|Systematic (IUPAC) name|
|4‑[1‑(3,5,5,8,8‑pentamethyltetralin-2‑yl)ethenyl] benzoic acid|
|Routes||Oral and topical|
|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.|
|Excretion||Parent drug and metabolites are eliminated primarily through the hepatobiliary system. Less than 1% is excreted in the urine unchanged.|
|Mol. mass||348.478 g/mol|
| (what is this?)
Bexarotene (tradenamed Targretin) is an oral antineoplastic agent indicated by the U.S. Food and Drug Administration (FDA) (in 2000) for cutaneous T cell lymphoma. It has been used off-label for lung cancer, breast cancer, and Kaposi's sarcoma.
Bexarotene is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in people who are refractory to at least one prior systemic therapy (oral) and for the topical treatment of cutaneous lesions in patients with CTCL who have refractory or persistent disease after other therapies or who have not tolerated other therapies (topical).
RXRs are located primarily in visceral organs such as the liver and kidney. Activated RXRs form homodimers or heterodimers with retinoic acid receptors, vitamin D receptors, thyroid receptors or peroxisome proliferator-activated 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.
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The developer of bexarotene (brand name Targretin) was Ligand Pharmaceuticals, a San Diego biotech company which received FDA approval for the drug in 1999. Japanese pharmaceutical Eisai bought the rights to Targretin and three other anti-cancer products from Ligand in 2006.
In 2012 it was announced in an epub ahead of print that researchers had discovered that bexarotene reduced amyloid plaque and improved mental functioning in a small sample of mice engineered to exhibit Alzheimer's symptoms. Three different mouse models (APP/PS1, APPPS1-21, Tg2576) were used. It is thought that bexarotene stimulates expression of apolipoprotein E (ApoE), which leads to intracellular clearance of β-Amyloid. The authors of the research article said, "We've fixed Alzheimer's in mice lots of times, so we need to move forward expeditiously but cautiously", and expect to start a safety study with healthy human subjects by February 2013. The chief executive of the Alzheimer's Foundation of America said that people desperate to find a treatment for Alzheimer's should not take matters into "their own hands" or rush to take the medication.
M. F. Boehm, R. A. Heyman, L. Zhi, C. K. Hwang, S. White, A. Nadzan, U.S. Patent 5,780,676 (1998).
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