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An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one (selective orexin receptor antagonist or SORA) or both (dual orexin receptor antagonis or DORA) of the orexin receptors, OX 1 and OX 2. [ 1] Medical applications include treatment of sleep disorders such as ...
Daridorexant. Daridorexant, sold under the brand name Quviviq, is an orexin antagonist medication which is used for the treatment of insomnia. [1] [4] [6] [7] [8] Daridorexant is taken by mouth. [1] [4] [7] Side effects of daridorexant include headache, somnolence, and fatigue. [1] [7] The medication is a dual orexin receptor antagonist (DORA).
The orexin/hypocretin system is the target of the insomnia medication suvorexant (Belsomra), which works by blocking both orexin receptors. [79] 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]
Seltorexant, also known by its developmental code names MIN-202 and JNJ-42847922, is an orexin antagonist medication which is under development for the treatment of depression and insomnia. [3] [2] It is a selective antagonist of the orexin OX 2 receptor (2-SORA). [2] [4] [1] The medication is taken by mouth. [1]
Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication which is used in the treatment of insomnia. [2] [6] It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults. [2] [6] Suvorexant helps with falling asleep faster, sleeping longer, being ...
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.
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]
Firazorexton ( INN; development code TAK-994) is an experimental orexin 2 (OX 2) receptor agonist first described in a 2019 patent filed by Takeda Pharmaceutical Company. [1] [2] Firazorexton was studied by Takeda for the treatment of narcolepsy. [3] [4] [5] It is a small-molecule and orally active compound and acts as a highly selective ...