Bexarotene (Targretin)

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General information

Class/mechanism: Retinoid, selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ), which allow them to function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. Exact mechanism of action in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.[1][2][3][4][5]
Route: PO, topical
Extravasation: n/a

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape,UpToDate (courtesy of Lexicomp), or the prescribing information.[1][3]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 1999-12-29: Initial approval for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy. (Based on Duvic et al. 2001a & Duvic et al. 2001b)

History of changes in EMA indication

  • 2001-03-29: Initial authorization

History of changes in PMDA indication

Also known as

  • Code name: LGD-1069
  • Brand names: Bexgratin, Targretin