Gonadorelin (GnRH) is a decapeptide gonadotropin-releasing hormone agonist. It stimulates the synthesis and release of luteinizing hormone and follicle stimulating hormone. It is used in human medicine to treat infertility, menstrual cycle irregularities, and hypogonadism. It is also used as a diagnostic agent in assessing pituitary function. Ongoing research has found potential uses for gonadorelin in breast and prostate cancer treatment as well as Alzheimer’s disease.
Molecular Formula: C55H75N17O13
Molecular Weight: 1182.311 g/mol
PubChem CID: 638793
CAS Number: 9034-40-6
Synonyms: Growth Hormone Releasing Factor, Somatocrinin, Somatoliberin
Gonadorelin Peptide Research and Breast Cancer Prevention
Research suggests that having a higher life-time exposure to estrogen may increase a woman’s chance of developing breast cancer. Women who start their period at a younger age, go through menopause at a later age, take estrogen-containing birth control, or have menopausal hormone replacement therapy all have a higher risk of developing breast cancer. Thankfully, in the case of birth control, the risk diminishes when the pills are no longer taken and eventually the increased risk returns to baseline. Of course, birth control is a double-edged sword because even though its use increases risk of breast cancer, it decreases risk of ovarian cancer.
Some breast cancer cells require estrogen to grow and minimizing estrogen production or blocking estrogen receptors has long been an established method for treating certain forms of breast cancer. Research into gonadorelin shows that it can be used to suppress ovarian production of estrogen and that this may be a means of preventing breast cancer in the first place. This concept is based on the idea that some women, due to genetic and environmental factors, are at higher risk of developing breast cancer in their postmenopausal years. The use of gonadorelin in this setting is safe and cost-effective, making it an attractive means of reducing cancer burden. Research suggests that using gonadorelin for 10 years could reduce the risk of breast cancer by as much as 50% and that using it for 15 years could reduce risk by 70%.
The benefits of gonadorelin do not stop at breast cancer prevention, however, Research indicates that adjuvant therapy with anti-estrogens reduces disease progression by as much as 50% in cases where cancer is sensitive to estrogen. Unfortunately, currently available treatments are limited in their efficacy because cancer cells tend to develop resistance to them over time. This resistance usually arises as a result of increased estrogen receptor expression, making it impossible to block every estrogen receptor without severe side effects. Gonadorelin could circumvent this problem by reducing estrogen expression in the first place. This would not only directly reduce growth of estrogen-sensitive cancer, it would boost the efficacy of receptor blocking medications and extend their useful lifespan
Research in postmenopausal women with hyperandrogenism (too much estrogen) has revealed that long-term GnRH treatment reduces overall levels of estrogen and thus the risk of developing breast cancer. It does so without serious side effects and thus offers an alternative to the current therapy, which is surgical removal of the ovaries
Gonadorelin Peptide a Breakthrough in Prostate Cancer
Despite what we are led to believe by popular media, prostate cancer is actually the most hormone-sensitive of all cancers. This may seem problematic, but it actually represents an opportunity for intervention. In short, by cutting off the supply of testosterone and its derivatives to prostate cancer, it is possible to dramatically slow growth and even halt it altogether. The challenge, of course, is to cut off all hormone flow. This led initially to the surgical removal of the testicles in men with aggressive prostate cancer, a procedure that was quickly replaced by gonadorelin Peptide administration when it was found to be just as effective and, potentially, reversible.
The use of GnRH in men suffering from prostate cancer began as far back as 1979 and was referred to as medical castration. This mode of treatment eventually led to an interesting finding, however, which is that some androgens are made locally in the prostate via a mechanism called intracrinology. This, of course, means that GnRH blockade is only partially effective in treating prostate cancer. With the help of gonadorelin, scientists were able to develop two new drugs that have been accepted by the FDA for the treatment of castration-resistant prostate cancer (CRPC). These drugs are highly important and offer a new line of defense against prostate cancer progression and metastasis. They may even eventually find use as preventatives in older men.
The use of both gonadorelin and newer, localized drugs in the treatment of prostate cancer is referred to as combined androgen blockage (CAB). When combined with effective screening and early detection, CAB is one of the few therapies in the realm of oncology to offer a cure – not just remission, but a cure When used effectively and combined with early detection, CAB makes it possible to cure 99% of all prostate cancer.