Targretin

Targretin is indicated for the treatment of skin manifestations in advanced stage Cutaneous T-Cell Lymphoma (CTCL) patients who are refractory to at least one systemic treatment. Clinical trials included three dose-ranging phase I-II studies with 141 patients, and additional studies with Targretin capsules.

In refractory CTCL patients, Targretin demonstrated an objective response rate of 34%. For patients with prior irradiation therapies, the overall response rate to Targretin was 31%, compared to a 72% response rate for electron beam therapy and 38% for radiotherapy. When compared to photopheresis and PUVA, Targretin showed a 30% response rate, while photopheresis had a 30% response rate and PUVA had a 24% response rate. The oral bioavailability of micronised bexarotene was 6 to 8 times better than non-micronised, and absorption was enhanced by 40% with a fat-containing dietary supplement. The elimination half-life of bexarotene was 1 to 3 hours.

Safety findings indicate that 97.4% of CTCL patients experienced drug-related adverse events. Hypertriglyceridemia/hypercholesterolemia was a dose-limiting toxicity in 39% of patients at the recommended posology, while neutropenia/leucopenia was a dose-limiting toxicity in 3.6%. Serious adverse events occurred in 3.1% of patients. One death was considered possibly related to bexarotene, and two treatment-related deaths occurred in non-CTCL oncology patients.