Bexarotene

drugbox
IUPAC_name = 4- [1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl]
benzoic acid

---

width = 150
CAS_number = 153559-49-0
ATC_prefix = L01
ATC_suffix = XX25
PubChem = 82146
DrugBank = APRD00114
C=24 | H=28 | O=2
molecular_weight = 348.478 g/mol
bioavailability =
protein_bound = >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.
elimination_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.
pregnancy_AU =
pregnancy_US =
pregnancy_category = X
legal_AU =
legal_UK =
legal_US =
legal_status =
routes_of_administration = Oral and Topical

Bexarotene (Targretin) is an oral antineoplastic agent indicated by the FDA for cutaneous T cell lymphoma.cite journal |author=Gniadecki R, Assaf C, Bagot M, "et al" |title=The optimal use of bexarotene in cutaneous T-cell lymphoma |journal=Br. J. Dermatol. |volume=157 |issue=3 |pages=433–40 |year=2007 |pmid=17553039 |doi=10.1111/j.1365-2133.2007.07975.x] It has been used off-label for lung cancer,cite journal |author=Dragnev KH, Petty WJ, Shah SJ, "et al" |title=A proof-of-principle clinical trial of bexarotene in patients with non-small cell lung cancer |journal=Clin. Cancer Res. |volume=13 |issue=6 |pages=1794–800 |year=2007 |pmid=17363535 |doi=10.1158/1078-0432.CCR-06-1836] breast cancer, and Kaposi's sarcoma.

Mechanism

Bexarotene is a rexinoid 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.

Clinical uses

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).

External links

* [http://www.eisai.com/pdf_files/TargretinCapsPI%20ver-1%20ver-1%20jan07.pdf Targretin prescribing information (capsules)]
* [http://www.eisai.com/pdf_files/TargretinGelM%20PI%20rev-1%20ver-1%20jan07.pdf Targretin prescribing information (topical gel)]

References