ALZ-801 是一种有效的口服小分子 β-淀粉样蛋白 (Aβ) 抗寡聚体和聚集抑制剂，与母体化合物相比，具有显着改善的 PK 特性和胃肠道耐受性的曲米酸的缬氨酸结合前药。
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound[1]. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease[2].
ALZ-801 (oral administration; 172 mg/kg; single dose) exhibits mean AUCt values of 58,758 and 5841 ng/ml.h in plasma and brain, respectively. The ALZ-801: Tramiprosate ratio in plasma and brain is 1.8 and 3.1, respectively in male CD-1 mice[1].
[1]. John A. Hey, et al. Discovery and Identification of an Endogenous Metabolite of Tramiprosate and Its Prodrug ALZ-801 that Inhibits Beta Amyloid Oligomer Formation in the Human Brain. CNS Drugs. 2018; 32(9): 849-861.
[2]. Hey JA, et al. Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer’s Disease. Clin Pharmacokinet. 2018 Mar;57(3):315-333.
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