Targretin
Targretin Uses, Dosage, Side Effects, Food Interaction and all others data.
Targretin (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 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 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 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 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.
| Trade Name | Targretin |
| Availability | Prescription only |
| Generic | Bexarotene |
| Bexarotene Other Names | Bexaroten, Bexarotène, Bexarotene, Bexaroteno, Bexarotenum |
| Related Drugs | methoxsalen, Targretin, romidepsin, vorinostat, Targretin Gel, Actimmune |
| Weight | 75mg, |
| Type | Oral Capsule, Gel, Topical |
| Formula | C24H28O2 |
| Weight | Average: 348.4779 Monoisotopic: 348.20893014 |
| Protein binding | >99% |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Eisai Ltd, Eisai Ltd |
| Available Country | United Kingdom, United States, France, Italy, Netherlands, Spain, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Targretin 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 is also used to associated treatment for these conditions: Refractory peripheral cutaneous T-cell lymphoma
How Targretin works
Targretin selectively binds with and activates retinoid X receptor subtypes. There are three subtypes in total: RXRα, RXRβ, RXRγ. 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 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.
Targretin Drug Interaction
Major: valproic acid, valproic acidUnknown: arginine, arginine, levocarnitine, levocarnitine, cysteine, cysteine, lithium, lithium, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, cholecalciferol, cholecalciferol, phytonadione, phytonadione, menaquinone, menaquinone
Targretin Disease Interaction
Moderate: cataracts, diabetes, hyperlipidemia, hypothyroidism, liver dysfunction, neutropenia, pancreatitis
Half Life
7 hours
Elimination Route
Urinary elimination of bexarotene and its known metabolites is a minor excretory pathway (<1% of administered dose).
Innovators Monograph
You find simplified version here Targretin
