Degarelix Dosage

Degarelix is ​​a decapeptide synthesized in the laboratory and is composed of seven unnatural amino acids. The peptide is linear in structure and antagonist of the natural GnRH hormone, so its main function is to block receptors in the anterior pituitary gland, thus reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This effect results in the suppression of testosterone secretion, which could potentially be used to treat certain conditions. The primary application of this peptide is based on the potential treatment of advanced prostate cancer in men. There are many different forms of this cancer at different ages, but most feed mainly on the male sex hormone testosterone, so suppressing it could resolve further tumor growth. Therefore, this form of hormone therapy in the right dose is mentioned as a possible solution.

Dosage Chart

Timeline	Week 1 – 4	Until the end of treatment
Advanced prostate cancer treatment protocol	240 mg (2 subcutaneous injections) 120 mg each at a concentration of 40 mg/mL.	80 mg (1 subcutaneous injection)   At a concentration of 20 mg/mL every 28 days.

About the Peptide

Gonadotropin-releasing hormone is a naturally occurring hormone that regulates the release of gonadotropins (the aforementioned FSH and LH). Degarelix is ​​an antagonist that competitively binds to receptors located primarily in the anterior pituitary gland, thus blocking or reducing further secretion of both hormones. This effect itself may have a potential therapeutic effect, however, in the case of Degarelix, there is a consequent suppression of testosterone (the male sex hormone) secretion.

Adenocarcinoma in stage III, advanced hormonal prostate cancer in adult patients, and high-risk localized cancer in combination with radiotherapy are just some forms of prostate cancer that can potentially be successfully treated with this peptide.

The reason for such widespread use lies in the fact that most cases of prostate cancer are fueled by testosterone. This means that high levels of this hormone result in an increase in tumor size, changes in histological characteristics, and, therefore, a worsening of the condition. By consequently reducing testosterone secretion, Degarelix eliminates the possibility of additional tumor growth, so in combination with additional therapies, significant improvement is possible. Numerous scientific studies have confirmed that there is no reason for limited use in older or younger populations (children), which means that this type of hormone therapy is equally effective at all ages. It is always administered in the recommended dose and always subcutaneously in the abdominal area.

List of Uses of This Peptide

Newly Diagnosed Advanced Prostate Cancer

The diagnosis of advanced prostate cancer indicates that the disease has spread to surrounding organs such as lymph nodes and bones. The prognosis is very poor in this case, and adequate therapies are required. The goal is to reduce testosterone levels because the tumor feeds with it, which is why the diagnosis states that it is a hormone-dependent tumor. All therapies that ultimately increase the hormone levels can worsen the condition. The mechanism of certain drugs works precisely by initially raising levels and then lowering them sharply and abruptly.

Genirelix does not have the effect of the initial surge in hormones, making it almost the first choice in the potential treatment of these diagnoses. Given these favorable effects, peptides like this are used even in cases of such a tumor that has already metastasized because they reduce its size and the tendency to spread further. This is the reason why this potential therapy should be started as early as possible so that the level of male sex hormones can be reduced immediately and deterioration can be avoided.

Various scientific studies have included cases of newly diagnosed cancer in patients who were at high risk of death. The results of all studies have shown that there is a significant improvement in the condition and shrinkage of the tumor, with a reduced tendency to spread further to surrounding organs. The effect of Degarelix on cardiovascular problems, especially in patients who are prone to similar problems such as myocardial infarction and atherosclerosis, is very uncertain. There is a chance that the drug is applicable in this case and can even reduce the chance of the occurrence of the aforementioned problems, but this is not official information.

Stage Three Prostate Adenocarcinoma

Adenocarcinoma is a form of cancer that develops in our glands and can be hormone-dependent. Since its name contains the word carcinoma, it is clearly a malignant epithelial tumor. Depending on the stage of this cancer, it can spread to other organs or remain in the form of primary cancer. Certain studies have investigated the effectiveness of Degarelix in the treatment of prostate adenocarcinoma in stage III. At this stage, the cancer is still localized exclusively in the prostate, but it has grown and threatens to spread to the lymph nodes, so effective therapy is necessary in this case. In such cases, androgen deprivation therapy is the most common choice, while neoadjuvant hormonal treatment has not yet become an everyday practice. After Degarelix therapy, patients had significantly lower cholesterol levels, as well as significantly lower tumor marker levels than at the beginning of hormone therapy. In addition to achieving excellent results in all patients with this form of cancer, this therapy also achieved advantages over other forms of treatment that were most widely used until then, which was shown in the results of various research that compared the effectiveness of different therapy options. The biggest reason for this is that GnRH antagonists such as Degarelix do not cause an initial jump in hormone levels but immediately work on its decline.

