Esmirtazapine

Esmirtazapine
Systematic (IUPAC) name
(S)-1,2,3,4,10,14b-hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benzazepine
Clinical data
Legal status
  • Uncontrolled
Routes of
administration		 Oral
Pharmacokinetic data
Metabolism Liver (CYP2D6)[1]
Identifiers
CAS Number 61337-87-9 YesY
ATC code None
PubChem CID 3085218
E. maleate: CID 6451144
DrugBank DB00316 YesY
ChemSpider 2342166 YesY
UNII 4685R51V7M YesY
KEGG D04055 YesY
Chemical data
Formula C17H19N3
Molar mass 265.35 g/mol
Physical data
Melting point 114 to 116 °C (237 to 241 °F)
Solubility in water Soluble in methanol and chloroform mg/mL (20 °C)
  (verify)

Esmirtazapine (ORG-50,081) is a drug which was under development by Organon for the treatment of insomnia and vasomotor symptoms (e.g., hot flashes) associated with menopause.[2][3][4][5] Esmirtazapine is the (S)-(+)-enantiomer of mirtazapine and possesses similar overall pharmacology, including inverse agonist actions at H1 and 5-HT2 receptors and antagonist actions at α2-adrenergic receptors.[2][6] As of March 2010, Merck terminated internal clinical development program for esmirtazapine, for hot flashes and insomnia, for strategic reasons.[7]

See also

References

  1. ↑ "A population analysis on the effects of the CYP2D6 deficiency on pharmacokinetics and exposure of esmirtazapine in healthy volunteers" (PDF).
  2. 1 2 "Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net".
  3. ↑ "A Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov".
  4. ↑ Teegarden BR, Al Shamma H, Xiong Y (2008). "5-HT(2A) inverse-agonists for the treatment of insomnia". Current Topics in Medicinal Chemistry 8 (11): 969–76. doi:10.2174/156802608784936700. PMID 18673166.
  5. ↑ Lewis V (November 2009). "Undertreatment of menopausal symptoms and novel options for comprehensive management". Current Medical Research and Opinion 25 (11): 2689–98. doi:10.1185/03007990903240519. PMID 19775194.
  6. ↑ Depression and bipolar disorder: Stahl's essential psychopharmacology. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-88663-5.
  7. ↑ http://www.merck.com/investors/financials/form-10-K-2009-final.pdf
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