La gonadorelina (GNRH) è un agonista dell'ormone a rilascio di gonadotropina decapeptide. Stimola la sintesi e il rilascio dell'ormone luteinizzante e dell'ormone stimolante il follicolo. È usato nella medicina umana per trattare l'infertilità, le irregolarità del ciclo mestruale e l'ipogonadismo. Viene anche usato come agente diagnostico per valutare la funzione ipofisaria. Ricerche in corso hanno trovato potenziali usi per la gonadorelina nel trattamento del cancro al seno e alla prostata e nel morbo di Alzheimer.

Fonte:Pubch

Sequenza:Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly
Formula molecolare:C₅₅H₇₅N₁₇O₁₃
Peso molecolare:1182.311 g/mol
Pubchem cid: 638793
Numero CAS:9034-40-6
Sinonimi:Fattore di rilascio dell'ormone della crescita, somatocrinina, somatoliberina

Ricerca con gonadorelina e prevenzione del cancro al seno

La ricerca suggerisce che avere un'esposizione a vita più elevata agli estrogeni può aumentare la possibilità di una donna di sviluppare il cancro al seno. Le donne che iniziano il ciclo in giovane età, passano attraverso la menopausa in età avanzata, prendono il controllo delle nascite contenenti gli estrogeni o hanno la terapia ormonale sostitutiva della menopausa hanno tutte un rischio più elevato di sviluppare il cancro al seno. Per fortuna, nel caso del controllo delle nascite, il rischio diminuisce quando le pillole non vengono più assunte e alla fine l'aumento del rischio ritorna al basale. Naturalmente, il controllo delle nascite è una spada a doppio taglio perché anche se il suo uso aumenta il rischio di carcinoma mammario, riduce il rischio di carcinoma ovarico.

Alcune cellule di carcinoma mammario richiedono che gli estrogeni crescano e minimizzano la produzione di estrogeni o bloccano i recettori degli estrogeni è stato a lungo un metodo stabilito per il trattamento di alcune forme di carcinoma mammario. La ricerca sulla gonadorelina mostra che può essere utilizzato per sopprimere la produzione ovarica di estrogeni e che questo può essere un mezzo per prevenire il cancro al seno in primo luogo. Questo concetto si basa sull'idea che alcune donne, a causa di fattori genetici e ambientali, hanno un rischio maggiore di sviluppare il cancro al seno negli anni postmenopausa. L'uso della gonadorelina in questo contesto è sicuro ed economico, rendendolo un mezzo attraente per ridurre il carico del cancro^[1]. 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%^[2].

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^[3].

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^[4].

Gonadorelin 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 administration when it was found to be just as effective and, potentially, reversible^[5].

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^[6]. 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^[7].

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^[8]. When used effectively and combined with early detection, CAB makes it possible to cure 99% of all prostate cancer.

Gonadorelin May Reduce Dementia Risk

Research indicates that sex hormones, particularly leuteinizing hormone (LH), act on the brain in ways that are well outside the scope of sexual dimorphism or reproductive capacity. In fact, the associated rise in LH that occurs with menopause has been correlated with an increased incidence of Alzheimer’s disease and decreased memory performance in both humans and animals. Careful research in rats further reveals that LH acts directly on the hippocampus, the primary memory center in the brain. Rats given LH exhibit decreased memory performance and hippocampus dysfunction, a deficit that is reverse by administration of an LH blocking drug^[9].

Further research on LH has revealed that higher levels of the hormone are associated with increased neuropathology. In particular, it has been revealed that LH promotes the development of plaques associated with Alzheimer’s^[10]. It stands to reason then that reducing LH levels may help to reduce the progression of Alzheimer’s disease. This has been born out, at least partially, in mouse models showing that getting rid of the LH receptor in the brain improves amyloid pathology and helps to preserve the health of cells like astrocytes, which support and protect neurons^[11].

As it turns out, testosterone is beneficial to brain health and actually helps to preserve cognitive function. Thus, simply blocking the entire hypothalamic-pituitary-gondal axis is not necessarily an effective means of treating Alzheimer’s disease. That is why scientists have set out to test gonadorelin derivatives to discern if selective interference in LH production is possible and can have potential benefits. This research, while ongoing, has led to the understanding that leuprolide (a common medication used to treat uterine fibroids and a GnRH receptor agonist) is effective in decreasing the risk of Alzhimer’s compared to other gonadorelin analogues^[12]. Ongoing research can help to define why this is the case, but it is important to note that men looking to use highly effective CAB treatment against prostate cancer need not choose between cancer and Alzheimer’s disease. Leuprolide can be used in this setting to offset the risks of CAB with regard to Alzheimer’s disease. In particular, the ability of leuprolide to down-regulate levels of serum gonadotrophins (LH in particular) is generally enough to offset the effects of reduced testosterone^[13].

New research is seeking to understand how gonadorelin and its analogues affect APOE and MS4A6A expression in Alzheimer’s disease. Both genetic loci are associated with late-onset Alzheimer’s disease, but research suggests that they need to operate in tandem to produce serious problems and that interfering with one gene loci or the other is enough to short-circuit the pathway to pathology. Gonadorelin affects this process of tandem interaction, but it isn’t clear how or why^[14]. Right now, researchers are working to understand how the interaction of genes in Alzheimer’s disease can be interrupted to both treat and prevent the condition. Gonadorelin is am important peptide in that research.

