TARGRETIN

Terminal half-life of bexarotene is approximately 7 hours. Studies in patients with advanced malignancies show approximate single dose linearity within the therapeutic range.

AbsorptionAfter oral administration of TARGRETIN, bexarotene is absorbed with a T max of about 2 hours. Plasma bexarotene AUC and C max values resulting from a 75 to 300 mg dose were 35% and 48% higher, respectively, after a fat-containing meal than after a glucose solution.

DistributionBexarotene is highly bound (>99%) t...

TARGRETIN was evaluated in two clinical trials in 152 patients with advanced and early stage cutaneous T-cell lymphoma (CTCL) in two multicenter, open-label, historically controlled clinical trials conducted in the U.S., Canada, Europe, and Australia. The advanced disease patients had disease refractory to at least one prior systemic therapy (median of two, range 1 to 6 prior systemic therapies) and had been treated with a median of five (range 1 to 11) prior systemic, irradiation, and/or topical therapies. Early disease patients were intolerant to, had disease that was refractory to, or had r...

The following serious adverse reactions are discussed in greater detail in other sections of the prescribing information:

• Hyperlipidemia [see Warnings and Precautions (5.1) ]
• Pancreatitis [see Warnings and Precautions (5.2) ]
• Hepatotoxicity, Cholestasis, and Hepatic Failure [see Warnings and Precautions (5.3) ]
• Hypothyroidism [see Warnings and Precautions (5.4) ]
• Neutropenia [see Warnings and Precautions (5.5) ]
• Cataracts [see Warnings and Precautions (5.6) ]
• Vitamin A Supple...

• Pregnancy (Boxed Warning, 4.1 )
• Known hypersensitivity to bexarotene ( 4.2 ) 4.1 Pregnancy TARGRETIN can cause fetal harm when administered to a pregnant female. TARGRETIN is a member of the retinoid class of drugs that is associated with birth defects in humans and is contraindicated in females who are pregnant. Bexarotene was also teratogenic and caused developmental mortality when administe...

• Hyperlipidemia: TARGRETIN causes elevations in blood lipids. Obtain baseline values, monitor, and manage elevations during therapy by dose reduction, interruption, discontinuation and/or lipid lowering therapy. ( 5.1 , 5.11 )
• Pancreatitis: Interrupt TARGRETIN and evaluate if suspected. ( 5.2 )
• Hepatotoxicity, Cholestasis, and Hepatic Failure: Interrupt or discontinue TARGRETIN and evaluate if liver chemistry tests exceed three times the upper limit of normal values. ( 5.3 )
• Hypothyroidis...

7 DRUG INTERACTIONS

Effect of Other Drugs on TARGRETIN GemfibrozilConcomitant administration of TARGRETIN and gemfibrozil resulted in increases in plasma concentrations of bexarotene. Concomitant administration of gemfibrozil with TARGRETIN is not recommended. Effect of TARGRETIN on Other Drugs TARGRETIN may be an inducer for the CYP3A4 enzymes, and may reduce plasma concentrations of other subs...