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Chemical Compound Review

Targret     4-[1-(3,5,5,8,8-pentamethyl- 6,7...

Synonyms: Targretin, Targretyn, Targrexin, Bexarotene, bexaroteno, ...
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Disease relevance of LGD 1069


High impact information on LGD 1069

  • Our results demonstrate that the combination of denileukin diftitox and bexarotene is well tolerated and that even low doses (150 mg/day) of bexarotene are capable of in vivo upregulation of CD25 expression on circulating leukemia cells [5].
  • In vitro studies demonstrated that the retinoid X receptor (RXR) retinoid, bexarotene, at biologically relevant concentrations of 10(-6) M to 10(-8) M, upregulated both the p55 and p75 subunits of the IL-2R and enhanced 5- to 10-fold the susceptibility of T-cell leukemia cells to denileukin diftitox [5].
  • To determine whether this biomodulatory effect could be recapitulated in vivo, we treated 14 patients with relapsed or refractory cutaneous T-cell lymphoma with escalating doses of bexarotene (75 mg/day-300 mg/day) and denileukin diftitox (18 mcg/kg per day x 3 days every 21 days) in a phase 1 trial [5].
  • In addition to tumor multiplicity, proliferation and apoptosis were modulated by bexarotene treatment independently of estrogen signaling [6].
  • The rexinoids LG100268 and bexarotene (LG1069, Targretin) were highly efficacious in the prevention of neu-induced mammary carcinomas [6].

Chemical compound and disease context of LGD 1069


Biological context of LGD 1069


Anatomical context of LGD 1069


Associations of LGD 1069 with other chemical compounds

  • CONCLUSION: In patients with advanced NSCLC, bexarotene with cisplatin and vinorelbine yielded acceptable phase II response rates (25%) and was associated with better-than-expected survival (14-month median survival time; 61% 1-year, 32% 2-year, and 30% projected 3-year survival rates) [4].
  • RESULTS: Combining erlotinib with bexarotene enhanced growth suppression in vitro compared with each single-agent treatment [19].
  • For example, isotretinoin, followed by TSEB (for stage I to II disease) or preceded by chemotherapy (for stage II and IV disease) and bexarotene plus PUVA or photopheresis plus IFN, gave overall response rates of 82% and 69% in patients who had MF and SS, respectively [20].
  • In January 2000, Alfa Wassermann signed an agreement with Ligand to exclusively market and distribute Targretin gel and capsules in Italy [21].
  • These observations suggest that bexarotene probably has two fundamental effects on thyroid function: to suppress TSH production and to increase thyroid hormone metabolic clearance [22].

Gene context of LGD 1069


Analytical, diagnostic and therapeutic context of LGD 1069

  • The degree of suppression of thyrotropin secretion tended to be greater in patients treated with higher doses of bexarotene (>300 mg per square meter of body-surface area per day) and in those with a history of treatment with interferon alfa [1].
  • CONCLUSION: Bexarotene can be safely added to platinum-based chemotherapy provided that there is aggressive prophylaxis of hypertriglyceridemia [23].
  • Chemoprevention of mammary carcinoma by LGD1069 (Targretin): an RXR-selective ligand [24].
  • Identification of biomarkers modulated by the rexinoid LGD1069 (bexarotene) in human breast cells using oligonucleotide arrays [25].
  • In vivo, the bexarotene/paclitaxel combination regimen produced a statistically significant decrease in tumor growth in a Calu3 NSCLC xenograft model compared with the single agents (two-tailed, P < 0.05) [12].


