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QuickView for Bexarotene (compound)


PubChem
Name: bexarotene
PubChem Compound ID: 10337961
Molecular formula: C24H28O2
Molecular weight: 350.47 g/mol
DrugBank
Identification
Name: bexarotene
Name (isomeric): DB00307
Drug Type: small molecule
Brand: Targretyn, Targretin, Targret, Targretin-gel, Targrexin
Category: Anticarcinogenic Agents
CAS number: 153559-49-0
Pharmacology
Indication: Used orally for the treatment of skin manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy. Also used topically for the treatment of skin lesions in early (stage IA and IB) CTCL in patients who experience refractory or persistent disease with the use of other therapies or are intolerant of other therapies.
Pharmacology:
Bexarotene is a member of a subclass of retinoids that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs). Bexarotene is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least o...
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Mechanism of Action: Bexarotene selectively binds with and activates retinoid X receptor subtypes. There are three subtypes in total: RXRα, RXRβ, RXRγ. The exact mechanism of action of bexarotene in the treatment of CTCL is unknown but the drug has activity in all clinical stages of CTCL.
Protein binding: >99%
Route of elimination: Urinary elimination of bexarotene and its known metabolites is a minor excretory pathway (<1% of administered dose).
Half Life: 7 hours
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
NorgestimateBexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of norgestimate, it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
EtonogestrelBexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of etonogestrel, it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
DoxycyclineTetracycline derivatives like doxycycline may enhance the adverse/toxic effect of Retinoic Acid Derivatives. Due to the risk of developing pseudotumor cerebri (also known as intracranial hypertension), avoid this combination of drugs if possible. If used concomitantly, monitor for evidence of this interaction (eg, dizziness, diplopia, headache).
estrogenBexarotene may decrease the serum concentration of contraceptives (estrogens) and is teratogenic. Women of childbearing age receiving bexarotene should use two forms of contraception, including at least one non-hormonal form.
Ethynodiol DiacetateBexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of ethynodiol diacetate it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
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Enzymes