Bexarotene

Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRß, 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).

• 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. TARGRETIN (bexarotene) is a retinoid indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.ICD-10: C85.90

• • Pregnancy (Boxed Warning, 4.1 ) • Known hypersensitivity to bexarotene ( 4.2 ) 4.1 Pregnancy TARGRETIN can cause fetal harm when administered to a pregnant female. TARGRETIN is a member of the retinoid class of drugs that is associated with birth defects in humans and is contraindicated in females who are pregnant.contraindicated

The recommended initial dose of TARGRETIN is 300 mg/m 2 /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 [ see Use in Specific Populations (8.1) ]. Table 1: TARGRETIN Initial Dose Calculation According to Body Surface Area Initial Dose Level (300 mg/m 2 /day) Number of 75 mg TARGRETIN Capsules Body Surface Area (m 2 ) Total Daily Dose (mg/day) 0.88 – 1.12 300 4 1.13 – 1.37 375 5 1.38 – 1.62 450 6 1.63 – 1.87 525 7 1.88 – 2.12 600 8 2.13 – 2.37 675 9 2.38 – 2.62 750 10 Dose Modification Guidelines: The 300 mg/m 2 /day dose level of TARGRETIN may be adjusted to 200 mg/m 2 /day then to 100 mg/m 2 /day, or temporarily suspended, if necessitated by toxicity. When toxicity is controlled, doses may be carefully readjusted upward. If there is no tumor response after 8 weeks of treatment and if the initial dose of 300 mg/m 2 /day is well tolerated, the dose may be escalated to 400 mg/m 2 /day with careful monitoring. Duration of Therapy: In clinical trials in CTCL, TARGRETIN was administered for up to 97 weeks. TARGRETIN should be continued as long as the patient is deriving benefit. • Recommended initial dose is 300 mg/m 2 /day. ( 2 ) • Take TARGRETIN as a single oral daily dose with a meal. ( 2 ) • Dose Adjustment: May be adjusted to 200 mg/m 2 /day then to 100 mg/m 2 /day. ( 2 )

• Hyperlipidemia: TARGRETIN causes elevations in blood lipids. Obtain baseline values, monitor, and manage elevations during therapy by dose reduction, interruption, discontinuation and/or lipid lowering therapy. ( 5.1 , 5.11 ) • Pancreatitis: Interrupt TARGRETIN and evaluate if suspected. ( 5.2 ) • Hepatotoxicity, Cholestasis, and Hepatic Failure: Interrupt or discontinue TARGRETIN and evaluate if liver chemistry tests exceed three times the upper limit of normal values. ( 5.3 ) • Hypothyroidism: TARGRETIN therapy can cause hypothyroidism. Monitor and replace thyroid hormone if needed. ( 5.5 ) • Neutropenia: Monitor for neutropenia. Reduce TARGRETIN dose or interrupt as indicated. ( 5.6 ) • Photosensitivity: Minimize exposure to sunlight and artificial ultraviolet light during treatment. ( 5.10 ) 5.1 Hyperlipidemia TARGRETIN induces substantial elevations in lipids in most patients. About 70% of patients with CTCL who received an initial dose of > 300 mg/m 2 /day of TARGRETIN had fasting triglyceride levels greater than 2.5 times the upper limit of normal. About 55% had values over 800 mg/dL with a median of about 1200 mg/dL in those patients. Cholesterol elevations above 300 mg/dL occurred in approximately 60% and 75% of patients with CTCL who received an initial dose of 300 mg/m 2 /day or greater than 300 mg/m 2 /day, respectively. Decreases in high density lipoprotein (HDL) cholesterol to less than 25 mg/dL were seen in about 55% and 90% of patients receiving an initial dose of 300 mg/m 2 /day or greater than 300 mg/m 2 /day, respectively, of TARGRETIN.

The following serious adverse reactions are discussed in greater detail in other sections of the prescribing information: • Hyperlipidemia [ see Warnings and Precautions (5.1) ] • Pancreatitis [ see Warnings and Precautions (5.2) ] • Hepatotoxicity, Cholestasis, and Hepatic Failure [ see Warnings and Precautions (5.3) ] • Hypothyroidism [ see Warnings and Precautions (5.4) ] • Neutropenia [ see Warnings and Precautions (5.5) ] • Cataracts [ see Warnings and Precautions (5.6) ] • Vitamin A Supplementation Hazard [ see Warnings and Precautions (5.7) ] • Hypoglycemia Risk in Patients with Diabetes Mellitus [ see Warnings and Precautions (5.8) ] • Photosensitivity [ see Warnings and Precautions (5.9) ] • Laboratory Tests [ see Warnings and Precautions (5.10) ] • Drug/Laboratory Test Interactions [ see Warnings and Precautions (5.11) ] The most common adverse reactions (greater than 10%) include: hyperlipidemia, hypercholesteremia, headache, hypothyroidism, asthenia, leukopenia, rash, nausea, infection, peripheral edema, abdominal pain, and dry skin. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bausch Health US, LLC at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