Efficacy of Degarelix in the Treatment of Localized Prostate Cancer

When a diagnosis of localized prostate cancer is made, it means that the tumor cells have not spread to surrounding organs, which means that it is a primary tumor and not a metastasis. However, such tumors also tend to spread, but at this level, the survival rate is higher, and effective treatment is indeed possible.

Various studies have confirmed the potential effectiveness of this peptide, as in the case of previously described cancers. So, in the case of localized form, the mechanism of action is the same and is reflected in the rapid and sudden decrease in testosterone secretion. The result of such therapy in most cases, as before, will be a reduced tumor, reduced tumor markers, and an improvement in the patient's general condition. Degarelix therapy could be combined with radiotherapy, which is sometimes applied before surgery to reduce the tumor size to surgical standards and sometimes after surgery to maintain the achieved results and prevent further spread. However, in this and other cases of cancer, certain accompanying symptoms occur, such as difficulty urinating, severe pain in the prostate area, burning sensation, and false urges to urinate. This occurs not only because of the tumor but also because of the generally increased size of the prostate in such diagnoses. Degarelix has a great advantage from this point of view compared to androgen deprivation therapy because it improves the aforementioned symptoms and makes life easier for patients. In addition, it does not cause complications such as spinal cord compression.

Dosage Calculator

The dosage of the peptide is very important because if the dose is exceeded, side effects may occur. The indications for the use of Degarelix are various forms of prostate cancer with associated urinary symptoms. The recommended dose in the first four weeks of treatment is 240 mg with two subcutaneous injections in the abdomen, each containing 120mg of a concentration of 40mg/mL. Then, until the end of treatment, a dose of 80mg is applied with one subcutaneous injection in the abdomen of a concentration of 20 mg/mL. This dosage method represents a maintenance dose and is applied every 28 days. Given that the drug is excreted through urine and stool, it can be found in these two body secretions, as well as in vomit. Therefore, hands should not come into contact with these secretions for 48 hours after taking the drug.

Conclusion

This decapeptide has shown great potential in the treatment of various forms of prostate cancer in children and adults, according to the results of various studies. Only some of the described forms are localized, newly discovered advanced carcinoma, and adenocarcinoma in the third stage. The use of this peptide as part of a single therapy or in combination with radiotherapy can improve in all criteria related to the tumor, but also to a recovery in the quality of life and a reduction in symptoms related to urination. It is essential to use it in the recommended dose, according to the indications, and with mandatory medical supervision. Degarelix will certainly be the subject of future research.

References:

1. Klotz, L., Boccon-Gibod, L., Shore, N. D., Andreou, C., Persson, B. E., & Jensen, J. K. (2008). The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer. The Journal of Urology, 180(3), 978–984. https://doi.org/10.1016/j.juro.2008.05.047
2. Crawford, E. D., Heidenreich, A., Shore, N. D., Tombal, B., & Klotz, L. (2015). An update on the role of GnRH antagonists in the treatment of prostate cancer. Therapeutic Advances in Urology, 7(1), 13–33. https://doi.org/10.1177/1756287214562062
3. Van Poppel, H., & Klotz, L. (2012). Gonadotropin-releasing hormone: an update review of the antagonists versus agonists. International Journal of Urology, 19(8), 594–601. https://doi.org/10.1111/j.1442-2042.2012.02997.x
4. Tombal, B., Shore, N. D., & Abrahamsson, P. A. (2010). Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor antagonist for the treatment of prostate cancer. Therapeutics and Clinical Risk Management, 6, 291–297. https://doi.org/10.2147/TCRM.S7730
5. Klotz, L. (2012). Degarelix: evolution of a gonadotropin-releasing hormone antagonist. Expert Opinion on Pharmacotherapy, 13(6), 875–884. https://doi.org/10.1517/14656566.2012.666891
6. Gittelman, M. C., Pommerville, P. J., Persson, B. E., & Jensen, J. K. (2010). A 1-year, open-label, randomized study of degarelix vs leuprolide in prostate cancer patients: comparison of urinary symptom relief. BJU International, 107(5), 760–767. https://doi.org/10.1111/j.1464-410X.2010.09864.x
7. Miller, K., Conners, W., & Ramsden, R. (2011). Degarelix: a gonadotropin-releasing hormone antagonist for the management of prostate cancer. Clinical Interventions in Aging, 6, 391–399. https://doi.org/10.2147/CIA.S22185
8. Schally, A. V., & Comaru-Schally, A. M. (2005). Hypothalamic hormones and cancer: new aspects of endocrine control of tumor growth. Archives of Medical Research, 36(5), 504–513. https://doi.org/10.1016/j.arcmed.2005.01.007
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   Disposition and metabolism of cetrorelix, a potent luteinizing hormone-releasing hormone antagonist, in rats and dogs
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