New Drug for Refractory Cutaneous T-Cell Lymphoma

In vitro anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells

“…LGD1069, a selective retinoid X receptor agonist, is used in patients for cutaneous T-cell lymphoma [7], and is also demonstrated that it is an efficacious chemopreventive and chemotherapeutic agent in a number of preclinical rodent models breast cancer [7,16-18]. Furthermore, LGD1069 was shown recently to prevent tumor-induced angiogenesis and metastasis.…”

“…LGD1069 (Targretin) is a selective retinoid X receptor (RXR) ligand, termed rexinoid [6], which is used in patients for cutaneous T-cell lymphoma [7]. Several observations demonstrated that LGD1069 prevented and overcome acquired drug resistance in advanced breast cancer [8] and non-small cell lung cancer [9], and also in advanced prostate cancer [10].…”

In vitro anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells

“…LGD1069, a selective retinoid X receptor agonist, is used in patients for cutaneous T-cell lymphoma [7], and is also demonstrated that it is an efficacious chemopreventive and chemotherapeutic agent in a number of preclinical rodent models breast cancer [7,16-18]. Furthermore, LGD1069 was shown recently to prevent tumor-induced angiogenesis and metastasis.…”

“…LGD1069 (Targretin) is a selective retinoid X receptor (RXR) ligand, termed rexinoid [6], which is used in patients for cutaneous T-cell lymphoma [7]. Several observations demonstrated that LGD1069 prevented and overcome acquired drug resistance in advanced breast cancer [8] and non-small cell lung cancer [9], and also in advanced prostate cancer [10].…”

Highly Potent Naphthofuran‐Based Retinoic Acid Receptor Agonists

“…[7] Similarly, RXR ligands (rexinoids) expand the therapeutic potential of retinoids to metabolic diseases, as several of the nuclear receptors (NRs) such as RARs, VDR, PPARs, and LXR form functional RXR-NR heterodimers. [8] A synthetic RXR agonist, LGD1069 (bexarotene, Targretin), has been marketed for the treatment of cutaneous T-cell lymphoma [9] and holds promise for other indications as well. [10] One of the major concerns in retinoid research over the years has been the instability of the native ligand 1, given the sensitivity of its polyene chain to light, heat, and common reaction conditions.…”

In vitro anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells

“…LGD1069, a selective retinoid X receptor agonist, is used in patients for cutaneous T-cell lymphoma [7], and is also demonstrated that it is an efficacious chemopreventive and chemotherapeutic agent in a number of preclinical rodent models breast cancer [7,16-18]. Furthermore, LGD1069 was shown recently to prevent tumor-induced angiogenesis and metastasis.…”

“…LGD1069 (Targretin) is a selective retinoid X receptor (RXR) ligand, termed rexinoid [6], which is used in patients for cutaneous T-cell lymphoma [7]. Several observations demonstrated that LGD1069 prevented and overcome acquired drug resistance in advanced breast cancer [8] and non-small cell lung cancer [9], and also in advanced prostate cancer [10].…”

Highly Potent Naphthofuran‐Based Retinoic Acid Receptor Agonists

“…[7] Similarly, RXR ligands (rexinoids) expand the therapeutic potential of retinoids to metabolic diseases, as several of the nuclear receptors (NRs) such as RARs, VDR, PPARs, and LXR form functional RXR-NR heterodimers. [8] A synthetic RXR agonist, LGD1069 (bexarotene, Targretin), has been marketed for the treatment of cutaneous T-cell lymphoma [9] and holds promise for other indications as well. [10] One of the major concerns in retinoid research over the years has been the instability of the native ligand 1, given the sensitivity of its polyene chain to light, heat, and common reaction conditions.…”

In vitro anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells

“…LGD1069, a selective retinoid X receptor agonist, is used in patients for cutaneous T-cell lymphoma [7], and is also demonstrated that it is an efficacious chemopreventive and chemotherapeutic agent in a number of preclinical rodent models breast cancer [7,16-18]. Furthermore, LGD1069 was shown recently to prevent tumor-induced angiogenesis and metastasis.…”

“…LGD1069 (Targretin) is a selective retinoid X receptor (RXR) ligand, termed rexinoid [6], which is used in patients for cutaneous T-cell lymphoma [7]. Several observations demonstrated that LGD1069 prevented and overcome acquired drug resistance in advanced breast cancer [8] and non-small cell lung cancer [9], and also in advanced prostate cancer [10].…”

Highly Potent Naphthofuran‐Based Retinoic Acid Receptor Agonists

“…[7] Similarly, RXR ligands (rexinoids) expand the therapeutic potential of retinoids to metabolic diseases, as several of the nuclear receptors (NRs) such as RARs, VDR, PPARs, and LXR form functional RXR-NR heterodimers. [8] A synthetic RXR agonist, LGD1069 (bexarotene, Targretin), has been marketed for the treatment of cutaneous T-cell lymphoma [9] and holds promise for other indications as well. [10] One of the major concerns in retinoid research over the years has been the instability of the native ligand 1, given the sensitivity of its polyene chain to light, heat, and common reaction conditions.…”