Targretin (bexarotene) 75mg capsules

Mfg by: R.P. Scherer for:  Ligand Pharmaceuticals Inc.  

Indication(s):  Treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.

Administration:  A single oral daily dose with a meal.  Initial dose is 300mg/m²/day.

Pharmacology:  Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRalpha, RXRßeta, RXRgamma).

WebRx Editorial Notes:  Pregnancy category X (must NOT be given to a pregnant woman).  Although no formal drug interaction studies have been performed with bexarotene it is known that the drug is metabolized by cytochrome P450 3A4.  Inhibitors of cyt-P450 3A4 such as ketoconazole, itraconazole, erythromycin, gemfibrozil, and grapefruit juice would be expected to increase levels of bexarotene.  Inducers of cyt-P450 3A4 such as rifampin, phenytoin, phenobarbital, and others would be expected to reduce levels of bexarotene.

This drug should not be used as a first-line agent.  The side effect profile is extensive including dose-dependent lipid abnormalities, hypothyroidism, rash, leukopenia, nausea, peripheral edema, headache, asthenia (loss of strength), and infection as major sequalae.

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