TARGRETIN- bexarotene capsule, liquid filled
Valeant Pharmaceuticals North America LLC
WARNING: BIRTH DEFECTS
TARGRETIN is a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene also caused birth defects when administered orally to pregnant rats. TARGRETIN must not be administered to a pregnant woman. (8.1)
1 INDICATIONS AND USAGE
TARGRETIN� (bexarotene) Capsules are indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.
2 DOSAGE AND ADMINISTRATION
The recommended initial dose of TARGRETIN is 300 mg/m2 /day (see Table 1). TARGRETIN should be taken as a single oral daily dose with a meal. For precautions to prevent pregnancy and birth defects in women of child-bearing potential.
DOSAGE FORMS AND STRENGTHS
Capsules: 75 mg, off-white, oblong soft gelatin capsules, imprinted with black ink "Targretin".
DESCRIPTION
TARGRETIN� (bexarotene) Capsules contain bexarotene, 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).
The chemical name of bexarotene is 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl] benzoic acid,
Bexarotene is an off-white to white powder with a molecular weight of 348.48 and a molecular formula of C24 H28 O2 . It is insoluble in water and slightly soluble in vegetable oils and ethanol, USP.
Each TARGRETIN capsule contains 75 mg of bexarotene for oral administration. It also contains the following inactive ingredients: polyethylene glycol 400, NF, polysorbate 20, NF, povidone, USP, and butylated hydroxyanisole, NF. The capsule shell contains gelatin, NF, sorbitol special-glycerin blend, and titanium dioxide, USP.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXR�, 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. 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. The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.
TARGRETIN� (bexarotene) Capsules are supplied as 75 mg off-white, oblong soft gelatin capsules, imprinted with "Targretin", in high density polyethylene bottles with child-resistant closures.
Bottles of 100 capsules: NDC 0187-5526-75
Store at 2� to 25�C (36� to 77�F). Avoid exposing to high temperatures and humidity after the bottle is opened. Protect from light.
