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Bexarotene
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| Systematic (IUPAC) name | |
| 4-[1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl] benzoic acid |
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| Identifiers | |
| CAS number | |
| ATC code | L01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C24H28O2 |
| Mol. mass | 348.478 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | >99% |
| Metabolism | Bexarotene undergoes oxidative metabolism via CYP450 3A4 and its metabolites are then glucuronidated. Four bexarotene metabolites have been identified in the plasma: 6- and 7- hydroxy-bexarotene and 6-and 7-oxo-bexarotene. All of the metabolites are active in vitro, but their clinical significance is not known. |
| Half life | 7 hours |
| Excretion | Parent drug and metabolites are eliminated primarily through the hepatobiliary system. Less than 1% is excreted in the urine unchanged. |
| Therapeutic considerations | |
| Pregnancy cat. |
X |
| Legal status | |
| Routes | Oral and Topical |
Bexarotene (Targretin) is an oral antineoplastic agent indicated by the FDA for cutaneous T cell lymphoma.[1] It has been used off-label for lung cancer,[2] breast cancer, and Kaposi's sarcoma.
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Bexarotene is a retinoid specifically selective for retinoid X receptors, as opposed to the retinoic acid receptors.
RXRs are located primarily in visceral organs such as the liver and kidney. Activated RXRs form homodimers or heterodimers with RAR (retinoic acid receptors), vitamin D receptors, thyroid receptors or peroxisome proliferator activator receptors. Once activated, these retinoid receptor dimers bind to DNA at retinoic acid response elements and act as transcription factors that regulate the expression of genes which control cellular differentiation and proliferation. Retinoid agonists can activate the expression of retinoid regulated genes by removing negative transcription control or by facilitating positive transcriptional activity. They exert anticancer action by interfering with the growth of cells of the tumor.
Bexarotene is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy (oral) and for the topical treatment of cutaneous lesions in patients with CTCL (Stage IA and IB) who have refractory or persistent disease after other therapies or who have not tolerated other therapies (topical).
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