Gonadorelin is hardly a new peptide in the treatment of human and mammalian disease, but researchers are constantly uncovering new ways in which GnRH and GnRH analogues operate in both normal physiology as well as the development of disease. The discovery that gonadorelin can play a role in treating prostate cancer was a breakthrough that has allowed doctors to develop a cure so effective that fully 99% of people with prostate cancer can be cured if the disease is caught early enough. It looks like similar breakthroughs are on the horizon with the finding the gonadorelin and its down-stream hormones are substantial players in the pathways that lead to Alzheimer’s disease risk.

Gonadorelin exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. Gonadorelin for sale at

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

Dr. Giorgio Secreto currently studies at the IRCCS National Cancer Institute in Italy. His accolades include, a 1963 High School degree, Maturità Classica 1969 Degree in Medicine and Surgery, University of Milan, Italy 1974 Degree Specialist in Endocrinology, University of Turin, Italy. Doctor Secreto has been working at the National Cancer Institute of Milan since 1970 up to now, after his retirement in December 2010. The role of androgens in breast cancer is his main field of study. He has been teacher at the Italian School of Senology (1989-1996), Associate Professor in Oncology, L.U.de.S. University, Lugano, Switzerland (1999-2008), and Associate Professor in Endocrinology, Nurses’ School, University of Milan (2003-2008). He is active member of the New York Academy of Sciences and the American Association for the Advancement of Sciences. He published about 100 papers, including a few that pertain to GnRH’s effects on the reduction of breast cancer via minimizing excessive androgens.

Dr. Giorgio Secreto is being referenced as one of the leading scientists involved in the research and development of Gonadorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between

1. G. Secreto et al., “A novel approach to breast cancer prevention: reducing excessive ovarian androgen production in elderly women,” Breast Cancer Res. Treat., vol. 158, no. 3, pp. 553–561, 2016.
2. D. V. Spicer and M. C. Pike, “Sex steroids and breast cancer prevention,” J. Natl. Cancer Inst. Monogr., no. 16, pp. 139–147, 1994.
3. G. Secreto, P. Muti, M. Sant, E. Meneghini, and V. Krogh, “Medical ovariectomy in menopausal breast cancer patients with high testosterone levels: a further step toward tailored therapy,” Endocr. Relat. Cancer, vol. 24, no. 11, pp. C21–C29, 2017.
4. E. S. Vollaard, A. P. van Beek, F. A. J. Verburg, A. Roos, and J. A. Land, “Gonadotropin-releasing hormone agonist treatment in postmenopausal women with hyperandrogenism of ovarian origin,” J. Clin. Endocrinol. Metab., vol. 96, no. 5, pp. 1197–1201, May 2011.
5. F. Labrie, “Hormonal therapy of prostate cancer,” Prog. Brain Res., vol. 182, pp. 321–341, 2010.
6. F. Labrie, “GnRH agonists and the rapidly increasing use of combined androgen blockade in prostate cancer,” Endocr. Relat. Cancer, vol. 21, no. 4, pp. R301-317, Aug. 2014.
7. F. Labrie, “Combined blockade of testicular and locally made androgens in prostate cancer: a highly significant medical progress based upon intracrinology,” J. Steroid Biochem. Mol. Biol., vol. 145, pp. 144–156, Jan. 2015.
8. F. Labrie, “[Keyrole of endocrinology in the victory against prostate cancer],” Bull. Cancer (Paris), vol. 93, no. 9, pp. 949–958, Sep. 2006.
9. V. Burnham, C. Sundby, A. Laman-Maharg, and J. Thornton, “Luteinizing hormone acts at the hippocampus to dampen spatial memory,” Horm. Behav., vol. 89, pp. 55–63, 2017.
10. C. V. Rao, “Involvement of Luteinizing Hormone in Alzheimer Disease Development in Elderly Women,” Reprod. Sci. Thousand Oaks Calif, vol. 24, no. 3, pp. 355–368, 2017.
11. J. Lin et al., “Genetic ablation of luteinizing hormone receptor improves the amyloid pathology in a mouse model of Alzheimer disease,” J. Neuropathol. Exp. Neurol., vol. 69, no. 3, pp. 253–261, Mar. 2010.
12. R. L. Bowen, T. Butler, and C. S. Atwood, “Not All Androgen Deprivation Therapies Are Created Equal: Leuprolide and the Decreased Risk of Developing Alzheimer’s Disease,” J. Clin. Oncol., vol. 34, no. 23, p. 2800, Aug. 2016.
13. M. A. Smith, R. L. Bowen, R. Q. Nguyen, G. Perry, C. S. Atwood, and A. A. Rimm, “Putative Gonadotropin-Releasing Hormone Agonist Therapy and Dementia: An Application of Medicare Hospitalization Claims Data,” J. Alzheimers Dis. JAD, vol. 63, no. 4, pp. 1269–1277, 2018.
14. A. Cáceres, J. E. Vargas, and J. R. González, “APOE and MS4A6A interact with GnRH signaling in Alzheimer’s disease: Enrichment of epistatic effects,” Alzheimers Dement. J. Alzheimers Assoc., vol. 13, no. 4, pp. 493–497, Apr. 2017.

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