Bexarotene: profile and news






Bexarotene Gel 1% Enhances Efficacy of Phototherapy for Psoriasis ...  06 Mar 2006
SAN FRANCISCO, CA -- March 6, 2006 -- Treatment with bexarotene gel 1% appears to enhance the efficacy of narrowband ultraviolet B (UVB) phototherapy with ... - DG News

New treatment could knock out asthma  Feb 7, 2006
Louis. And, here's even better news: The compound, called bexarotene, doesn't cause the severe skin irritations that have limited the use of other vitamin A ... - Belleville News-Democrat,

Bexarotene shows promise in cancer treatment.  Jan 18, 2006
The compound, called bexarotene, doesn't cause the severe skin irritations that have limited the use of other vitamin A derivatives in cancer therapies. ... - News-Medical.net,

Vitamin A analog bexarotene fights lung cancer  Jan 17, 2006
Bexarotene is already used to treat a form of cancer known as cutaneous T-cell lymphoma (CTCL). It acts to interfere with the growth of tumor cells. ... - Food Consumer,

Vitamin A analog bexarotene helps prevent lung cancer  Jan 17, 2006
As a result, bexarotene reduced the total tumor burden by 50 percent in the mice. Also, bexarotene lowered the risk of benign tumor ... - Food Consumer,

New treatment could knock out asthma  Feb 7, 2006
Louis. And, here's even better news: The compound, called bexarotene, doesn't cause the severe skin irritations that have limited the use of other vitamin A ... - Belleville News-Democrat,

Vitamin A-Like Compound Fights Lung Cancer  Jan 24, 2006
The compound bexarotene put the brakes on lung tumors in mice genetically engineered to be susceptible to the cancer, say researchers at the Washington ... - HealthCentral.com

Drug derived from vitamin A slows lung cancer in mice  Jan 18, 2006
...of the Chemoprevention Program at the Siteman Cancer Center at Washington University, the researchers found that the compound, called bexarotene, also doesn't ... - Cancerfacts.com,

Vitamin A for lung cancer?  Jan 21, 2006
A group of US scientists has discovered that a new type of vitamin A called bexarotene possesses a potent anti-cancer property against lung cancer, according ... - myDNA.com,

Compound in vitamin A can prevent lung cancer  Jan 18, 2006
The compound, called bexarotene, besides preventing tumour growth, also doesn't cause the severe skin irritations that have limited the use of other vitamin A ... - Webindia123,

Cephalon, Inc. Announces Agreement to Acquire Zeneus Holdings ...  Dec 5, 2005
Myocet(R) (liposomal doxorubicin), a cardio-protective chemotherapy agent used to treat late-stage breast cancer; Targretin(R) (bexarotene), a treatment for ... - PR Newswire UK (press release),

Biotechnology and Pharmaceutical Executives to Convene at SRI ...  Oct 12, 2005
...undergoing preclinical evaluation. Marketed examples of these drugs include bexarotene and halofantrine. Additionally, working with ... - Business Wire (press release),

Allogeneic Stem Cell Transplants Effective for Refractory ...  Sep 6, 2005
...include psoralen and ultraviolet A radiation (PUVA), interferon alfa, local radiation therapy, electron beam therapy, bexarotene, topical chemotherapy ... - Cancer Consultants (press release),

New Developments in Treatment of Advanced Non-Small-Cell Lung ...  Aug 19, 2005
Gatzemeier and colleagues reported the results of a phase 3 trial (SPIRIT II) incorporating the selective retinoid X receptor agonist bexarotene into standard ... - Medscape (subscription)

New Accutane controls praised by March of Dimes, USA  Aug 13, 2005
Claravis, and Sotret. Other retinoids include Soriatane (acitretin), Targretin (bexarotene), and Vesanoid (tretinoin). In a January ... - Medical News Today (press release), <**results**>

Investigators Present Targretin(R) Data at World Lung Cancer ...  Jul 5, 2005
Results of Ligand Pharmaceuticals Incorporated (Nasdaq:LGNDE) two pivotal Phase III studies (SPIRIT I & SPIRIT II) of Targretin(R) (bexarotene) capsules in ... - Genetic Engineering News

SRI International Celebrates 50 Years of Drug Discovery and ...  Jun 20, 2005
Bexarotene was discovered at SRI and is marketed for cutaneous T-cell lymphoma. SRI has more than a dozen cancer drugs in R&D, including: ... - Business Wire (press release)

SRI International Celebrates 50 Years of Drug Discovery and ...  Jun 20, 2005
Division since its inception. Bexarotene was discovered at SRI and is marketed for cutaneous T-cell lymphoma. SRI has more than ... - PharmaLive.com (press release),

SRI International Celebrates 50 Years of Drug Discovery and ...  Jun 20, 2005
Bexarotene was discovered at SRI and is marketed for cutaneous T-cell lymphoma. SRI has more than a dozen cancer drugs in R&D, including: ... - Business Wire (press release),

SRI International Celebrates 50 Years of Drug Discovery and ...  Jun 20, 2005
Division since its inception. Bexarotene was discovered at SRI and is marketed for cutaneous T-cell lymphoma. SRI has more than ... - PharmaLive.com (press release),


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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