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Brand Name :
Targretin
Synonyms :
bexarotene
Class :
Retinoids, Antineoplastics
Brand Name :
Targretin
Synonyms :
bexarotene
Class :
Retinoids, Antineoplastics
Dosage Forms & StrengthsÂ
gelÂ
1%Â
capsuleÂ
75mgÂ
300 mg/m² orally daily with the food; titrate according to toxicity or response; if there is no improvement after 8 weeks of treatment, increase the dose to 400 mg/m2/day
Topical: Apply on to the lesions every alternate day for one week, following may increase every week to every 4 times a day.
Monitor: thyroid function, cholesterol levels, and WBCs.
Sezary Syndrome or Refractory Mycosis Fungoides (Off-label)
75-150 mg orally daily in combination with the PUVA; should not exceed more than 300 mg/day
Dose Adjustments
Hepatic Impairment
use caution; Not known
Renal Impairment
use caution; Not known
Safety & efficacy were not establishedÂ
Refer to the adult dosing regimenÂ
drospirenone/ethinyl estradiol/levomefolateÂ
may diminish the therapeutic effect of progestins
the level of effect of lorlatinib will decrease by MDR1 P-glycoprotein efflux transporter due to istradefylline
when both drugs are combined, there may be increased toxicity of sarecycline  
when both drugs are combined, there may be increased toxicity of omadacycline
it decreases by affecting the hepatic enzyme CYP3A4 metabolism
may increase the adverse effect of Multivitamins/Fluoride
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
it increases the toxicity of retinoic acid derivatives
the toxicity of either of the drugs is increased due to pharmacokinetic synergism
Combining bexarotene with pranlukast may cause a reduction in the bexarotene’s metabolism
Combining tegafur with bexarotene can reduce tegafur’s metabolism
It may enhance the risk of adverse effects when combined with oxazolidinones
It may enhance the risk of adverse effects when combined with oxazolidinones
When domeperidone and bexarotene is used together, this leads to reduction in the domeperidone’s metabolism
When bexarotene is used together with fluconazole, this leads to reduction in the bexarotene metabolism
The potential for bleeding risk or its seriousness may elevate when bexarotene is used together with troxerutin
When acetohexamide is used together with bexarotene, this lead to reduction in acetohexamide’s metabolism
When mometasone furoate is used together with bexarotene, this leads to enhanced risk or seriousness of adverse outcomes
When bexarotene is used together with capsaicin, this leads to enhanced risk or seriousness of methemoglobinemia
When bexarotene is used together with norelgestromin, this leads to a rise in norelgestromin’s metabolism
When bexarotene is used together with andrographolide, this leads to enhanced risk or seriousness of bleeding
the metabolism of bexarotene can be decreased when combined with sulfinpyrazone
bexarotene: it may increase the risk of bleeding with indobufen
bexarotene: it may decrease the therapeutic efficacy of gestodene
the metabolism of digitoxin can be heightened when combined with bexarotene
when both drugs combine bexarotene will increase effect of ifosfamide by affecting the enzyme CYP3A4 metabolism.
when both drugs are combined, there may be an increased the serum concentration of bexarotene 
when both drugs are combined, there may be an increased risk or severity of adverse effects  
when both drugs are combined, there may be a decreased level of serum concentration of bexarotene   
lapatinib increases the effect of bexarotene by altering the intestinal or hepatic CYP3A4 enzyme metabolism
bismuth subcitrate, metronidazole and tetracycline
may enhance the risk of adverse effect of retinoic acid derivatives
may enhance the risk of adverse effect of retinoic acid derivatives
may enhance the risk of adverse effect of retinoic acid derivatives
may enhance the risk of adverse effect of retinoic acid derivatives
may enhance the risk of adverse effect of retinoic acid derivatives
may increase the risk of adverse effects
l-methylfolate-pyridoxal 5′-phosphate-methylcobalamine
may increase the risk of adverse effects
bismuth subcitrate, metronidazole and tetracycline
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may enhance the adverse/toxic effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
retinoic acid derivatives decrease the efficacy of progestins
retinoic acid derivatives decrease the efficacy of progestins
retinoic acid derivatives decrease the efficacy of progestins
It may enhance the risk of adverse reactions when combined with Enzymes
the toxicity of either of the drugs is increased due to pharmacokinetic synergism
applying resorcinol with bexarotene topical on the same area may lead to excessive drying and irritation of the skin
the rate of metabolism of bexarotene may be reduced
When bexarotene is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
the activity of the anthrax vaccine can be reduced when used in combination with bexarotene
retinoic acid derivatives decrease the efficacy of progestins
retinoic acid derivatives decrease the efficacy of progestins
retinoic acid derivatives decrease the efficacy of progestins
Actions and spectrum:Â
bexarotene is a medication that belongs to the class of retinoids, specifically a retinoid X receptor (RXR) agonist. It exerts its actions through selective binding and activation of RXR subtypes. The spectrum of actions of bexarotene includes:Â
Frequency definedÂ
1-10%Â
TopicalÂ
OralÂ
>10%Â
Oral (CTCL trial)Â
Black Box Warning:Â
bexarotene carries a black box warning due to its potential for serious adverse effects, including hepatotoxicity, pancreatitis, and hyperlipidemia. It may have increased risk of birth defects if used during pregnancy. Close monitoring of liver function, lipids, and blood glucose levels is recommended during treatment with bexarotene.Â
Contraindication/Caution:Â
Contraindication:Â
Caution:Â
Comorbidities:Â
Pregnancy consideration: N/AÂ
Lactation: N/AÂ Â
Pregnancy category:Â
Pharmacology:Â
Pharmacodynamics:Â
Pharmacokinetics:Â
AbsorptionÂ
bexarotene is administered orally, and its absorption from the gastrointestinal tract is variable. The presence of food can significantly enhance its absorption. Peak plasma concentrations are reached within 2-5 hours after oral administration.Â
DistributionÂ
bexarotene has a moderate volume of distribution, indicating that it distributes well into body tissues. It has a higher affinity for the plasma proteins, primarily albumin. bexarotene crosses the blood-brain barrier and placenta and is excreted into breast milk.Â
MetabolismÂ
bexarotene undergoes extensive metabolism primarily in the liver, primarily via cytochrome P450 enzymes, particularly CYP3A4 and CYP2C8. The major metabolite is 4-oxo-bexarotene, which retains some pharmacological activity. Metabolism of bexarotene leads to the formation of several metabolites, which are subsequently eliminated.Â
Elimination and excretionÂ
bexarotene and its metabolites are primarily eliminated through the feces (70-80% of the dose) and a less extent in the urine (5-20% of the dose). The elimination half-life of bexarotene is short, ranging from about 30 to 60 hours.Â
Administration:Â
Patient information leafletÂ
Generic Name: bexaroteneÂ
Pronounced: (becks-uh-ROH-teen)Â Â
Why do we use bexarotene?Â
bexarotene is primarily used for the treatment of cutaneous T-cell lymphoma (CTCL), a type of cancer that affects the skin. Â
Cutaneous T-cell Lymphoma (CTCL): bexarotene is used to treat CTCL, a type of non-Hodgkin lymphoma that primarily affects the skin. It helps to decrease the size and number of cancerous skin lesions and improve symptoms such as itching and redness.Â
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