  1. Central hypothyroidism associated with retinoid X receptor-selective ligands. Sherman, S.I., Gopal, J., Haugen, B.R., Chiu, A.C., Whaley, K., Nowlakha, P., Duvic, M. N. Engl. J. Med. (1999) [Pubmed]
  2. Retinoids increase human apolipoprotein A-11 expression through activation of the retinoid X receptor but not the retinoic acid receptor. Vu-Dac, N., Schoonjans, K., Kosykh, V., Dallongeville, J., Heyman, R.A., Staels, B., Auwerx, J. Mol. Cell. Biol. (1996) [Pubmed]
  3. Immunomodulatory effects of RXR rexinoids: modulation of high-affinity IL-2R expression enhances susceptibility to denileukin diftitox. Gorgun, G., Foss, F. Blood (2002) [Pubmed]
  4. Multi-institutional phase I/II trial of oral bexarotene in combination with cisplatin and vinorelbine in previously untreated patients with advanced non-small-cell lung cancer. Khuri, F.R., Rigas, J.R., Figlin, R.A., Gralla, R.J., Shin, D.M., Munden, R., Fox, N., Huyghe, M.R., Kean, Y., Reich, S.D., Hong, W.K. J. Clin. Oncol. (2001) [Pubmed]
  5. A phase-1 trial of bexarotene and denileukin diftitox in patients with relapsed or refractory cutaneous T-cell lymphoma. Foss, F., Demierre, M.F., DiVenuti, G. Blood (2005) [Pubmed]
  6. Neu-induced retroviral rat mammary carcinogenesis: a novel chemoprevention model for both hormonally responsive and nonresponsive mammary carcinomas. Woditschka, S., Haag, J.D., Waller, J.L., Monson, D.M., Hitt, A.A., Brose, H.L., Hu, R., Zheng, Y., Watson, P.A., Kim, K., Lindstrom, M.J., Mau, B., Steele, V.E., Lubet, R.A., Gould, M.N. Cancer Res. (2006) [Pubmed]
  7. Abrogation of transforming growth factor-alpha/epidermal growth factor receptor autocrine signaling by an RXR-selective retinoid (LGD1069, Targretin) in head and neck cancer cell lines. Song, J.I., Lango, M.N., Hwang, J.D., Drenning, S.D., Zeng, Q., Lamph, W.W., Grandis, J.R. Cancer Res. (2001) [Pubmed]
  8. Novel treatment of chronic severe hand dermatitis with bexarotene gel. Hanifin, J.M., Stevens, V., Sheth, P., Breneman, D. Br. J. Dermatol. (2004) [Pubmed]
  9. Differentiation and growth inhibition mediated via the RXR:PPARgamma heterodimer in colon cancer. Cesario, R.M., Stone, J., Yen, W.C., Bissonnette, R.P., Lamph, W.W. Cancer Lett. (2006) [Pubmed]
  10. Bexarotene: a clinical review. Farol, L.T., Hymes, K.B. Expert review of anticancer therapy. (2004) [Pubmed]
  11. Prevention of lung cancer progression by bexarotene in mouse models. Wang, Y., Zhang, Z., Yao, R., Jia, D., Wang, D., Lubet, R.A., You, M. Oncogene (2006) [Pubmed]
  12. A selective retinoid X receptor agonist bexarotene (Targretin) prevents and overcomes acquired paclitaxel (Taxol) resistance in human non-small cell lung cancer. Yen, W.C., Corpuz, M.R., Prudente, R.Y., Cooke, T.A., Bissonnette, R.P., Negro-Vilar, A., Lamph, W.W. Clin. Cancer Res. (2004) [Pubmed]
  13. RXR agonists activate PPARalpha-inducible genes, lower triglycerides, and raise HDL levels in vivo. Mukherjee, R., Strasser, J., Jow, L., Hoener, P., Paterniti, J.R., Heyman, R.A. Arterioscler. Thromb. Vasc. Biol. (1998) [Pubmed]
  14. Prevention of mouse lung tumors by targretin. Pereira, M.A., Kramer, P.M., Nines, R., Liu, Y., Alyaqoub, F.S., Gunning, W.T., Steele, V.E., Lubet, R.A. Int. J. Cancer (2006) [Pubmed]
  15. A selective retinoid X receptor agonist bexarotene (LGD1069, targretin) inhibits angiogenesis and metastasis in solid tumours. Yen, W.C., Prudente, R.Y., Corpuz, M.R., Negro-Vilar, A., Lamph, W.W. Br. J. Cancer (2006) [Pubmed]
  16. Synergistic effect of a retinoid X receptor-selective ligand bexarotene (LGD1069, Targretin) and paclitaxel (Taxol) in mammary carcinoma. Yen, W.C., Prudente, R.Y., Lamph, W.W. Breast Cancer Res. Treat. (2004) [Pubmed]
  17. A multiparameter flow cytometric analysis of the effect of bexarotene on the epidermis of the psoriatic lesion. Franssen, M.E., Smit, J.V., Van Erp, P.E., Van De Kerkhof, P.C. Br. J. Dermatol. (2003) [Pubmed]
  18. Biological effects of bexarotene in cutaneous T-cell lymphoma. Budgin, J.B., Richardson, S.K., Newton, S.B., Wysocka, M., Zaki, M.H., Benoit, B., Rook, A.H. Archives of dermatology. (2005) [Pubmed]
  19. Bexarotene and erlotinib for aerodigestive tract cancer. Dragnev, K.H., Petty, W.J., Shah, S., Biddle, A., Desai, N.B., Memoli, V., Rigas, J.R., Dmitrovsky, E. J. Clin. Oncol. (2005) [Pubmed]
  20. Topical and systemic retinoid therapy for cutaneous T-cell lymphoma. Kempf, W., Kettelhack, N., Duvic, M., Burg, G. Hematol. Oncol. Clin. North Am. (2003) [Pubmed]
  21. Bexarotene ligand pharmaceuticals. Hurst, R.E. Current opinion in investigational drugs (London, England : 2000) (2000) [Pubmed]
  22. Etiology, diagnosis, and treatment recommendations for central hypothyroidism associated with bexarotene therapy for cutaneous T-cell lymphoma. Sherman, S.I. Clinical lymphoma. (2003) [Pubmed]
  23. Phase II trial of the novel retinoid, bexarotene, and gemcitabine plus carboplatin in advanced non-small-cell lung cancer. Edelman, M.J., Smith, R., Hausner, P., Doyle, L.A., Kalra, K., Kendall, J., Bedor, M., Bisaccia, S. J. Clin. Oncol. (2005) [Pubmed]
  24. Chemoprevention of mammary carcinoma by LGD1069 (Targretin): an RXR-selective ligand. Gottardis, M.M., Bischoff, E.D., Shirley, M.A., Wagoner, M.A., Lamph, W.W., Heyman, R.A. Cancer Res. (1996) [Pubmed]
  25. Identification of biomarkers modulated by the rexinoid LGD1069 (bexarotene) in human breast cells using oligonucleotide arrays. Kim, H.T., Kong, G., Denardo, D., Li, Y., Uray, I., Pal, S., Mohsin, S., Hilsenbeck, S.G., Bissonnette, R., Lamph, W.W., Johnson, K., Brown, P.H. Cancer Res. (2006) [Pubmed]
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