Getting to know TARGRETIN

The active ingredient in TARGRETIN is bexarotene

Bexarotene is in a subclass of retinoids (rexinoids) that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs).1,2

Selectively activated retinoid X receptors

Bexarotene selectively activates retinoid X receptors.

Activated receptors regulate gene expression in the cell.

Activated receptors regulate gene expression in the cell.

Inhibited tumor growth

Tumor growth is inhibited and regression is induced.

The exact mechanism of action of bexarotene in the treatment of CTCL is unknown.

Available as a gel or capsule

Indicated for

the topical treatment of cutaneous lesions from CTCL (Stage IA and IB) in patients who:Have refractory or persistent disease OR Have not tolerated other therapies.


bsa involvement

A topical treatment may be appropriate1,3

Indicated for

the treatment of cutaneous manifestations of CTCL in patients who:Are refractory to at least one prior systemic therapy.

About TARGRETIN capsules

bsa involvement

A systemic treatment may be appropriate2,3

Gel pharmacokinetics

In clinical studies with patients following single or multiple daily dose applications of TARGRETIN Gel1:

Animation of bexarotene plasma concentration

Samples from two patients with very intense dosing regimens (>40% BSA lesions and QID dosing) showed plasma concentrations of bexarotene were generally less than 5 ng/mL and did not exceed 55 ng/mL after repeated dosing up to 132 weeks.

Animation of body surface area

The frequency of detecting quantifiable plasma bexarotene increased with increasing body surface area (BSA) treated and increasing TARGRETIN gel applied.

Animation of dosage intensity
Animation of dosage intensity

In patients receiving doses of low to moderate intensity, there is a low potential for significant plasma concentrations following repeated application of TARGRETIN Gel. Plasma concentrations were studied up to 132 weeks.1

Capsule pharmacokinetics

The terminal half-life of bexarotene is approximately 7 hours.2

Dose linearity within the therapeutic range

Studies in patients with advanced tumors show dose linearity within the therapeutic range.

2 hours

Tmax of TARGRETIN Capsules is about 2 hours.


Recommended initial dose

The recommended initial dose for TARGRETIN Capsules is 300 mg/m2/day.2

Not recommended

Higher doses from pharmacokinetic studies

Doses up to 1000 mg/m2/day of TARGRETIN in patients with advanced CTCL did not induce acute toxic effects in pharmacokinetic studies.2


Important Safety Information and Indications

Important Safety Information


TARGRETIN capsules are 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 capsules must not be administered to a pregnant woman (8.1)


Both TARGRETIN capsules and TARGRETIN gel are contraindicated in women who are pregnant and in patients with a known hypersensitivity to bexarotene. If a woman becomes pregnant during treatment with TARGRETIN, treatment must be stopped immediately, and the woman provided appropriate counseling about the risks.

Contraception, Pregnancy Testing and Nursing

With both TARGRETIN capsules and TARGRETIN gel, to prevent pregnancy, effective contraception must be used for one month prior to the initiation of TARGRETIN therapy, during therapy and for at least one month following discontinuation of therapy; it is recommended that two reliable forms of contraception be used simultaneously unless abstinence is the chosen method. For TARGRETIN capsules, it is strongly recommended that one of the two reliable forms of contraception should be non-hormonal. Male patients with sexual partners who are pregnant, possibly pregnant or who could become pregnant must use condoms during treatment and for at least one month after the last dose of drug.

No more than a one-month supply of TARGRETIN should be given to the patient so that the results of pregnancy testing can be assessed and counseling regarding avoidance of pregnancy and birth defects can be reinforced.

For nursing women, a decision should be made whether to discontinue nursing or discontinue TARGRETIN gel, taking into account the importance of the drug to the mother. Because of the potential for serious adverse reactions in nursing infants from TARGRETIN capsules, discontinue breastfeeding during treatment with TARGRETIN capsules.

Warnings and Precautions
TARGRETIN capsules and TARGRETIN gel

Vitamin A Supplementation: Patients should be advised to limit Vitamin A intake to avoid potential additive toxicity.

Photosensitivity: Advise patients to minimize exposure to the sun and artificial sunlight during treatment.

TARGRETIN capsules

Hyperlipidemia is present in most patients treated with TARGRETIN capsules. Obtain baseline values, monitor during treatment, and manage elevations during therapy.

Acute pancreatitis, including a fatal case, has been reported in patients treated with TARGRETIN capsules. Interrupt treatment and evaluate if suspected.

Hepatotoxicity, cholestasis, and hepatic failure: TARGRETIN capsules had a dose-related effect on liver chemistry tests in clinical trials, including incidence of cholestasis and liver failure.

Hypothyroidism: TARGRETIN capsules induce hypothyroidism in about half of all patients; obtain baseline thyroid function tests. Monitor and replace thyroid hormone if needed during treatment.

Neutropenia: Leukopenia and neutropenia occurred in clinical trials with TARGRETIN capsules; obtain complete blood counts at baseline and periodically during treatment. Reduce TARGRETIN dose or interrupt as indicated.

Hypoglycemia in Patients with Diabetes: TARGRETIN capsules may cause hypoglycemia in patients using insulin, agents enhancing insulin secretions, or insulin-sensitizers.

Laboratory tests including CBC, fasting lipid profile, liver function tests, and thyroid profile should be obtained prior to and monitored during treatment.

CA125 assay values in ovarian cancer patients may be elevated by treatment with TARGRETIN capsules.

Cataracts: Although a causal relationship has not been established, cataracts have been observed in animal and clinical studies with TARGRETIN capsules. Refer patients who experience visual difficulties for ophthalmologic evaluation.

Adverse Reactions

The most common adverse reactions (≥10%) include rash, pruritus, pain, and skin disorder.

TARGRETIN capsules

The most common adverse reactions (>10%) include hyperlipidemia, hypercholesteremia, headache, hypothyroidism, asthenia, leukopenia, rash, nausea, infection, peripheral edema, abdominal pain, and dry skin.

To report SUSPECTED ADVERSE REACTIONS contact customer service at 1-800-321-4576 or FDA at 1-800-FDA-1088 or visit

Indications and usage

TARGRETIN® (bexarotene) gel is indicated for the topical treatment of cutaneous lesions in patients with cutaneous T-cell lymphoma, CTCL (Stage 1A and 1B) who have refractory or persistent disease after other therapies or who have not tolerated other therapies. TARGRETIN® (bexarotene) capsules is indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma (CTCL) in patients who are refractory to at least one prior systemic therapy.

Please click here for full Prescribing Information, including Boxed Warning for TARGRETIN capsules

Please click here for full Prescribing information for TARGRETIN gel

  1. TARGRETIN gel 1% [prescribing information]. Bridgewater, NJ: Bausch Health US, LLC.
  2. TARGRETIN 75 mg capsules [prescribing information]. Bridgewater, NJ: Bausch Health US, LLC.
  3. Olsen E, Vonderheid E, Pimpinelli N, et al. Revisions to the staging and classification of mycosis fungoides and S├ęzary syndrome: a proposal of the International Society for Cutaneous Lymphomas (ISCL) and the cutaneous lymphoma task force of the European Organization of Research and Treatment of Cancer (EORTC). Blood. 2007;110(6):1713-1722.