8.1 Pregnancy Risk Summary TARGRETIN, a retinoid, can cause fetal harm based on findings from animal studies when administered to a pregnant female and is contraindicated during pregnancy. Bexarotene was teratogenic and caused developmental mortality in rats following oral administration during organogenesis [see Data] . TARGRETIN must not be given to a pregnant female or a female who intends to become pregnant. If pregnancy does occur during treatment with TARGRETIN, immediately discontinue the drug and advise the pregnant female of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated populations is unknown. However, the background risk in the U.S. general population of major birth defects is 2-4% and of miscarriage is 15-20% of clinically recognized pregnancies. Data Animal Data Bexarotene caused malformations when administered orally to pregnant rats during days 7-17 of gestation. Developmental abnormalities included incomplete ossification at 4 mg/kg/day and cleft palate, depressed eye bulge/microphthalmia, and small ears at 16 mg/kg/day. The plasma AUC of bexarotene in rats at 4 mg/kg/day is approximately one third the AUC in humans at the recommended daily dose. At doses greater than 10 mg/kg/day, bexarotene caused developmental mortality.

Metabolism

Terminal half-life of bexarotene is approximately 7 hours. Studies in patients with advanced malignancies show approximate single dose linearity within the therapeutic range.

Doses up to 1000 mg/m 2 /day of TARGRETIN have been administered in short-term trials in patients with advanced cancer without acute toxic effects. Single doses of 1500 mg/kg and 720 mg/kg were tolerated without significant toxicity in rats and dogs, respectively. These doses are approximately 30 and 50 times, respectively, the recommended human dose on a mg/m 2 basis.

• Dec 29, 1999NDANDA021055Bausch
• Jun 28, 2000NDANDA021056Bausch
• Aug 12, 2014ANDAANDA203174Bionpharma
• May 8, 2018ANDAANDA209861Ani Pharms
• Jul 25, 2018ANDAANDA209886Upsher Smith Labs
• Sep 4, 2018ANDAANDA210105Amneal Pharms Ny
• Jan 14, 2021ANDAANDA209931Teva Pharms Usa
• Apr 27, 2022ANDAANDA215398Amneal

1. 1Drug Ineffective1068.2%
2. 2Hypothyroidism755.8%
3. 3Death745.7%
4. 4Off Label Use725.6%
5. 5Hypertriglyceridaemia594.6%
6. 6Disease Progression554.3%
7. 7Fatigue503.9%
8. 8Pruritus463.6%
9. 9Malignant Neoplasm Progression433.3%
10. 10Condition Aggravated382.9%
11. 11Nausea372.9%
12. 12Pneumonia342.6%
13. 13Mycosis Fungoides302.3%
14. 14Cutaneous T-cell Lymphoma272.1%
15. 15Product Use In Unapproved Indication272.1%

Recent PubMed references pinned to Bexarotene as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Positive net antiviral benefit of bexarotene against patient-derived archetype and rearranged BK polyomavirus isolates.
  Antiviral research · 2026 · Feld P, Lauterbach-Rivière L, Götz KM, et al.
  PMID 41864357DOI 10.1016/j.antiviral.2026.106398
• Brain Single-Cell Transcriptional Responses to Bexarotene-Activated RXR in an Alzheimer's Disease Model.
  International journal of molecular sciences · 2026 · Saibro-Girardi C, Lu Y, Fitz NF, et al.
  PMID 41828651DOI 10.3390/ijms27052435
• Potential effects of bexarotene on neural development and function in zebrafish embryos.
  Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2026 · Zha W, Wang M, Meng Y, et al.
  PMID 41579708DOI 10.1016/j.biopha.2026.119050
• Bexarotene signaling in human B and T lymphocytes induces gut-homing receptor expression.
  Frontiers in immunology · 2025 · Kaiser S, Suhrkamp I, He J, et al.
  PMID 41132678DOI 10.3389/fimmu.2025.1664199
• An Open-Label, Multicenter, Phase II Study of Bexarotene in Patients with Adult T-Cell Leukemia/Lymphoma.
  The Journal of dermatology · 2025 · Yonekura K, Muto I, Takenaka M, et al.
  PMID 40847644DOI 10.1111/1346-8138.17919
• A bexarotene-attached Re(I) tricarbonyl complex for NADH oxidation and ROS-mediated cancer phototherapy.
  Chemical communications (Cambridge, England) · 2025 · Kushwaha R, Singh V, Koch B, et al.
  PMID 40772411DOI 10.1039/d5cc03374h
• Serum neurofilament light chain levels suggest neuroprotection following bexarotene-induced remyelination in people with relapsing remitting multiple sclerosis.
  Multiple sclerosis and related disorders · 2025 · Riboni-Verri G, McMurran C, Kuhle J, et al.
  PMID 40749568DOI 10.1016/j.msard.2025.106655
• Comparative evaluation of the biological characteristics of a novel retinoid X receptor agonist and bexarotene.
  Molecular pharmacology · 2025 · Tomita K, Nakashima KI, Yamaguchi E, et al.
  PMID 40701035DOI 10.1016/j.molpha.2025.100057

