Relugolix

Superiority:

瑞卢戈利用途与合成方法简介目前，瑞卢戈利已经在1期、2期和3期临床试验的近1600名研究参与者中进行了评估。Relugolix在每日口服一次时，可以迅速降低女性的雌激素和孕激素水平。武田制药通过一系列在日本进行的临床III期研究，对比了Relugolix与leuprorelin(亮丙瑞林)治疗月经过多的子宫纤维化的安全性和有效性，以及上述两个药物在治疗与子宫纤维化有关的疼痛症状上的安全性和有效性，最终证实了relugolix用于子宫纤维瘤的的安全性和有效性。此外，武田制药进行了relugolix的子宫内膜异位和前列腺癌的II期临床研究，证实relugolix能显著减轻子宫内膜异位引起的疼痛，也能降低血清睾酮到去势水平并显著降低前列腺特异性抗原(PSA)。应用瑞卢戈利(Relugolix)，化学名称为N-(4-(1-(2,6-二氟苄基)-5-((二甲氨基)甲基)-3-(6-甲氧基-3-哒嗪基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-d]嘧啶-6-基)苯基)-N'-甲氧基脲。其是由Myovant公司和武田药业(Takeda)共同开发的一种新药，是一种小分子促性腺激素释放素(GnRH)受体拮抗剂，有潜力用于子宫纤维瘤、子宫内膜异位、前列腺癌等适应症。

The melting point of the Ruilugoli property is 228 ° C (decomp) (Solv: ethyllacestate (141-78-6); Tetrahydrofuran (109-99-9) density 1.442 ± 0.06g/cm3 (Predicted) storage conditions Storeat-20 ° C solubility DMSO: 2.0 (MaxConc. mg/mL); 32.1 (MaxConc. mM) Ethanol: 1.0 (MaxConc. mg/mL); 1.6 (MaxConc. mM) Form Acrystallinesolid Acid dissociation constant (pKa) 13.17 ± 0.70 (Predicted) InChIKeyAOMXMOCNKJTRQP-UHFFFAOYSA-NSMILESN (C1=CC=C (C2SC3=C (C=2CN (C) C) C (=O) N (C2=NN=C (OC) C=C2) C (=O) N3CC2=C (F) C=CC=C2F) C=C1) C (NOC)=O Introduction to the use and synthesis method of Ruilugoli Li has been evaluated among nearly 1600 study participants in Phase 1, Phase 2 and Phase 3 clinical trials. Relugolix can rapidly reduce the estrogen and Progestogen levels of women when taken orally once a day. Takeda Pharmaceutical compared the safety and effectiveness of Relugolix and Leupreelin in the treatment of uterine fibrosis with menorrhagia, as well as the safety and effectiveness of the above two drugs in the treatment of pain symptoms related to uterine fibrosis through a series of clinical phase III studies conducted in Japan, and finally confirmed the safety and effectiveness of relagolix in the treatment of uterine Fibroma. In addition, Takeda Pharmaceuticals conducted a phase II clinical study on relugolix for endometriosis and prostate cancer, confirming that relugolix can significantly reduce pain caused by endometriosis, reduce serum testosterone to castration levels, and significantly reduce prostate specific antigen (PSA). Apply Relugolix, with the chemical name of N - (4- (1- (2,6-difluorobenzyl) -5- ((dimethylamino) methyl) -3- (6-neneneba methoxy -3-pyridazinyl) -2,4-dioxo-1,2,3,4- Tetrahydrothiophene o [2,3-d] pyrimidin-6-yl) phenyl) - N '- Methoxy group urea. It is a new drug jointly developed by Myovant Company and Takeda Pharmaceutical Co., Ltd. It is a small molecule Gonadotropin releasing hormone (GnRH) receptor antagonist and has potential for use in indications such as Fibroma of uterus, endometriosis and prostate cancer.