Targretin (Northern Ireland)

Targretin (Northern Ireland) Uses, Dosage, Side Effects, Food Interaction and all others data.

Targretin (Northern Ireland) (Targretin) is an antineoplastic agent indicated by the FDA for Cutaneous T cell lymphoma. It has been used off-label for lung cancer, breast cancer, and Kaposi's sarcoma.

Targretin (Northern Ireland) 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). Targretin (Northern Ireland) 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. Targretin (Northern Ireland) selectively binds and activates retinoid X receptor subtypes (RXRα, RXRβ, RXRγ). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D 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. Targretin (Northern Ireland) 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.

Targretin (Northern Ireland)
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Targretin (Northern Ireland)
Availability	Prescription only
Generic	Bexarotene
Bexarotene Other Names	Bexaroten, Bexarotène, Bexarotene, Bexaroteno, Bexarotenum
Related Drugs	methoxsalen, Targretin, romidepsin, vorinostat, Targretin Gel, Actimmune
Type
Formula	C₂₄H₂₈O₂
Weight	Average: 348.4779 Monoisotopic: 348.20893014
Protein binding	>99%
Groups	Approved, Investigational
Therapeutic Class
Manufacturer	Eisai Ltd
Available Country	United Kingdom
Last Updated:	September 19, 2023 at 7:00 am

Uses

Targretin (Northern Ireland) is a retinoid drug used for cutaneous manifestations of T-cell lymphoma in patients who have not responded well to previous systemic therapy.

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.

Targretin (Northern Ireland) is also used to associated treatment for these conditions: Refractory peripheral cutaneous T-cell lymphoma

How Targretin (Northern Ireland) works

Targretin (Northern Ireland) selectively binds with and activates retinoid X receptor subtypes. There are three subtypes in total: RXR_α, RXR_β, RXR_γ. 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.

Food Interaction

Take with food.

[Moderate] ADJUST DOSING INTERVAL: Food may enhance the oral bioavailability of bexarotene.

In one clinical study, bexarotene peak plasma concentration (Cmax) and systemic exposure (AUC) resulting from a 75 to 300 mg dose were 35% and 48% higher, respectively, when administered after a fat-containing meal relative to a glucose solution.

In all clinical trials, patients were instructed to take bexarotene with or immediately following a meal.

Coadministration with inhibitors of CYP450 3A4 such as grapefruit juice may theoretically increase the plasma concentrations of bexarotene.

In vitro studies suggest that bexarotene is metabolized by CYP450 3A4.

However, concomitant administration with multiple doses of ketoconazole, a potent CYP450 3A4 inhibitor, did not alter bexarotene plasma concentrations, which would imply that bexarotene elimination is not substantially dependent on CYP450 3A4 metabolism in vivo.

MANAGEMENT: Because safety and efficacy data are based upon administration with food, bexarotene should be administered once daily with a meal.

Patients may want to avoid consuming large amounts of grapefruit or grapefruit juice.

Targretin (Northern Ireland) Cholesterol interaction

[Moderate] The use of bexarotene may cause elevations in lipids.

It is recommended to monitor lipid levels closely and to obtain a fasting blood lipid reading at baseline and weekly until lipid response to the drug is established.

Exercise caution when using this agent in patients with hyperlipidemia.