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Relugolix

CAS No. : 737789-87-6

MCE 站：Relugolix

产品活性：Relugolix (TAK-385) 是一种有效的，具有口服活性，非肽性促性腺激素释放激素(GnRH) 的拮抗剂。与 TAK-013 (HY-100209) 相比，Relugolix 对人 (IC₅₀=0.33 nM) 和猴子 (IC₅₀=0.32 nM) 的受体具有高亲和力和强拮抗活性。Relugolix 用于性激素依赖性疾病的研究，如子宫内膜异位症、子宫肌瘤、前列腺癌等。

研究领域：GPCR/G Protein

作用靶点：GnRH Receptor

In Vitro: Relugolix exhibits strong binding affinity (IC₅₀=0.32 nM) for the monkey receptor comparable to that for the human receptor (IC₅₀=0.33 nM) while displaying a 30000-fold decrease for the rat receptor (IC₅₀=9800 nM). The antagonistic in vitro activity of TAK-385 with respect to the human receptor (IC₉₀=18 nM) exceeded that for the monkey receptor (IC₉₀=1700 nM) by 95-fold in the presence of 40% serum.

In Vivo: Relugolix (oral administration; 1-3 mg/kg; single dose for pharmacokinetic study) exhibits a good pharmacokinetic profile and obvious suppressive effects of circulating LH levels in monkeys at a dose of 1 mg/kg. The pharmacokinetic profile exhibits with 16.0 ng/mL, 2.7 h, and 90.1 ng for C_max, T_max, and AUC_o, respectively in male cynomolgus monkeys.
Relugolix (oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks) significantly decreases the testis weight, and reduces the ventral prostate weight at 3 mg/kg and decreases it to castrate levels at 10 mg/kg in male hGNRHR-knock-in mice.
Relugolix (oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks) induces constant diestrous phases in all mice within the first week at 100 mg/kg, and significantly decreases the weights of ovaries and uteri at this dose after 4 weeks in female hGNRHR-knock-in mice.

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