TARGRETIN (bexarotene)
TARGRETIN is indicated for the treatment of Cutaneous T-Cell Lymphoma.
How TARGRETIN Works
Bexarotene selectively binds and activates retinoid X receptor (RXR) subtypes (α, β, γ). Once activated, these receptors heterodimerize with various partners—including retinoic acid receptors (RARs), vitamin D receptors, and thyroid receptors—to function as transcription factors that regulate genes controlling cellular differentiation and proliferation. While bexarotene has demonstrated the ability to inhibit tumor cell growth in vitro and induce regression in vivo, its exact mechanism of action in treating CTCL is not fully elucidated.
Development Insights
Details
- Status
- Prescription
- First Approved
- 1999-12-29
- Routes
- TOPICAL, ORAL
- Dosage Forms
- GEL, CAPSULE
TARGRETIN Approval History
What TARGRETIN Treats
1 indicationsTARGRETIN is approved for 1 conditions since its original approval in 1999. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Cutaneous T-Cell Lymphoma
TARGRETIN Boxed 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...
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 )
TARGRETIN Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in TARGRETIN's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications TARGRETIN treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to TARGRETIN
3 of 9FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
11 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT05296304 | 21-501 | Ph 1 | recruiting | A Study of Bexarotene Combined With Radiotherapy in People With Mycosis Fungoides |
| NCT04664829 | BEXMET | Ph 1 | completed | The Role of Bexarotene in Inducing Susceptibility to Chemotherapy in Metastatic TNBC |
| NCT03323658 results posted | NCI-2017-01960 NCI-2017-01960, N01-CN-2012-00034 | Ph 1 | completed | Bexarotene in Preventing Breast Cancer in Patients at High Risk for Breast Cancer |
| NCT01578499 ALCANZA results posted | C25001 2010-024215-14 | Ph 3 | completed | 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) |
| NCT00615784 UPCC04407 results posted | UPCC 04407 UPCC 04407 | Ph 2 | terminated | Phase II Study of Bexarotene in Patients With Acute Myeloid Leukemia |
| NCT01007448 results posted | E7273-G000-401 | Ph 4 | completed | Study Evaluating Two Dose Levels of Targretin Capsules in Participants With Refractory Cutaneous T-Cell Lymphoma (CTCL) |
| NCT01782742 BEAT-AD results posted | CCF-IRB 12-783 | Ph 2 | completed | Bexarotene Amyloid Treatment for Alzheimer's Disease |
| NCT02061878 | REXCEPTOR-101 | Ph 1 | completed | A Study to Evaluate the Effect of Bexarotene on Beta-Amyloid and Apolipoprotein E Metabolism in Healthy Subjects |
| NCT00660231 GemBex | UCL/06/009 CRUK-UCL-GEMBEX, EU-20841 | Ph 2 | completed | Gemcitabine and Bexarotene in Treating Patients With Progressive or Refractory Stage IB, Stage II, Stage III, or Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma |
| NCT01001143 AML | 09-1661 / 201012801 | Ph 1 | completed | Intravenous (IV) Decitabine and Oral Bexarotene for Acute Myelogenous Leukemia (AML) |
| NCT00535574 | LRM250850 | Ph 3 | completed | Bexarotene Augmentation of Antipsychotic Treatment for Chronic Schizophrenia |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TARGRETIN FDA Label Details
Indications & Usage
FDA Label (PDF)TARGRETIN is indicated for the treatment of Cutaneous T-Cell Lymphoma.
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...
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment