生物活性

• 描述Gonadotropin-releasing hormone (GnRH) is a decapeptide, which is synthesized in the hypothalamus and plays a pivotal role in the secretion of gonadotropins, such as luteinizing hormone and follicle-stimulating hormone. Relugolix is a novel, non-peptide, orally active GnRH antagonist with IC₅₀s of 0.33 and 0.32 nM for human and monkey GnRH receptor, respectively. In vivo, twice-daily oral administration of relugolix (10 mg/kg) for 4 weeks reduced the prostate weight to castrate levels in male knock-in mice. In female knock-in mice, twice-daily oral administration of relugolix (100 mg/kg) induced constant diestrous phases within the first week, decreased the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks. Moreover, gonadal function of relugolix-treated knock-in mice began to recover after 5 days and almost completely recovered within 14 days after drug withdrawal in both sexes suggesting suppression the hypothalamic-pituitary-gonadal axis caused by relugolix is reversible^[3].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01458301	Endometriosis	Phase 2	Completed	-	-
  NCT01452659	Uterine Fibroids	Phase 2	Completed	-	Japan ... more >> Chiba-shi, Chiba, Japan Itchihara-shi, Chiba, Japan Matsuno-shi, Chiba, Japan Matsuyama-shi, Ehime, Japan Nihama-shi, Ehime, Japan Fukui-shi, Fukui, Japan Fukuoka-shi, Fukuoka, Japan Iizuka-shi, Fukuoka, Japan Yanagigawa-shi, Fukuoka, Japan Mebashi-shi, Gunma, Japan Ebetsu-shi, Hokkaido, Japan Sapporo-shi, Hokkaido, Japan Amagasaki-shi, Hyogo, Japan Kobe-shi, Hyogo, Japan Kamakura-shi, Kanagawa, Japan Yokohama-shi, Kanagawa, Japan Oita-shi, Oita, Japan Ibaraki-shi, Osaka, Japan Osaka-shi, Osaka, Japan Sakai-shi, Osaka, Japan Tondabayashi-shi, Osaka, Japan Chuo-ku, Tokyo, Japan Itabashi-ku, Tokyo, Japan Setagaya-ku, Tokyo, Japan Shinagawa-ku, Tokyo, Japan Suginami-ku, Tokyo, Japan Toyama-shi, Toyama, Japan Collapse <<
  NCT02655237	Uterine Fibroids	Phase 3	Completed	-	Japan ... more >> Nagoya, Aichi, Japan Matsudo, Chiba, Japan Kouriyama, Fukushima, Japan Ebetsu, Hokkaido, Japan Sapporo, Hokkaido, Japan Kako-gun, Hyogo, Japan Nishinomiya, Hyogo, Japan Kawasaki, Kanagawa, Japan Yamato, Kanagawa, Japan Yokohama, Kanagawa, Japan Ibaraki, Osaka, Japan Sakai, Osaka, Japan Suita, Osaka, Japan Yao, Osaka, Japan Bunkyo-ku, Tokyo, Japan Chiyoda-ku, Tokyo, Japan Chuou-ku, Tokyo, Japan Minato-ku, Tokyo, Japan Setagaya-ku, Tokyo, Japan Suginami-ku, Tokyo, Japan Taitou-ku, Tokyo, Japan Kagoshima, Japan Kyoto, Japan Osaka, Japan Saitama, Japan Collapse <<

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• 参考文献

• [1] MacLean DB, Shi H, et al. Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87.

  [2] Nakata D, Masaki T, et al. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Pharmacol. 2014 Jan 15;723:167-74.

  [3] Nakata D, Masaki T, Tanaka A, Yoshimatsu M, Akinaga Y, Asada M, Sasada R, Takeyama M, Miwa K, Watanabe T, Kusaka M. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Pharmacol. 2014 Jan 15;723:167-74