Samelisant (INNTooltip International Nonproprietary Name; developmental code name SUVN-G3031) is an experimental wakefulness-promoting agent acting as a selective histamine H3 receptor inverse agonist which is under development for the treatment of narcolepsy.[1][2][3][4] It was also under development for the treatment of cognition disorders and Parkinson's disease, but no recent development has been reported for these indications.[1][3] As of June 2024, samelisant is in phase 2 clinical trials for the treatment of narcolepsy.[1][5]

Samelisant
Clinical data
Other namesSUVN-G3031
Drug classHistamine H3 receptor inverse agonist; Wakefulness-promoting agent
Pharmacokinetic data
Elimination half-life23-34 hours
Identifiers
  • N-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-morpholin-4-ylacetamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC21H31N3O3
Molar mass373.497 g·mol−1
3D model (JSmol)
  • C1CC(C1)N2CCC(CC2)OC3=CC=C(C=C3)NC(=O)CN4CCOCC4
  • InChI=1S/C21H31N3O3/c25-21(16-23-12-14-26-15-13-23)22-17-4-6-19(7-5-17)27-20-8-10-24(11-9-20)18-2-1-3-18/h4-7,18,20H,1-3,8-16H2,(H,22,25)
  • Key:LNXDUSQEXVQFGP-UHFFFAOYSA-N

See also

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References

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  1. ^ a b c "Samelisant - Suven Life Sciences". AdisInsight. 12 June 2024. Retrieved 22 September 2024.
  2. ^ Alhusaini M, Eissa N, Saad AK, Beiram R, Sadek B (2022). "Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep-Wake Cycle Disorder". Frontiers in Pharmacology. 13: 861094. doi:10.3389/fphar.2022.861094. PMC 9198498. PMID 35721194.
  3. ^ a b Konofal E (August 2024). "From past to future: 50 years of pharmacological interventions to treat narcolepsy". Pharmacology, Biochemistry, and Behavior. 241: 173804. doi:10.1016/j.pbb.2024.173804. PMID 38852786.
  4. ^ Nirogi R, Jayarajan P, Benade V, Abraham R, Goyal VK (June 2024). "Hits and misses with animal models of narcolepsy and the implications for drug discovery". Expert Opinion on Drug Discovery. 19 (6): 755–768. doi:10.1080/17460441.2024.2354293. PMID 38747534.
  5. ^ Nirogi R, Mudigonda K, Bhyrapuneni G, Muddana NR, Shinde A, Goyal VK, et al. (July 2020). "Safety, Tolerability, and Pharmacokinetics of SUVN-G3031, a Novel Histamine-3 Receptor Inverse Agonist for the Treatment of Narcolepsy, in Healthy Human Subjects Following Single and Multiple Oral Doses". Clinical Drug Investigation. 40 (7): 603–615. doi:10.1007/s40261-020-00920-8. PMID 32399853.