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.

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

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

Indication and usage

TARGRETIN® (bexarotene) capsules and gel are indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma (only stages 1A and 1B for gel) in patients who are refractory to at least one prior systemic therapy.

Important Safety Information

Birth defects

Because of the risk of fetal harm, TARGRETIN capsules and gel must not be given to a woman who is pregnant or who intends to become pregnant. If a woman becomes pregnant during treatment with TARGRETIN, treatment must be stopped immediately, and the woman provided appropriate counseling about the risks.

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. 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.


TARGRETIN capsules and gel are contraindicated in patients with a known serious hypersensitivity to bexarotene or other components of the product.

Warnings and precautions

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 and monitor patients during treatment.

Neutropenia Leukopenia and neutropenia occurred in clinical trials with TARGRETIN capsules; obtain complete blood counts at baseline and periodically during treatment.

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.

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

Nursing: Discontinue nursing during treatment with TARGRETIN.

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

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

Capsules and Gel

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

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


Patients who are applying TARGRETIN gel should not concurrently use products that contain DEET, a common component of insect repellent products.

For nursing women, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Adverse reactions

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


The most common adverse events reported in TARGRETIN gel clinical trials with an incidence at the application site of at least 10% were: rash, pruritus, skin disorder, and pain.

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

Click here for full Prescribing Information, including Boxed Warning for TARGRETIN capsules.

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 Sézary 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.