I have not heard of any progress on the GNRH antagonist program, but I do know that this is one of the former general research areas of interest of Andres Negro-Villar, both while he was at Southwestern working with McCann and while at NIEHS.
As to this program, the development of any drug here would have to compete with injectable compounds such as Leupride and others, perhaps Buserelin, both of which are long acting GNRH receptor agonists that are useful for steroid dependent prostate cancer, among other things. There is an interesting biology here (you could have predicted that I would say that). The chronic treatment with these superagonists downregulate the GNRH receptor, ultimately making it unresponsive to stimulation. There is certainly an inconvenience with an injectable, as for Leupride one has to get repeat injections every 30 or so days (my father is on this). An antagonist has a similar end effect. In the normal situation, GNRH is released from hypothalamic preoptic hypophysiotropic neurons in a pulsatile manner, not in a chronic manner, thus avoiding the desensitization.
If my memory serves me correctly, then the AMGN/Praecis program with abarelix is peptide in nature, no? |
