BEXAROTENE

Pharmacokinetics General Plasma concentrations of bexarotene were determined during clinical studies in patients with CTCL or following repeated single or multiple-daily dose applications of bexarotene gel, 1% for up to 132 weeks. Plasma bexarotene concentrations were generally less than 5 ng/mL and did not exceed 55 ng/mL. However, only two patients with very intense dosing regimens (> 40% BSA lesions and QID dosing) were sampled. Plasma bexarotene concentrations and the frequency of detecting ...

CLINICAL STUDIES Bexarotene gel was evaluated for the treatment of patients with early stage (Stage IA-IIA) CTCL in one multicenter, open-label, clinical trial as well as in a Phase I-II program (dose-seeking trials with different response criteria than the multicenter trial). These clinical studies enrolled a total of 117 patients. In the multicenter, open-label clinical trial, bexarotene gel was evaluated for the treatment of patients with early stage CTCL who were refractory to, intolerant to, or reached a response plateau for at least six months on at least two prior therapies. The study w...

ADVERSE REACTIONS The safety of bexarotene gel has been assessed in clinical studies of 117 patients with CTCL who received bexarotene gel for up to 172 weeks. In the multicenter open-label study, 50 patients with CTCL received bexarotene gel for up to 98 weeks. The mean duration of therapy for these 50 patients was 199 days. The most common adverse events reported with an incidence at the application site of at least 10% in patients with CTCL were rash, pruritus, skin disorder, and pain. Advers...

CONTRAINDICATIONS Bexarotene gel, 1% is contraindicated in patients with a known hypersensitivity to bexarotene or other components of the product. PREGNANCY Bexarotene gel, 1% may cause fetal harm when administered to a pregnant woman. Bexarotene gel must not be given to a pregnant woman or a woman who intends to become pregnant. If a woman becomes pregnant while taking bexarotene gel, bexarotene...

DRUG-DRUG INTERACTIONS Patients who are applying bexarotene gel should not concurrently use products that contain DEET ( N,N -diethyl- m -toluamide), a common component of insect repellent products. An animal toxicology study showed increased DEET toxicity when DEET was included as part of the formulation. No formal studies to evaluate drug interactions with bexarotene have been conducted. Bexarot...