Lemborexant is an orally active dual orexin receptor antagonist (DORA) used in the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. It is a small-molecule active pharmaceutical ingredient that selectively inhibits the activity of orexin OX1 and OX2 receptors.
The orexin system plays an important role in maintaining wakefulness. Lemborexant reduces orexin-mediated wake signaling by blocking both OX1 and OX2 receptors, thereby facilitating sleep onset and supporting sleep maintenance.
Lemborexant is a synthetic small-molecule pharmaceutical compound with the molecular formula C22H20F2N4O2 and a molecular weight of approximately 410.42 g/mol. Its CAS Number is 1369764-02-2.
Lemborexant is a selective orexin receptor antagonist and is supplied as a pharmaceutical-grade active ingredient for formulation and pharmaceutical manufacturing applications.
Lemborexant is a dual orexin receptor antagonist that binds to and inhibits both OX1R (orexin receptor type 1) and OX2R (orexin receptor type 2).
Orexin signaling promotes wakefulness and arousal. By blocking OX1R and OX2R, Lemborexant decreases orexin-mediated wake-promoting signaling, helping patients initiate and maintain sleep.
Lemborexant is used for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.
It is administered orally and is formulated as tablets for pharmaceutical use.
Lemborexant API can be evaluated using validated analytical procedures for identification, assay, related substances, stereochemical purity, water content, residual solvents, elemental impurities and other applicable quality attributes.
HPLC and suitable spectroscopic and chromatographic techniques may be used for identity, assay and purity testing. Control of stereochemical purity and degradation products is important because Lemborexant contains a defined stereochemical configuration.
Acceptance criteria should be based on the applicable approved manufacturer's drug-substance specification, Certificate of Analysis and relevant regulatory requirements.
Lemborexant should be stored in a tightly closed pharmaceutical-grade container under controlled storage conditions. The API should be protected from excessive heat, moisture, direct light and contamination. Specific storage requirements should follow the applicable manufacturer's approved specification.
Lemborexant API may be supplied for qualified pharmaceutical manufacturing, formulation development, research and analytical applications. Product specifications, Certificate of Analysis, packaging details and regulatory documentation should be confirmed according to the intended application.
Lemborexant API is available for pharmaceutical development and manufacturing requirements subject to applicable quality and regulatory requirements. Customers can request product specifications, analytical documentation, Certificate of Analysis, packaging information and commercial details for their specific requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 2.0% |