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Biotech / Medical : Ligand (LGND) Breakout! -- Ignore unavailable to you. Want to Upgrade?

To: Koerte Andreas who wrote (28531)	3/16/1999 2:16:00 AM
From: Cheryl Galt	Respond to of 32384

>> I couldn't find anything about mechanism of action of Targretin in Breast Cancer. The only thing I found was that Targretin activates RXRs leading cells into apoptosis. Could anybody comment on advantages of the treatment or give references for reviews? << The 12/23/98 announcement of the Ph II trial for Advanced Breast Cancer businesswire.com includes a section " Preclinical Studies with Targretin And Breast Cancer Tumors," that discusses Targretin's effectiveness in tumor regression, and in preventing preventing the emergence of breast cancer tumors in the animal model. It does NOT discuss mechanism of action, but adds: "Ligand scientists have previously reported that Targretin does not alter estrogen, progesterone, or prolactin levels in this scientific model, and that Targretin can inhibit the undesirable side effects of uterine growth stimulation by both estrogen and tamoxifen." ------------------------------- The March 20, 1997 press release Ligand Starts Phase II Targretin (LGD1069) Trial In Diabetic Patients in Europe prnewswire.com includes this section: Targretin Mechanism of Action Targretin, a small organic compound discovered by Ligand scientists, selectively activates a subclass of retinoid receptors called retinoid X receptors (RXRs). RXR receptors play an important role in regulating cellular activities, including the enhancement of insulin action and lipid metabolism. When the RXR receptor is paired to another unique cell receptor, peroxisome proliferator activated receptor (PPAR) gamma, which is known to be a target for antidiabetic therapies, activation of the pair causes increased insulin sensitivity which impacts glucose metabolism and creates an anti-diabetic effect. Since Targretin binds to the RXR receptor, which is part of the paired heterodimer RXR/PPAR complex, it, too, influences the way the body uses insulin, glucose and lipids. In addition to affecting glucose and lipid metabolism, RXRs also play an important role in other cellular activities, such as programmed cell death or "apoptosis," a natural process by which the body eliminates unwanted cells. This unique activity may be involved in the actions of Targretin as an anti-cancer agent. ---------------------------------------------------------------------- Henry or others, is there anything in addition to apoptosis that relates to Targretin's anti-tumor activity?