The 10 most recently updated of 47 ClinicalTrials.gov registrations naming Bexarotene as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Phase I/II Study of Bexarotene in Combination With ZD1839 (IRESSA®) in the Treatment of Non-Small Cell Lung Cancer
  Completed · Phase 1 · Phase 2 · Interventional · 6 enrolled · Stanford University
  NCT00238628updated 2026-06-04
• A Study of Bexarotene Combined With Radiotherapy in People With Mycosis Fungoides
  Recruiting · Phase 1 · Interventional · 20 enrolled · Memorial Sloan Kettering Cancer Center
  NCT05296304updated 2026-02-04
• The Role of Bexarotene in Inducing Susceptibility to Chemotherapy in Metastatic TNBC
  Completed · Phase 1 · Interventional · 12 enrolled · National Cancer Centre, Singapore
  NCT04664829updated 2025-09-23
• Triamcinolone Acetonide Injections in Primary Cutaneous Lymphoma Plaques With a Novel Needle-free Drug-delivery System.
  Withdrawn · Interventional · 0 enrolled · Case Comprehensive Cancer Center
  NCT05106192updated 2025-06-12
• Erlotinib (Tarceva) and Bexarotene (Targretin) Oral Capsules in Advanced Cancers of the Aerodigestive Tract
  Completed · Phase 1 · Interventional · 24 enrolled · Dartmouth-Hitchcock Medical Center
  NCT01116622updated 2023-10-18
• Bexarotene in Preventing Breast Cancer in Patients at High Risk for Breast Cancer
  Completed · Phase 1 · Interventional · 24 enrolled · National Cancer Institute (NCI)
  NCT03323658updated 2023-01-10
• High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia
  Completed · Interventional · 34 enrolled · University of Washington
  NCT02551718updated 2022-06-30
• Study of Oral LBH589 in Adult Patients With Refractory Cutaneous T-Cell Lymphoma
  Completed · Phase 2 · Interventional · 139 enrolled · Novartis Pharmaceuticals
  NCT00425555updated 2021-08-20
• 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)
  Completed · Phase 3 · Interventional · 131 enrolled · Millennium Pharmaceuticals, Inc.
  NCT01578499updated 2021-01-05
• Phase II Study of Bexarotene in Patients With Acute Myeloid Leukemia
  Terminated · Phase 2 · Interventional · 24 enrolled · Abramson Cancer Center at Penn Medicine
  NCT00615784updated 2020-12-17

Frequently asked questions

How does Bexarotene work?

Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRß, 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).

What is Bexarotene used for?

According to FDA labeling, Bexarotene carries indications including: 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. TARGRETIN (bexarotene) is a retinoid indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bexarotene?

Bexarotene is classified as Retinoids for cancer treatment, Retinoid, Receptor Interactions, Unknown Cellular or Molecular Interaction, Cellular Growth Phase Arrest, Decreased Transcription to RNA.

What are the brand names for Bexarotene?

Bexarotene is marketed under brand names including Targretin.

What are the contraindications for Bexarotene?

Bexarotene labeling lists contraindications including: • Pregnancy (Boxed Warning, 4.1 ) • Known hypersensitivity to bexarotene ( 4.2 ) 4.1 Pregnancy TARGRETIN can cause fetal harm when administered to a pregnant female. TARGRETIN is a member of the retinoid class of drugs that is associated with birth defects in humans and is contraindicated in females who are pregnant.. Always consult the full prescribing information and a clinician.