Bexarotene

Review and update by

The Cutaneous Lymphoma Foundation's Writers Bureau 

What is bexarotene?

Brand Name: Targretin®
Generic is available

Bexarotene is in the family of retinoids, which are synthetic versions of vitamin A. Bexarotene activates a specific type of retinoid receptor (known as RXR) and influences cancer cell growth and differentiation.

It is used to treat cutaneous T-cell lymphoma (CTCL).

How is it delivered?

TOPICAL BEXAROTENE 1% GEL
Topical bexarotene is approved by the U.S. Food and Drug Administration (FDA) for the treatment of Stage 1A and 1B CTCL in patients who have not responded to, or tolerated, other therapies. In clinical practice, the topical retinoid class of drugs like bexarotene are often considered second line therapy for patients who have demonstrated persistent disease after treatment with topical corticosteroids or other skin directed therapies.

It is applied to affected lesions between 1-4 times per day as tolerated.

Topical bexarotene gel can find an effective and perhaps niche role in treating more sensitive and photoprotected areas (such as armpit or groin areas). This is where this medication may find its most useful role as other skin-directed therapies are typically more effective, but more difficult to use or irritating in these sensitive regions.

ORAL BEXAROTENE CAPSULES
Oral bexarotene has been shown to be effective in treating CTCL when administered systemically in capsule form. Oral bexarotene has been approved for the treatment of all stages of CTCL. It may be given as a single agent or may be combined with other forms of therapy. 
 

What is the expected result?

TOPICAL BEXAROTENE:
Median response with bexarotene gel for CTCL is 20 weeks, and overall response rate was 44%-54%.

ORAL BEXAROTENE:
A study of advanced stage CTCL patients treated with oral bexarotene yielded response rates of 45-55%.

Are There Special Considerations To Be Aware Of?

ORAL BEXAROTENE: It may be given as a single agent or may be combined with other forms of therapy.  

Most patients require several months of this oral therapy before improvement is observed.

What are Common Side Effects?

The following is not an exhaustive list of the possible side effects. For a complete list of possible side effects, please see the manufacturer's available information on the specific therapy.

TOPICAL BEXAROTENE: 
Common side effects from topical retinoids, including topical bexarotene, include skin irritation, redness, itching, rash, and burning. These local side effects can be reduced by gradual increase in frequency of application when starting or by combining with topical steroids to treat the irritation.

Skin treated with topical retinoids should be protected from prolonged exposure to sunlight or other sources of ultraviolet (UV) light, such as tanning lamps.

Because retinoids are teratogenic, bexarotene gel is considered contraindicated in pregnant patients (pregnancy category X).

ORAL BEXAROTENE:
Blood tests to monitor side effects are required while taking oral bexarotene. An increase in the blood levels of lipids (fats) is very common. Medications to lower cholesterol and triglyceride levels are often prescribed to patients taking bexarotene. Decreased thyroid levels, which can cause fatigue, can be a side effect of bexarotene and are monitored closely throughout the course. Oral bexarotene should be AVOIDED in patients who are pregnant, as it can cause birth defects (pregnancy category X). Oral bexarotene can be photosensitizing, so patients are recommended to avoid prolonged UV light exposure. 

 

 

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