Last reviewed 2026-04-20 · How we verify

Targretin (BEXAROTENE)

Targretin works by binding to the retinoic acid receptor RXR-beta, which helps regulate cell growth and differentiation.

Targretin (BEXAROTENE) is a small molecule retinoid that targets the retinoic acid receptor RXR-beta. It was originally developed by VALEANT LUXEMBOURG and is now owned by Bausch. Targretin was FDA-approved in 1999 for the treatment of primary cutaneous T-cell lymphoma. The drug is off-patent and has multiple generic manufacturers. As an off-patent medication, Targretin's commercial status is primarily driven by generic competition.

At a glance

Mechanism of action

Mechanism of Action. Bexarotene selectively binds and activates retinoid receptor subtypes (RXR, RXR, RXR). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin 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.

Approved indications

• Primary cutaneous T-cell lymphoma

Boxed warnings

• 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 ) WARNING: BIRTH DEFECTS See full prescribing information for complete boxed warning. 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 )

Common side effects

• Rash
• Pruritus
• Pain
• Skin Disorder
• Contact Dermatitis
• Headache
• Exfoliative Dermatitis
• Sweating
• Asthenia
• Paresthesia
• Leukopenia
• Lymphadenopathy

Drug interactions

• gemfibrozil

Key clinical trials

• A Study of Bexarotene Combined With Radiotherapy in People With Mycosis Fungoides (PHASE1)
• The Role of Bexarotene in Inducing Susceptibility to Chemotherapy in Metastatic TNBC (PHASE1)
• Triamcinolone Acetonide Injections in Primary Cutaneous Lymphoma Plaques With a Novel Needle-free Drug-delivery System. (NA)
• Erlotinib (Tarceva) and Bexarotene (Targretin) Oral Capsules in Advanced Cancers of the Aerodigestive Tract (PHASE1)
• Bexarotene in Preventing Breast Cancer in Patients at High Risk for Breast Cancer (PHASE1)
• High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia (NA)
• Study of Oral LBH589 in Adult Patients With Refractory Cutaneous T-Cell Lymphoma (PHASE2)
• A Phase 3 Trial of Brentuximab Vedotin(SGN-35) Versus Physician's Choice (Methotrexate or Bexarotene) in Participants With CD30-Positive Cutaneous T-Cell Lymphoma (ALCANZA Study) (PHASE3)

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Targretin CI brief — competitive landscape report
• Targretin updates RSS · CI watch RSS
• Bausch Health portfolio CI