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Bexarotene.

M N Lowe1, G L Plosker

  • 1Adis International Limited, Auckland, New Zealand. demail@adis.co.nz

American Journal of Clinical Dermatology
|November 13, 2001
PubMed
Summary
This summary is machine-generated.

Bexarotene effectively treats cutaneous T cell lymphoma (CTCL) and psoriasis by activating retinoid X receptors (RXRs). Oral and topical formulations show significant response rates in CTCL patients and improve psoriasis symptoms.

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Area of Science:

  • Oncology
  • Dermatology
  • Molecular Biology

Background:

  • Bexarotene is a selective retinoid X receptor (RXR) agonist.
  • RXRs are ligand-activated transcription factors regulating gene expression, influencing cell growth, apoptosis, and differentiation.

Purpose of the Study:

  • To evaluate the efficacy and safety of bexarotene in treating cutaneous T cell lymphoma (CTCL) and psoriasis.
  • To assess response rates and adverse events associated with both oral and topical bexarotene formulations.

Main Methods:

  • Clinical trials involving patients with early and advanced stage CTCL.
  • Administration of oral bexarotene (300 mg/m2/day or 0.5-2 mg/kg/day) and topical bexarotene (0.1-1% solutions).
  • Assessment of overall response rates, plaque elevation, and symptom severity.

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Main Results:

  • Oral bexarotene demonstrated overall response rates of 54% in early-stage and 45% in advanced-stage CTCL.
  • Topical bexarotene achieved response rates of 63% (early-stage CTCL) and 44% in another trial.
  • Significant reduction in plaque elevation and psoriasis severity was observed with oral bexarotene.
  • Oral bexarotene decreased serum thyrotropin and free thyroxine levels.

Conclusions:

  • Bexarotene is an effective treatment for CTCL, with both oral and topical routes showing significant efficacy.
  • Oral bexarotene also improves symptoms in moderate to severe psoriasis.
  • Common adverse events include hypertriglyceridemia, hypercholesterolemia, hypothyroidism, and headache; topical use is associated with rash, pruritus, and pain.