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Drugs of interest to pathologists

Drugs related to surgical pathology and clinical pathology

Bexarotene

Author: Him G. Kwee, M.D. (see Reviewers/Authors page)
Revised: 22 December 2011, last major update December 2011
Copyright: (c) 2011, PathologyOutlines.com, Inc.

General
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● A retinoid that selectively activates retinoid X receptors

Trade name
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● Targretin (oral and topical)

Clinical information
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Approved by US Food and Drug Administration for:
● Cutaneous T-cell lymphoma (CTCL) that is refractory to at least one prior systemic therapy
● The oral capsules are used for generalized CTCL and the topical gel is used for localized plaques with CTCL

● It has been used “off-label” for lung carcinoma, breast carcinoma and Kaposi’s sarcoma (Wikipedia)
● A clinical trial using bexarotene gel for alopecia areata is in progress

● Approximate costs: $2600 for 30 days oral therapy for adult taking 150 mg (Drugstore.com), $1800 for 60 gm topical gel (link)

Pathophysiology
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● Bexarotene selectively binds and activates retinoid X receptors RXR-alpha, RXR-beta and RXR-gamma
● RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor and peroxisome proliferator activitor receptors (PPARs)
● Once activated, these receptors function as transcripton factors that regulate the expression of genes that control cellular differentiation and proliferation
● However, the exact mechanism of action of bexarotene in the treatment of CTCL is unknown (Drugs.com)

Side effects
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● Lipids: bexarotene can cause elevations in serum triglyceride and LDL cholesterol and a decrease in HDL cholesterol; the triglyceride elevation can cause acute pancreatitis
● Liver: elevations in AST, ALT, bilirubin, LDH, cholestasis and liver failure
● Skin: photosensitivity, acne, rash (macular, papular, vesicular, bullous or pustular), alopecia and exfoliative dermatitis (Physicians’ Desk Reference, 66th ed, 2012, page 934)
● Thyroid: decreases in TSH and T4 with hypothyroidism
● Blood counts: leukopenia, neutropenia, anemia, eosinophilia, increase or decrease in platelet count
● May cause false increase in serum CA-125 assay values

End of Drugs > Drugs related to surgical pathology and clinical pathology > Bexarotene

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