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Bexarotene 75mg capsules

Updated 2 Feb 2023 | Bexarotene


Oral formulations of bexarotene

Drugs List

  • bexarotene 75mg capsules
  • TARGRETIN 75mg capsules
  • Therapeutic Indications


    Treatment of skin symptoms of advanced stage cutaneous T-cell lymphoma

    Treatment of skin manifestations of advanced stage cutaneous T-cell lymphoma (CTCL) refractory to at least one systemic treatment.


    Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.


    The recommended initial dosage is 300 mg/square metre daily.

    Initial dose calculations according to body surface area (BSA) are as follows:

    BSA 0.88 to 1.12 metre squared: 300 mg (4 capsules) daily.
    BSA 1.13 to 1.37 metre squared: 375 mg (5 capsules) daily.
    BSA 1.38 to 1.62 metre squared: 450 mg (6 capsules) daily.
    BSA 1.63 to 1.87 metre squared: 525 mg (7 capsules) daily.
    BSA 1.88 to 2.12 metre squared: 600 mg (8 capsules) daily.
    BSA 2.13 to 2.37 metre squared: 675 mg (9 capsules) daily.
    BSA 2.38 to 2.62 metre squared:750 mg (10 capsules) daily.

    Doses greater than 650 mg/square metre daily have not been evaluated in patients.


    (See Dosage; Adults)

    Additional Dosage Information

    Dose modifications
    If adverse reactions occur the dose may be suspended or reduced as follows:

    Full dose: 300 mg/square metre/day
    1st dose reduction: 200 mg/square metre daily.
    2nd dose reduction: 100 mg/square metre daily.

    Once the toxicity has been controlled doses may be readjusted upward.


    Children under 18 years
    Hypervitaminosis A
    Systemic infection
    Hepatic impairment
    Hereditary fructose intolerance
    History of pancreatitis
    Uncontrolled hypercholesterolaemia
    Uncontrolled hypertriglyceridaemia
    Uncontrolled thyroid disorder

    Precautions and Warnings

    Females of childbearing potential
    History of high alcohol intake
    Biliary tract disorder
    Diabetes mellitus
    History of depression
    Renal impairment
    Uncontrolled diabetes mellitus

    Adjustment of hypoglycaemic therapy may be necessary in diabetes mellitus
    Advise ability to drive/operate machinery may be affected by side effects
    Treatment to be initiated and supervised by a specialist
    Presentations with sorbitol unsuitable in hereditary fructose intolerance
    Consult local policy on the safe use of oral anti-cancer drugs
    Staff: Not to be handled by pregnant staff
    Ensure negative pregnancy test in week preceding initiation of treatment
    Monitor blood lipids before and during treatment
    Monitor haemoglobin prior to initiating therapy and periodically thereafter
    Monitor thyroid function prior to and periodically during treatment
    Perform liver function tests before commencing therapy and during therapy
    Initiate antilipaemic therapy if fasting triglycerides raised
    Monitor blood counts weekly for 1 month, then monthly thereafter
    Monitor patient for signs and symptoms of depression
    Advise eye examination if visual disturbance occurs:Lens opacities reported
    Advise patient to report any new or worsening depression/suicidal ideation
    Risk of pancreatitis
    Discontinue if ALT level exceeds 3 times the upper limit of normal
    Discontinue if AST level exceeds 3 times the upper limit of normal
    Discontinue treatment if total bilirubin >3 times upper limit of normal
    Reduce dose or discontinue if fasting triglycerides raised
    Advise patient to limit vitamin A supplements to less than 15,000 IU/day
    Advise patient grapefruit products may increase plasma level
    Female: Two reliable methods of contraception should be used simultaneously
    Female:Contraception required before & until at least 1 month after therapy
    Male: Use barrier contraception during and for 1 month after treatment
    Advise patient to avoid exposure to sunlight and UV rays during treatment
    Patients should not donate blood for transfusion during treatment

