Hormone sensitive cancers such as prostate and breast cancers can require
testosterone or estrogen for survival. Luteinizing
hormone-releasing hormone analogue therapy is one of the most widely
used hormonal therapies for advanced prostate cancer. Today's standard
of drug therapy involves repeated injections. As such, surgical sterilization
of either men or women is an important procedure in the treatment of
human prostate or breast cancer. A single injection drug derived from
Gonex's platform technology has the potential to replace monthly or quarterly
depot administration of Lupron®, Zoladex® or similar compounds. A single
injection of GnRH-conjugates can be used to replace surgical sterilization
of men and women. In addition, ongoing research is suggestive that Gonex's single injection drug
may be have a toxic effect on cancer cells that aberrantly express GnRH receptors.
The Technology Platform
Gonadotropin-releasing hormone (GnRH) is secreted by the brain. GnRH
binds to specific receptors on cells (gonadotropes) in the pituitary
gland and stimulates synthesis and secretion of two other hormones (LH
and FSH), that in turn control the production of hormone secretion by
the testes or ovaries. By linking GnRH to any of a number of protein
synthesis inhibitors, it is possible to target and destroy the gonadotrope
cells. This occurs when the gonadotropes internalize the GnRH conjugate
as part of the normal process of receptor de-activation. When the number
of gonadotrope cells is adequately reduced, there will be inadequate
levels of LH or FSH produced to stimulate the gonads, and the typical
production of testosterone or estrogen will cease. Without these hormones,
hormone sensitive cancers slow or stop their growth.
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