Bexarotene: a clinical review.

Article Details

Citation

Farol LT, Hymes KB

Bexarotene: a clinical review.

Expert Rev Anticancer Ther. 2004 Apr;4(2):180-8.

PubMed ID
15056048 [ View in PubMed
]
Abstract

Bexarotene (Targretin, Ligand Pharmaceuticals Inc.) is a synthetic retinoid analog with specific affinity for the retinoid X receptor and belongs to a group of compounds called rexinoids. Early clinical trials of this drug demonstrated activity in cutaneous T-cell lymphoma. Subsequent Phase II/III trials have demonstrated a greater than 50% response rate in patients with all stages of cutaneous T-cell lymphoma who were refractory or intolerant to the previous therapy. The principal toxicities of bexarotene include central hypothyroidism, xeroderma and elevation of cholesterol and triglycerides. These toxicities can be managed with dose attenuation or addition of atorvastatin (Lipitor, Pfizer) or fenofibrate (TriCor, Abbott Laboratories). Since bexarotene has little bone marrow toxicity, it is an excellent candidate for combination therapy with other modalities useful in the treatment of cutaneous T-cell lymphoma. These include ultraviolet B irradiation, psoralen and ultraviolet A photochemotherapy, interferons, denileukin diftitox (Ontak, Ligand Pharmaceuticals Inc.) and cytotoxic chemotherapy. Bexarotene has also been investigated in the treatment of breast cancer and non-small cell carcinoma of the lung with promising early results.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
BexaroteneRetinoic acid receptor RXR-alphaProteinHumans
Yes
Agonist
Details
BexaroteneRetinoic acid receptor RXR-betaProteinHumans
Yes
Agonist
Details
BexaroteneRetinoic acid receptor RXR-gammaProteinHumans
Yes
Agonist
Details