法赞雷生

法赞雷生
臨床資料
其他名稱	YZJ-1139; YZJ1139
给药途径	口服
藥物類別	食欲素受体拮抗剂（英语：Orexin receptor antagonist）
法律規範狀態
法律規範	研究性新药（英语：Investigational New Drug）;
藥物動力學數據
生物半衰期	1.9–3.7小时
识别信息
	IUPAC命名法 [(1S,2R,5S)-2-[(5-fluoropyridin-2-yl)oxymethyl]-8-azabicyclo[3.2.1]octan-8-yl]-(5-methyl-2-pyrimidin-2-ylphenyl)methanone; ;
CAS号	1808918-69-5 [GSRS]
PubChem CID	156889652;
ChemSpider	128922072;
UNII	MDH4D7M594;
ChEMBL	ChEMBL5314459;
化学信息
化学式	C25H25FN4O2
摩尔质量	432.50 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC1=CC(=C(C=C1)C2=NC=CC=N2)C(=O)N3[C@H]4CC[C@H]([C@@H]3CC4)COC5=NC=C(C=C5)F;
	InChI InChI=1S/C25H25FN4O2/c1-16-3-8-20(24-27-11-2-12-28-24)21(13-16)25(31)30-19-6-4-17(22(30)9-7-19)15-32-23-10-5-18(26)14-29-23/h2-3,5,8,10-14,17,19,22H,4,6-7,9,15H2,1H3/t17-,19-,22-/m0/s1; Key:PMJPLAGTPPVSRL-JLMWRMLUSA-N;

法赞雷生（INN：Fazamorexant，研发代号：YZJ-1139）是一种食欲素受体拮抗剂（英语：Orexin receptor antagonist），正在开发用于治疗失眠症^[1]^[5]^[2]^[3]。该药物通过口服给药^[1]。

法赞雷生是双食欲素受体拮抗剂（英语：Dual orexin receptor antagonist）（DORA），即同时作为食欲素受体（英语：Orexin receptor）OX1（英语：Hypocretin (orexin) receptor 1）和OX2（英语：Hypocretin (orexin) receptor 2）的拮抗剂^[2]^[3]。其达峰时间为0.6至1.3小时，消除半衰期为1.9至3.7小时^[4]。

法赞雷生正在由中国的江苏扬子江药业集团和/或上海海雁医药科技有限公司开发^[1]^[5]^[2]。截至2022年9月，该药物正处于失眠症治疗的Ⅲ期临床试验阶段^[1]^[5]^[3]。关于法赞雷生的公开信息相对较少^[2]。因此，它必须被排除在2020年针对失眠症的食欲素受体拮抗剂的文献综述之外^[2] 。

参见

研究性安眠药物列表（英语：List of investigational sleep drugs）

参考来源

^ ^1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 YZJ 1139. AdisInsight. 2022-09-14 [2024-10-31].
^ ^2.0 ^2.1 ^2.2 ^2.3 ^2.4 ^2.5 Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J. Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders. Expert Opinion on Drug Metabolism & Toxicology. 2020-11, 16 (11): 1063–1078. PMID 32901578. doi:10.1080/17425255.2020.1817380.
^ ^3.0 ^3.1 ^3.2 ^3.3 Beckenstrom AC, Coloma PM, Dawson GR, Finlayson AK, Malik A, Post A, Steiner MA, Potenza MN. Use of experimental medicine approaches for the development of novel psychiatric treatments based on orexin receptor modulation. Neuroscience and Biobehavioral Reviews. 2023-04, 147: 105107. PMC 10165155 . PMID 36828161. doi:10.1016/j.neubiorev.2023.105107.
^ ^4.0 ^4.1 Ni J, Jin L, Zhao D, Zhang W, Li B, Huang X, Hao X. Pharmacokinetics, Pharmacodynamic, Safety and Tolerability of Fazamorexant, a Novel Dual Orexin Receptor Antagonist: Report of the First-in-Human Study. Drug Design, Development and Therapy. 2025-06-19, 19: 5271–5282. PMID 40552089 请检查|pmid=值 (帮助). doi:10.2147/DDDT.S501111 .
^ ^5.0 ^5.1 ^5.2 Delving into the Latest Updates on Fazamorexant with Synapse. Synapse. 2024-10-31 [2024-10-31].

这是一篇作用於神经系统的藥品小作品。您可以通过编辑或修订扩充其内容。

[AdisInsight-1] 1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 YZJ 1139. AdisInsight. 2022-09-14 [2024-10-31].

[MuehlanVaillantZenklusen2020-2] 2.0 ^2.1 ^2.2 ^2.3 ^2.4 ^2.5 Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J. Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders. Expert Opinion on Drug Metabolism & Toxicology. 2020-11, 16 (11): 1063–1078. PMID 32901578. doi:10.1080/17425255.2020.1817380.

[BeckenstromColomaDawson2023-3] 3.0 ^3.1 ^3.2 ^3.3 Beckenstrom AC, Coloma PM, Dawson GR, Finlayson AK, Malik A, Post A, Steiner MA, Potenza MN. Use of experimental medicine approaches for the development of novel psychiatric treatments based on orexin receptor modulation. Neuroscience and Biobehavioral Reviews. 2023-04, 147: 105107. PMC 10165155 . PMID 36828161. doi:10.1016/j.neubiorev.2023.105107.

[NiJinZhao2025-4] 4.0 ^4.1 Ni J, Jin L, Zhao D, Zhang W, Li B, Huang X, Hao X. Pharmacokinetics, Pharmacodynamic, Safety and Tolerability of Fazamorexant, a Novel Dual Orexin Receptor Antagonist: Report of the First-in-Human Study. Drug Design, Development and Therapy. 2025-06-19, 19: 5271–5282. PMID 40552089 请检查|pmid=值 (帮助). doi:10.2147/DDDT.S501111 .

[Synapse-5] 5.0 ^5.1 ^5.2 Delving into the Latest Updates on Fazamorexant with Synapse. Synapse. 2024-10-31 [2024-10-31].

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