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Bexarotene ligand pharmaceuticals.

R E Hurst1

  • 1Department of Urology, Oklahoma University Health Sciences Center, Oklahoma City, OK 73190, USA. robert-hurst@ouhsc.edu

Current Opinion in Investigational Drugs (London, England : 2000)
|March 16, 2001
PubMed
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Bexarotene, a selective retinoid X receptor agonist, is an effective treatment for cutaneous T-cell lymphoma (CTCL). Targretin (bexarotene) offers a new therapeutic option for patients with CTCL refractory to other treatments.

Area of Science:

  • Oncology
  • Dermatology
  • Pharmacology

Background:

  • Bexarotene (LGD-1069) is the first retinoid X receptor (RXR)-selective antitumor retinoid.
  • Cutaneous T-cell lymphoma (CTCL) is a type of non-Hodgkin lymphoma affecting the skin.
  • Existing therapies for CTCL often have limitations in efficacy or tolerability.

Purpose of the Study:

  • To evaluate the efficacy and safety of bexarotene (Targretin) for the treatment of CTCL.
  • To assess bexarotene's utility in patients with early-stage and advanced-stage CTCL.
  • To provide an alternative treatment option for CTCL patients refractory to or intolerant of other therapies.

Main Methods:

  • FDA approval process for Targretin capsules (oral) and gel (topical).
  • Phase III multicenter trial (50 patients) and Phase I/II clinical program (67 patients) for Targretin gel.

Related Experiment Videos

  • Evaluation of bexarotene in patients with early-stage CTCL (IA-IIA) refractory or intolerant to prior therapies.

    • Main Results:

    • Targretin capsules approved by FDA for all stages of CTCL in refractory patients.
    • Targretin gel received Priority Review for early-stage CTCL cutaneous lesions.
    • Efficacy results for Targretin gel exceeded response target rates; side effects were mainly local skin reactions.

    Conclusions:

    • Bexarotene (Targretin) represents a significant advancement in CTCL treatment.
    • The drug offers a viable therapeutic option for patients with refractory or advanced CTCL.
    • Further post-approval studies and pharmacokinetic evaluations were mandated by the FDA.