Bexarotene 75mg capsules
- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Oral formulations of bexarotene
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
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
Hereditary fructose intolerance
History of pancreatitis
Uncontrolled thyroid disorder
Precautions and Warnings
Females of childbearing potential
History of high alcohol intake
Biliary tract disorder
History of depression
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 ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
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 https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Altered hormone levels
Changes in gonadotrophic luteinizing hormone levels
Congestive cardiac failure
Creatine phosphokinase increased
Decrease in high density lipoprotein (HDL)
Elevated amylase levels
Elevated serum lipase
Impaired renal function
Increase in alkaline phosphatase
Increase in lactate dehydrogenase
Mucous membrane disorder
Peripheral vascular disorders
Serum creatinine increased
Urinary tract disorders
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 ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: July 2015
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 https://www.drugs-porphyria.org/languages/UnitedKingdom/s1.php?l=gbr
Bexarotene Last revised: 14 June 2010.
Last accessed: 3 July 2015.
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Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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