Bexarotene (bexarotene)

The recommended initial adult dosage of bexarotene for the treatment of skin manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy is 300 mg/m2 orally daily. If no tumor response is observed after 8 weeks and the 300 mg/m2 daily dosage is well tolerated, the dosage may be increased to 400 mg/m2 daily with careful monitoring. Refer to Table 1 for the initial bexarotene dose of 300 mg/m2 daily according to body surface area (BSA).

Bexarotene should be continued as long as the patient is deriving benefit from therapy. Although therapy was continued for up to 97 weeks in clinical studies in patients with CTCL, the optimum duration is not known.

Table 1. Bexarotene Dose Based on an Initial Dose of 300 mg/m2Daily According to BSA

Body Surface Area (m2) Total Daily Dose (mg/day) 0.88-1.12 300 1.13-1.37 375 1.38-1.62 450 1.63-1.87 525 1.88-2.12 600 2.13-2.37 675 2.38-2.62 750

If intolerable adverse effects occur, the dosage may be decreased to 200 mg/m2 daily, then 100 mg/m2 daily, or the drug may be temporarily discontinued. When toxicity is controlled, the dosage may be carefully readjusted upward.

Administer bexarotene orally once daily with a meal.

Store at 2-25degreesC away from light, heat, and humidity.

No dosing information is available for this tab.

No dosing information is available for this tab.

Metabolized by CYP3A4.

In vitro, bexarotene inhibits cytochrome P-450 (CYP) isoenzyme 2C8 and induces CYP3A4.

In vitro, bexarotene does not significantly inhibit CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

*Known or suspected pregnancy.

*Known hypersensitivity to bexarotene or any ingredient in the formulation.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

The most common adverse reactions (occurring in >10% of patients in clinical trials and at least possibly related to treatment) include: lipid abnormalities (elevated triglycerides, elevated total and LDL cholesterol and decreased HDL cholesterol), hypothyroidism, headache, asthenia, rash, leukopenia, anemia, nausea, infection, peripheral edema, abdominal pain, and dry skin.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

No enhanced messaging available.

Safety and efficacy not established in children <18 years of age.

Bexarotene, a retinoid agent, is contraindicated during pregnancy. Retinoid agents are associated with birth defects in humans. In animal studies, bexarotene administration resulted in fetal harm.

Obtain a negative serum pregnancy test within 1 week prior to starting bexarotene therapy, and perform pregnancy testing at monthly intervals during therapy. Pregnancy should be avoided during therapy. If used during pregnancy, apprise of potential fetal hazard. Contraception (using 2 reliable forms, including at least one nonhormonal method) should be used for 1 month before, during, and for at least 1 month after bexarotene administration. Male patients receiving the drug should use condoms during sexual intercourse with women who are or may become pregnant.

There are no data on the presence of bexarotene in human milk, the effects on the breastfed infant, or the effects on milk production. Discontinue nursing or the drug, taking into account the importance of the drug to the mother.

The manufacturer makes no specific dosage recommendations for geriatric patients.

No substantial differences in safety relative to younger adults, but increased sensitivity cannot be ruled out.