Lemborexant_product_DataBase

Bioactivity

Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia[1].

Invitro

A high-fat and high-calorie meal has been found to delay the time to peak levels by 2 hours. Its plasma protein binding in vitro is 94%. Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5[2].

In Vivo

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, manifests by decreased body weight and food consumption, decreases mean fetal body weight, an increased number of dead fetuses, and skeletal, external and visceral malformations (omphalocele, cleft palate, and membranous ventricular septal defect) at >300 times the MRHD based on AUC[2]. 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].

Name

Lemborexant

CAS

1369764-02-2

Formula

C22H20F2N4O2

Molar Mass

410.42

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. OREXIN RECEPTOR ANTAGONIST PROVEN EFFECTIVE FOR BOTH SLEEP ONSET AND SLEEP MAINTENANCE IN CLINICAL DEVELOPMENT PROGRAM OF MORE THAN 2,000 PATIENTS. 2019. [2]. HIGHLIGHTS OF PRESCRIBING INFORMATION

PeptideDB

Lemborexant

CAS: 1369764-02-2 F: C22H20F2N4O2 W: 410.42