BEXAROTENE

Other

Brand names: Targretin

Oral

Mechanism of Action

12.1 Mechanism of Action Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRß, RXRγ). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs). Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. It also induces tumor regression in vivo in some animal models. The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.

Indications

See full prescribing information

Contraindications

• 4 CONTRAINDICATIONS • Pregnancy (Boxed Warning

FDA Warnings

5 WARNINGS AND PRECAUTIONS • Hyperlipidemia: TARGRETIN causes elevations in blood lipids
Maintain triglyceride levels below 400 mg/dL to reduce the risk of clinical sequelae [ see Warnings and Precautions (5
2 Pancreatitis Acute pancreatitis, including a fatal case, has been reported in four patients with CTCL and in six patients with non-CTCL cancers treated with TARGRETIN; the cases were associated with marked elevations of fasting serum triglycerides, the lowest being 770 mg/dL in one patient
Patients with CTCL who have risk factors for pancreatitis (e

Known Side Effects

6 documented side effects by frequency

Drug Not Working

>10%

Fatigue

1-10%

Itching

1-10%

Condition Worsened

1-10%

Nausea

0.1-1%

Fever

0.1-1%

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Formulations

Dosage Forms

Tablet

Route

Oral