ulcer, alopecia, skin hypertrophy, skin nodule, acne, sweating, dry skin; contact dermatitis (topical). Potentially Fatal: Hepatoxicity, particularly cholestasis and liver failure; acute pancreatitis associated with hypertriglyceridaemia.
Women of childbearing potential must use 2 effective forms of contraception (including at least 1 non-hormonal method) for 1 month before initiation, during treatment, and at least 1 month after stopping bexarotene therapy. Men with female partners of childbearing potential must use effective birth control methods during treatment and for 1 month after the last dose. Avoid or minimise exposure to sunlight and artificial UV light; if exposure cannot be avoided, use sunscreen and wear protective clothing. Oral: This drug may cause dizziness and visual disturbances, if affected, do not drive or operate machinery. Topical: Avoid application to normal skin and mucosal surfaces. Do not use occlusive dressings unless directed by the doctor.
Monitoring Parameters
Evaluate pregnancy status within 1 week before starting the treatment, then monthly during therapy in women of childbearing potential. Monitor fasting lipid panel at baseline, weekly until lipid response is established (usually for 2-4 weeks), then every 8 weeks thereafter; LFTs at baseline, then at weeks 1, 2 and 4 after initiation, then every 8 weeks thereafter if levels are stable; thyroid function tests (including free T4 levels) at baseline, weekly for the 1st 5-7 weeks, then every 1-2 months; CBC with differential at baseline and periodically during therapy; blood glucose (in diabetics). Perform ophthalmic exams if visual symptoms occur. Assess for signs and symptoms of neuropsychiatric changes, pancreatitis and skin reactions.
Drug Interactions
Additive toxicity may occur with vitamin A supplementation. May increase plasma bexarotene levels with ketoconazole, itraconazole, and erythromycin. May decrease plasma bexarotene levels with CYP3A4 inducers (e.g. rifampicin, phenytoin, dexamethasone). May reduce the plasma levels or efficacy of CYP3A4 substrates (e.g. tamoxifen, paclitaxel, oral or other systemic hormonal contraceptives, atorvastatin). May increase the hypoglycaemic action of insulin, sulfonylureas or thiazolidinediones. Gemfibrozil significantly increases bexarotene plasma concentrations. Increased risk of DEET toxicity when topical bexarotene is used with DEET-containing products.
Food Interaction
Oral: Increased bioavailability with fat-containing meals. May increase bexarotene plasma concentration with grapefruit juice.
Lab Interference
Oral: May interfere with the CA125 assay values in ovarian cancer patients.
Action
Description: Overview: Bexarotene, a synthetic retinoid analogue, is an antineoplastic agent. Mechanism of Action: The exact mechanism of action in the treatment of CTCL is unknown; however, bexarotene is known to selectively bind and activate the retinoid X receptor subtypes RXRα, RXRβ, and RXRγ. When activated, these receptors function as transcription factors regulating gene expression involved in controlling cellular differentiation and proliferation. Pharmacodynamics: In vitro, bexarotene inhibits the growth of haematopoietic and squamous tumour cell lines. Onset: Topical: Response may be observed at 4 weeks; however, full effect may require up to 56 weeks of application. Pharmacokinetics: Absorption: Increased bioavailability with fat-containing meals (cap). Systemically absorbed after topical application (gel). Time to peak plasma concentration: Approx 2 hours (oral). Distribution: Plasma protein binding: >99%. Metabolism: Oral: Metabolised in the liver via oxidation by CYP3A4 to form 4 metabolites, 6- and 7-hydroxy-bexarotene and 6- and 7-oxo-bexarotene, which undergo further glucuronidation. Excretion: Oral: Mainly via faeces; urine (<1%). Elimination half-life: Approx 7 hours.
Chemical Structure
Bexarotene Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 82146, Bexarotene. https://pubchem.ncbi.nlm.nih.gov/compound/Bexarotene. Accessed Feb. 24, 2026.
Storage
Oral: Cap: Store between 2-30°C. Protect from light. Avoid exposure to humidity and high temperatures after opening the bottle.
Topical: Gel: Store between 15-30°C. Protect from light. Avoid exposure to humidity and high temperatures after opening the tube. Keep away from open flame.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
Bexarotene (Systemic). UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/12/2025.Bexarotene (Systemic). UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/12/2025.Bexarotene (Topical). UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/12/2025.Bexarotene (Topical). UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/12/2025.Bexarotene 75 mg Soft Capsules (Celix Pharma Ltd). MHRA. https://products.mhra.gov.uk. Accessed 01/12/2025.Bexarotene Capsule (Amneal Pharmaceuticals NY LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/12/2025.Bexarotene Gel (Amneal Pharmaceuticals NY LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/12/2025.Bexarotene. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 01/12/2025.Brayfield A, Cadart C (eds). Bexarotene. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/12/2025.Joint Formulary Committee. Bexarotene. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/12/2025.Targetin Gel 1% (Stiefel Laboratories, Inc.). U.S. FDA. https://www.fda.gov. Accessed 04/12/2025.
Sign Out
Continue with Google