Bexarotene: a promising anticancer agent

  title={Bexarotene: a promising anticancer agent},
  author={Li-yan Qu and Xiuwen Tang},
  journal={Cancer Chemotherapy and Pharmacology},
Retinoids are biologically active derivatives of vitamin A, which play essential roles in embryonic or adult cell behavior modulating cell proliferation, differentiation and apoptosis. The biologic effects of retinoids are mediated by two distinct families of intracellular receptors: retinoid acid receptors (RARs)-α, -β and -γ and retinoid X receptors (RXR)-α, -β and -γ. Bexarotene is a selective RXR agonist, which exerts its effects in blocking cell cycle progression, inducing apoptosis and… 

Retinoid pathway and cancer therapeutics.

Retinoids as Chemo-Preventive and Molecular-Targeted Anti-Cancer Therapies

Reinoid-based target discovery presents an important line of attack toward designing new, more effective strategies for treating other cancer types and how the retinoid pathway genotype affects the ability of retinoids agents to inhibit the growth of colorectal cancer cells is discussed.

Retinoid X receptor agonist LG100268 modulates the immune microenvironment in preclinical breast cancer models

Treatment with LG 268, a RXR agonist, can improve response to immune checkpoint blockade in HER2+ or triple-negative breast cancer, and data suggest that the use of LG268, the only rexinoid approved by the FDA for the treatment of refractory cutaneous T-cell lymphoma, can be improved.

Targeting truncated RXRα for cancer therapy.

It is discovered that overexpression of tRXRα can promote tumor growth by interacting with tumor necrosis factor-alpha-induced phosphoinositide 3-kinase and NF-κB signal transduction pathways and nonsteroidal anti-inflammatory drug Sulindac and analogs are identified as effective inhibitors of t rxRα activities via a unique binding mechanism.

Cancer Chemopreventive Retinoids: Validation and Analysis of in Vivo and in Vitro Bioassay Results

Test retinoids, were tested for their capacity to inhibit the clonal growth of a squamous carcinoma cell line (SCC-25), which were found to be 2 - 3 logs less sensitive for each tested retinoid than the corresponding activity against NHK cells.

Design, synthesis, and biological evaluation of indenoisoquinoline rexinoids with chemopreventive potential.

The design, synthesis, and biological evaluation of both acidic and nonacidic indenoisoquinolines as new RXR ligands are presented, establishing a structural foundation for the design of new and novel rexinoid cancer chemopreventive agents.

Bexarotene inhibits cell proliferation by inducing oxidative stress, DNA damage and apoptosis via PPARγ/ NF-κB signaling pathway in C6 glioma cells

Bexarotene treatment in C6 glioma cells could modulate apoptosis profile, DNA damage, ROS production, and reduction of TAS levels through inhibition of NF-κB by enhancing PPARγ expression.

Rexinoid inhibits Nrf2-mediated transcription through retinoid X receptor alpha.




Recent advances in the use of vitamin A (retinoids) in the prevention and treatment of cancer.

Retinoids in cancer chemoprevention

  • R. Lotan
  • Medicine, Biology
    FASEB journal : official publication of the Federation of American Societies for Experimental Biology
  • 1996
Retinoids are potentially useful agent for cancer chemoprevention and appear to be associated with the ability of retinoids to modulate the growth, differentiation, and apoptosis of normal, premalignant, and malignant cells in vitro and in vivo.

A new class of retinoids with selective inhibition of AP-1 inhibits proliferation

A new class of retinoids is described that selectively inhibits AP-1 activity but does not activate transcription, and could serve as candidates for new retinoid therapeutic agents with reduced side effects.

Emerging role of rexinoids in non-small cell lung cancer: focus on bexarotene.

Bexarotene in combination with chemotherapeutic agents has demonstrated an encouraging median survival for patients with advanced non-small cell lung cancer compared with historical results with combination chemotherapy alone.

A selective retinoid X receptor agonist bexarotene (LGD1069, Targretin) prevents and overcomes multidrug resistance in advanced prostate cancer

The results confirmed that a retinoid X receptor agonist bexarotene prevented and overcame acquired drug resistance in advanced breast cancer and non‐small cell lung cancer and in advanced prostate cancer.

Clinical trials with retinoids for breast cancer chemoprevention.

Fenretinide was not found to affect risk biomarkers significantly in early postmenopausal women on hormone replacement therapy, who are at increased risk of developing breast cancer, and this combination appears to be safe and well tolerated in high-risk women, especially when low-dose tamoxifen is employed.

The retinoid X receptor-selective retinoid, LGD1069, prevents the development of estrogen receptor-negative mammary tumors in transgenic mice.

The studies described here demonstrate that LGD1069 effectively suppresses ER-negative tumor development in mouse mammary tumor virus-erbB2 transgenic mice with minimal toxicity and suggest that receptor-selective retinoids are promising agents for the prevention of breast cancer and that they may be particularly useful in preventing ER- negative breast cancer.

Synergistic effect of a retinoid X receptor-selective ligand bexarotene (LGD1069, Targretin) and paclitaxel (Taxol) in mammary carcinoma

The results demonstrated the potential of using a RXR selective ligand in combination with chemotherapy for the treatment of breast cancer.

Effects of novel retinoid X receptor-selective ligands on myeloid leukemia differentiation and proliferation in vitro.

It is concluded that the RAR/RXR pathway is more important than RXR/R XR pathway for differentiation and proliferation of acute myeloid leukemic cells, and certain retinoid or combination of retinoids with both RAR and RXR specificities may synergistically enhance the differentiation activity of ATRA.