Drugs of interest to pathologists
Drugs related to surgical pathology

Topic Completed: 1 December 2011

Minor changes: 11 December 2020

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PubMed Search: Bexarotene [title] review

Him G. Kwee, M.D.
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Cite this page: Kwee HG. Bexarotene. PathologyOutlines.com website. https://www.pathologyoutlines.com/topic/drugstargretin.html. Accessed January 22nd, 2021.
Definition / general
  • A retinoid that selectively activates retinoid X receptors
Trade name
  • Targretin® (oral and topical)
Clinical information
Approved by U.S. Food and Drug Administration for:
  • Cutaneous T cell lymphoma (CTCL) that is refractory to at least one prior systemic therapy
  • The oral capsules are used for generalized CTCL and the topical gel is used for localized plaques with CTCL

  • Approximate costs: $2,600 for 30 days oral therapy for adult taking 150 mg, $1,800 for 60 gm topical gel (links now invalid)
  • Bexarotene selectively binds and activates retinoid X receptors RXR alpha, RXR beta and RXR gamma
  • RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor and peroxisome proliferator activitor receptors (PPARs)
  • Once activated, these receptors function as transcripton factors that regulate the expression of genes that control cellular differentiation and proliferation
  • However, the exact mechanism of action of bexarotene in the treatment of CTCL is unknown (Drugs.com: Targretin [Accessed 14 December 2018])
Side effects
  • Lipids: bexarotene can cause elevations in serum triglyceride and LDL cholesterol and a decrease in HDL cholesterol; the triglyceride elevation can cause acute pancreatitis
  • Liver: elevations in AST, ALT, bilirubin, LDH, cholestasis and liver failure
  • Skin: photosensitivity, acne, rash (macular, papular, vesicular, bullous or pustular), alopecia and exfoliative dermatitis (PDR Staff: Physicians' Desk Reference, 66th edition, 2012)
  • Thyroid: decreases in TSH and T4 with hypothyroidism
  • Blood counts: leukopenia, neutropenia, anemia, eosinophilia, increase or decrease in platelet count
  • May cause false increase in serum CA 125 assay values
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