    Fasting blood lipid determinations (triglycerides and cholesterol) should be performed before bexarotene therapy is initiated and at weekly intervals until the lipid response to bexarotene is established, which usually occurs within 2 to 4 weeks, and then monthly. Fasting triglycerides should be normal or normalised with appropriate intervention prior to bexarotene therapy. Every attempt should be made to maintain triglyceride levels below 4.52 mmol/l. If fasting triglycerides are elevated or become elevated during treatment, institution of antilipaemic therapy is recommended, and if necessary, dose reductions or treatment discontinuation. Elevations of serum cholesterol should be managed according to current medical practice, however concomitant administration of gemfibrozil with bexarotene in NOT recommended.

    Baseline liver function tests (LFTs) should be obtained, and LFTs should be carefully monitored weekly during the first month and then monthly thereafter. Consideration should be given to a suspension or discontinuation of bexarotene if test results reach greater than three times the upper limit of normal values for AST, ALT or bilirubin.

    Baseline thyroid function tests should be obtained and then monitored at least monthly during treatment and as indicated by the emergence of symptoms consistent with hypothyroidism. Patients with symptomatic hypothyroidism on bexarotene therapy have been treated with thyroid hormone supplements with resolution of symptoms.

    Caution should be exercised when administering bexarotene in patients using insulin, agents enhancing insulin secretion (e.g. sulfonylureas), or insulin-sensitisers (e.g. thiazolidinediones). Based on the known mechanism of action, bexarotene may potentially enhance the action of these agents, resulting in hypoglycaemia.

    Use in Porphyria

    Some sources suggest bexarotene is unsuitable for use in porphyria as it is probably porphyrinogenic.

    Pregnancy and Lactation


    Bexarotene is contraindicated in pregnancy.

    At the time of writing there is no adequate data from the use of bexarotene in pregnant women. Studies in animals have shown have shown reproductive toxicity.

    The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( ) or if this is unavailable at the backup site ( ).


    Bexarotene is contraindicated in breastfeeding.

    It is not known whether bexarotene is excreted in human milk however the molecular weight is low enough that excretion should be expected, a risk to neonates cannot be excluded.

    Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
    Specialist advice is available from the UK Drugs in Lactation Advisory Service at

    Side Effects

    Allergic reaction
    Altered hormone levels
    Blood dyscrasias
    Breast enlargement
    Changes in gonadotrophic luteinizing hormone levels
    Coagulation disorders
    Congestive cardiac failure
    Creatine phosphokinase increased
    Decrease in high density lipoprotein (HDL)
    Electrolyte disturbances
    Elevated amylase levels
    Elevated serum lipase
    Exfoliative dermatitis
    Eye disorder
    Gait abnormality
    Gastro-intestinal symptoms
    Hair disorder
    Hepatic disorders
    Impaired renal function
    Increase in alkaline phosphatase
    Increase in lactate dehydrogenase
    Influenza-like syndrome
    Lymphoma-like disorder
    Mood changes
    Mouth ulcers
    Mucous membrane disorder
    Musculoskeletal disturbances
    Nail disorders
    Oral moniliasis
    Peripheral neuritis
    Peripheral vascular disorders
    Respiratory disorders
    Serous drainage
    Serum creatinine increased
    Sexual dysfunction
    Skin disorder
    Sleep disturbances
    Subdural haematoma
    Taste disturbances
    Urinary tract disorders
    Vascular disorders
    Weight changes


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: July 2015

    Reference Sources

    Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

    Joint Formulary Committee. British National Formulary(online) London: BMJ Group and Pharmaceutical Press. Accessed on 3 July 2015.

    Summary of Product Characteristics: Targretin tablets. Eisai Ltd. Revised March 2018.

    Napos. The drug database for acute porphyria.
    Available at
    Bexarotene Last revised: 14 June 2010.
    Last accessed: 3 July 2015.

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