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Relative to suvorexant, daridorexant has a shorter half-life (8 hours) while lemborexant has a longer half-life (17–55 hours). [14] However, although lemborexant has a longer terminal elimination half-life than suvorexant, it appears to be more rapidly cleared in the earlier phases of elimination.
Daridorexant, sold under the brand ... Besides daridorexant, other orexin receptor antagonists, like suvorexant and lemborexant, have also been introduced. [16] [17 ...
The pharmacokinetics of suvorexant are significantly affected by age, sex, and other factors, leading to increased blood concentrations in female, obese, and older patients. [7] These factors do not significantly affect the pharmacokinetics of lemborexant [7] or daridorexant. [31]
Lemborexant was approved for medical use in the United States in December 2019. [9] [10] [11] It is a schedule IV controlled substance in the United States and may have a low potential for misuse. [3] [8] Besides lemborexant, other orexin receptor antagonists including suvorexant and daridorexant have also been introduced. [12] [13]
Lemborexant, an orexin receptor antagonist, was approved for use in the United States in 2019. Most ligands acting on the orexin system so far are polypeptides modified from the endogenous agonists orexin-A and orexin-B, however there are some subtype-selective non-peptide antagonists available for research purposes.
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SB-408124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX 1, with around 70x selectivity for OX 1 over OX 2 receptors, and improved oral bioavailability compared to the older OX 1 antagonist SB-334867.
Suvorexant has undergone three phase III trials and was approved in 2014 by the US Food and Drug Administration (FDA) after being denied approval the year before. [80] The other FDA-approved orexin antagonists are lemborexant (Dayvigo) [81] and daridorexant (Quviviq). [82]
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