Difference between revisions of "Bexarotene (Targretin)"

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==General information==
 
==General information==
Class/mechanism: Retinoid, selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ), which allow them to 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. Exact mechanism of action in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.<ref name="insert">[http://targretin.com/pdf/CAPS-PI-Jan18.pdf Bexarotene (Targretin) capsules package insert]</ref><ref>[[Media:Bexarotene.pdf | Bexarotene (Targretin) capsules package insert (locally hosted backup)]]</ref><ref name="insert_gel">[http://targretin.com/pdf/GEL-PI-Jan-18.pdf Bexarotene (Targretin) gel package insert]</ref><ref>[[Media:Bexarotenegel.pdf | Bexarotene (Targretin) gel package insert (locally hosted backup)]]</ref><ref>[http://targretin.com/ Targretin manufacturer's website]</ref>
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Class/mechanism: Retinoid, selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ), which allow them to 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. Exact mechanism of action in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.<ref name="insert">[http://targretin.com/pdf/CAPS-PI-Jan18.pdf Bexarotene (Targretin) capsules package insert]</ref><ref>[[:File:Bexarotene.pdf | Bexarotene (Targretin) capsules package insert (locally hosted backup)]]</ref><ref name="insert_gel">[http://targretin.com/pdf/GEL-PI-Jan-18.pdf Bexarotene (Targretin) gel package insert]</ref><ref>[[:File:Bexarotenegel.pdf | Bexarotene (Targretin) gel package insert (locally hosted backup)]]</ref><ref>[http://targretin.com/ Targretin manufacturer's website]</ref>
 
<br>Route: PO, topical
 
<br>Route: PO, topical
 
<br>Extravasation: n/a
 
<br>Extravasation: n/a
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*[http://targretin.com/pdf/CAPS-PI-Jan18.pdf Bexarotene (Targretin) capsules package insert]<ref name="insert"></ref>
 
*[http://targretin.com/pdf/CAPS-PI-Jan18.pdf Bexarotene (Targretin) capsules package insert]<ref name="insert"></ref>
 
*[http://targretin.com/pdf/GEL-PI-Jan-18.pdf Bexarotene (Targretin) gel package insert]<ref name="insert_gel"></ref>
 
*[http://targretin.com/pdf/GEL-PI-Jan-18.pdf Bexarotene (Targretin) gel package insert]<ref name="insert_gel"></ref>
*[http://chemocare.com/chemotherapy/drug-info/bexarotene.aspx Bexarotene systemic (Targretin) patient drug information (Chemocare)]<ref>[http://chemocare.com/chemotherapy/drug-info/bexarotene.aspx Bexarotene systemic (Targretin) patient drug information (Chemocare)]</ref>
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*[https://chemocare.com/druginfo/bexarotene.aspx Bexarotene systemic (Targretin) patient drug information (Chemocare)]<ref>[https://chemocare.com/druginfo/bexarotene.aspx Bexarotene systemic (Targretin) patient drug information (Chemocare)]</ref>
 
*[http://www.uptodate.com/contents/bexarotene-systemic-patient-drug-information Bexarotene systemic (Targretin) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/bexarotene-systemic-patient-drug-information Bexarotene systemic (Targretin) patient drug information (UpToDate)]</ref>
 
*[http://www.uptodate.com/contents/bexarotene-systemic-patient-drug-information Bexarotene systemic (Targretin) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/bexarotene-systemic-patient-drug-information Bexarotene systemic (Targretin) patient drug information (UpToDate)]</ref>
 
*[http://www.uptodate.com/contents/bexarotene-topical-patient-drug-information Bexarotene topical (Targretin) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/bexarotene-topical-patient-drug-information Bexarotene topical (Targretin) patient drug information (UpToDate)]</ref>
 
*[http://www.uptodate.com/contents/bexarotene-topical-patient-drug-information Bexarotene topical (Targretin) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/bexarotene-topical-patient-drug-information Bexarotene topical (Targretin) patient drug information (UpToDate)]</ref>
  
 
==History of changes in FDA indication==
 
==History of changes in FDA indication==
* 12/29/1999: Initial FDA approval "for the treatment of cutaneous manifestations of [[cutaneous T-cell lymphoma]] in patients who are refractory to at least one prior systemic therapy."
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* 1999-12-29: Initial approval for the treatment of cutaneous manifestations of [[cutaneous T-cell lymphoma]] in patients who are refractory to at least one prior systemic therapy. ''(Based on Duvic et al. 2001a & Duvic et al. 2001b)''
 
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==History of changes in EMA indication==
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*2001-03-29: Initial authorization
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==History of changes in PMDA indication==
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*2016-01-22: Initial approval for the treatment of [[cutaneous T-cell lymphoma]].
 
==Also known as==
 
==Also known as==
*'''Code name:''' LGD1069
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*'''Code name:''' LGD-1069
 
*'''Brand names:''' Bexgratin, Targretin
 
*'''Brand names:''' Bexgratin, Targretin
  
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[[Category:FDA approved in 1999]]
 
[[Category:FDA approved in 1999]]
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[[Category:EMA approved in 2001]]
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[[Category:PMDA approved in 2016]]

Latest revision as of 23:39, 2 September 2023

General information

Class/mechanism: Retinoid, selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ), which allow them to 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. Exact mechanism of action in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.[1][2][3][4][5]
Route: PO, topical
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape,UpToDate (courtesy of Lexicomp), or the prescribing information.[1][3]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 1999-12-29: Initial approval for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy. (Based on Duvic et al. 2001a & Duvic et al. 2001b)

History of changes in EMA indication

  • 2001-03-29: Initial authorization

History of changes in PMDA indication

Also known as

  • Code name: LGD-1069
  • Brand names: Bexgratin, Targretin

References