Medical Uses
TARGRETIN capsules contain bexarotene, an oral retinoid used in cutaneous T-cell lymphoma (CTCL), the group of lymphomas that includes mycosis fungoides and Sézary syndrome. In the USA it is approved for the skin manifestations of CTCL when the disease has not responded to at least one earlier systemic treatment. The European and UK licences are narrower: adults with advanced-stage CTCL, again after at least one systemic treatment.
Bexarotene switches on retinoid X receptors (RXR-alpha, beta and gamma). These receptors pair with other nuclear receptors and act as transcription factors, changing the genes that decide whether a cell keeps dividing or matures. The prescribing information is open that the precise reason it works in CTCL is not known.
Approval rested on two open-label trials that together enrolled 152 patients, most of whom had already been through a median of two systemic therapies. At the starting dose of 300 mg/m² a day, 20 of 62 patients (about one in three) had a confirmed response, mostly partial. Some responses appeared within 4 weeks. A later study comparing two doses found a response rate of 34.5% at 300 mg/m² against 23.3% at 150 mg/m².
The capsule is one of several systemic choices for CTCL. Patients who need a different approach sometimes discuss Poteligeo (mogamulizumab) or the oral HDAC inhibitor Zolinza (vorinostat) with their dermatologist or oncologist. A 1% bexarotene gel (60 g tube) is also sold in the USA for early-stage (IA and IB) skin patches; in its study about a quarter of patients responded. Ask us if your doctor has prescribed the gel rather than the capsules.
