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Bexarotene: profile and news
Bexarotene Gel 1% Enhances Efficacy of Phototherapy for Psoriasis ... 06 Mar 2006 New treatment could knock out asthma Feb 7, 2006 Bexarotene shows promise in cancer treatment. Jan 18, 2006 Vitamin A analog bexarotene fights lung cancer Jan 17, 2006 Vitamin A analog bexarotene helps prevent lung cancer Jan 17, 2006 New treatment could knock out asthma Feb 7, 2006 Vitamin A-Like Compound Fights Lung Cancer Jan 24, 2006 Drug derived from vitamin A slows lung cancer in mice Jan 18, 2006 Vitamin A for lung cancer? Jan 21, 2006 Compound in vitamin A can prevent lung cancer Jan 18, 2006 Cephalon, Inc. Announces Agreement to Acquire Zeneus Holdings ... Dec 5, 2005 Biotechnology and Pharmaceutical Executives to Convene at SRI ... Oct 12, 2005 Allogeneic Stem Cell Transplants Effective for Refractory ... Sep 6, 2005 New Developments in Treatment of Advanced Non-Small-Cell Lung ... Aug 19, 2005 New Accutane controls praised by March of Dimes, USA Aug 13, 2005 Investigators Present Targretin(R) Data at World Lung Cancer ... Jul 5, 2005 SRI International Celebrates 50 Years of Drug Discovery and ... Jun 20, 2005 SRI International Celebrates 50 Years of Drug Discovery and ... Jun 20, 2005 SRI International Celebrates 50 Years of Drug Discovery and ... Jun 20, 2005 SRI International Celebrates 50 Years of Drug Discovery and ... Jun 20, 2005 Other information 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 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 |
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