Molecular Formula | C82H103ClN18O16 |
Molar Mass | 1632.26 |
Density | 1.325±0.06 g/cm3(Predicted) |
pKa | 10.38±0.40(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
In vitro study | Degarelix acts directly on the pituitary receptors for luteinizing hormone-releasing hormone (LHRH), blocking the action of endogenous LHRH. The use of degarelix eliminates the initial undesirable surge in gonadotropin and testosterone levels, which is produced by agonists of LHRH. Degarelix treatment reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells), with the exception of the PC-3 cells. The GnRH antagonist degarelix exerts a direct effect on prostate cell growth through apoptosis. |
In vivo study | At single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. Duration of LH suppression increases with the dose: in the rat, significant suppression of LH lasted 1, 2, and 7 days after a single subcutaneous injection of degarelix at 12.5, 50, or 200 μg/kg, respectively. Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.613 ml | 3.063 ml | 6.126 ml |
5 mM | 0.123 ml | 0.613 ml | 1.225 ml |
10 mM | 0.061 ml | 0.306 ml | 0.613 ml |
5 mM | 0.012 ml | 0.061 ml | 0.123 ml |
Overview | Diagarek acetate is a synthetic gonadotropin-releasing hormone (GnRH) receptor antagonist, which reversibly binds to the GnRH receptor of the pituitary gland to reduce the release of gonadotropins and testosterone, thereby exerting an anti-prostate cancer effect. |
Antagonist of prostate cancer GnRH | Degarek (trade name: Fermong®) is the latest generation of GnRH antagonist, which incorporates P-urylphenylalanine at the 5,6 positions of its molecule. The change of chemical structure prolongs the action time of the drug while avoiding the hypersensitivity caused by histamine release. reaction. The clinical efficacy, safety and long-term medication of Dijarik have been verified by many clinical trials, and it is currently the most widely used GnRH antagonist. For advanced prostate cancer bone metastasis, Dijarek also shows good superiority. Studies have shown that patients with prostate cancer bone metastasis have significantly reduced plasma alkaline phosphatase (S-ALP) compared with GnRH agonist treatment after 1 year of treatment with Dijarek, and the S-ALP is often increased, which is often related to bone metastasis. In November 2018, the National Medical Products Administration (NMPA) approved the listing of Garrick for androgen-dependent prostate cancer patients, which is undoubtedly a major benefit for prostate cancer patients in my country. |
Mechanism of Action | Degarek is a gonadotropin-releasing hormone (GnRH) receptor inhibitor drug developed by Denmark Huiling Pharmaceutical Co., Ltd., which reversibly inhibits the pituitary GnRH receptor to reduce the release of gonadotropins and then inhibit the release of testosterone. Digarek delays the growth and deterioration of prostate cancer by inhibiting testosterone, which is essential for the continued growth of prostate cancer. The initial stage of using hormones to treat prostate cancer to reduce testosterone concentration causes a surge in testosterone concentration. This initial stimulation of the hormone receptor can temporarily promote tumor growth instead of inhibiting it, while Digarek will not. |
Use | Degalac acetate is a gonadotropin-releasing hormone receptor blocker, which has been approved in the United States and Europe respectively For the treatment of advanced (hormone-dependent) prostate cancer, it is approved for the treatment of prostate cancer in Japan. |
biological activity | Degarelix is a competitive, reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. |
target | GnRHR |
toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |