Drugs of interest to pathologists
Drugs related to surgical pathology
Bexarotene

Author: Him G. Kwee, M.D. (see Authors page)

Revised: 21 November 2017, last major update December 2011

Copyright: (c) 2002-2017, PathologyOutlines.com, Inc.

PubMed Search: Bexarotene [title] review

Cite this page: Kwee, H.G. Bexarotene. PathologyOutlines.com website. http://www.pathologyoutlines.com/topic/drugstargretin.html. Accessed June 25th, 2018.
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)
Pathophysiology
  • 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 20 November 2017])
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