Lemborexant 是一种可逆的、可口服的食欲素 OX1 和 OX2 受体双重拮抗剂，IC50值分别为 6.1 和 2.6 nM。它有用于失眠的研究潜力。

Lemborexant is a reversible and orally active dual antagonist of the orexin OX1 and OX2 receptors (IC50s: 6.1 nM and 2.6 nM).

Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5 [2].

Lemborexant is administered orally to pregnant rats during the period of organogenesis in 2 studies at doses of 60, 200, and 600 mg/kg/day or 20, 60, and 200 mg/kg/day, which are approximately 6 to >300 times the maximum recommended human dose (MRHD) based on AUC. Lemborexant causes maternal toxicity that consisted of decreased body weight and food consumption and toxicity to offspring consisting of decreased pup body weights, decreases femur length, and decreases acoustic startle responses at 206 times the MRHD based on AUC. The no observed adverse effect levels (NOAEL) of 100 mg/kg/day is approximately 93 times the MRHD based on AUC [2].

1369764-02-2

C22H20F2N4O2

410.42

E-2006;莱博雷生

DMSO:250 mg/mL (609.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years