Indication: For the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy
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 one prior systemic therapy. Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRa, RXRb, RXRg). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin Dy receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs). Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. It also induces tumor regression in vivo in some animal models.
Mechanism Of Action: The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.
Drug Category: Anticarcinogenic Agents; ATC:L01XX25
Brand Names/Synonyms: Bexarotene; Bexarotene [Usan]; LG 1069; LG 69; LGD 1069; LGD1096; Targret; Targretin; Targretyn; Targrexin
Dosage Forms: Not Available
Absorption: Not Available
Interactions:
DrugBank: Interactions for Bexarotene
Interactions for Bexarotene:
No formal studies to evaluate drug interactions with bexarotene have been conducted. Bexarotene oxidative
metabolites appear to be formed by cytochrome P450 3A4.
On the basis of the metabolism of bexarotene by cytochrome P450 3A4, ketoconazole, itraconazole, erythromycin,
gemfibrozil, grapefruit juice, and other inhibitors of cytochrome P450 3A4 would be expected to lead to an increase
in plasma bexarotene concentrations. Furthermore, rifampin, phenytoin, phenobarbital, and other inducers of
cytochrome P450 3A4 may cause a reduction in plasma bexarotene concentrations.
Concomitant administration of Targretin ® capsules and gemfibrozil resulted in substantial increases in plasma
concentrations of bexarotene, probably at least partially related to cytochrome P450 3A4 inhibition by gemfibrozil.
Under similar conditions, bexarotene concentrations were not affected by concomitant atorvastatin administration.
Concomitant administration of gemfibrozil with Targretin ® capsules is not recommended.
Chemical IUPAC Name: 4-[1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl]benzoicacid
Chemical Formula: C24H28O2
Half Life: 7 hours
Drug Type: Approved Drug
# Accession No: APRD00114
CAS Registry Number: 153559-49-0
Bexarotene News (When available)
Cephalon, Inc. Announces Agreement to Acquire Zeneus Holdings ...Dec 5, 2005 PR Newswire UK (press release), Myocet(R) (liposomal doxorubicin), a cardio-protective chemotherapy agent used to treat late-stage breast cancer; Targretin(R) (bexarotene), a treatment for ...
Biotech Racks Up Another Impressive Quarter to Close Year in ...Jan 3, 2006 PR Newswire (press release), ...several products already in the market including Myocet, a cardio-protective chemotherapy agent used to treat late-stage breast cancer; Targretin, a treatment ...
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