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Contents

   



(Top)
  


1 Pharmacology  


1.1  Pharmacodynamics  




1.2  Pharmacokinetics  






2 History  




3 References  




4 External links  













Indiplon






●Igbo
 ●Српски / srpski
 ●Srpskohrvatski / српскохрватски
  
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From Wikipedia, the free encyclopedia
  

Indiplon
Clinical data
Routes of
administration		Oral
ATC code
  • none
Pharmacokinetic data
Elimination half-life1.5–1.8 hours
Identifiers

  • N-methyl-N-[3-[3-(thiophene-2-carbonyl)
    pyrazolo[5,1-b]pyrimidin-7-yl]phenyl]acetamide

CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.133.676 Edit this at Wikidata
Chemical and physical data
FormulaC20H16N4O2S
Molar mass376.43 g·mol−1
3D model (JSmol)

  • O=C(C1=CC=CS1)C2=C3N=CC=C(C4=CC(N(C)C(C)=O)=CC=C4)N3N=C2

  • InChI=1S/C20H16N4O2S/c1-13(25)23(2)15-6-3-5-14(11-15)17-8-9-21-20-16(12-22-24(17)20)19(26)18-7-4-10-27-18/h3-12H,1-2H3 checkY

  • Key:CBIAWPMZSFFRGN-UHFFFAOYSA-N checkY

 ☒NcheckY (what is this?)  (verify)

Indiplon (INN and USAN) is a nonbenzodiazepine, hypnotic sedative that was developed in two formulations—an immediate-release formulation for sleep onset, and a modified-release (also called controlled-release or extended-release) version for sleep maintenance.

Pharmacology[edit]

Pharmacodynamics[edit]

Indiplon works by enhancing the action of the inhibitory neurotransmitter GABA, like most other nonbenzodiazepine sedatives. It primarily binds to the α1 subunits of the GABAA receptors in the brain.[1]

Pharmacokinetics[edit]

Indiplon has a short elimination half-life of 1.5 to 1.8 hours in young and elderly subjects, respectively.[2]

History[edit]

Indiplon was discovered at Lederle Laboratories (which was later acquired by Wyeth) in the 1980s and was called CL 285,489.[3]: 454  In 1998 Lederle licensed it, along with other early stage drug candidates, to DOV Pharmaceutical, a startup formed by former Lederle employees, and Dov exclusively sublicensed its rights in the drug to Neurocrine Biosciences in that same year.[3] In 2002, Neurocrine entered into an agreement with Pfizer to develop the drug.[3]

Indiplon was originally scheduled for release in 2007, when Sanofi-Aventis' popular hypnotic zolpidem lost its patent rights in the United States and thus became available as a much less expensive generic. In 2002, Neurocrine Biosciences had entered into an agreement with Pfizer to co-market indiplon in the US, in a deal worth a potential $400mn.[4] However, following the issuing of a non-approvable letter for the modified-release 15 mg formulation and an approvable letter with stipulations for the 5 mg and 10 mg immediate-release version by the FDA in May 2006,[5] Pfizer ended its relationship with Neurocrine.[6] Neurocrine's stock price dropped 60% on the news.[7]

Following a resubmission, the FDA in December 2007 deemed Neurocrine's new drug application (NDA) 'approvable' in the 5 and 10 mg formulations,[8] but requested new studies as a prerequisite to approval, including a clinical trial in the elderly, a safety study comparing adverse effects to those of similarly marketed drugs, and a preclinical study examining indiplon's safety in the third trimester of pregnancy.[9]

Following the 2007 FDA letter, Neurocrine decided to discontinue all clinical and marketing development of Indiplon in the United States.[8][9]

References[edit]

  1. ^ Petroski RE, Pomeroy JE, Das R, Bowman H, Yang W, Chen AP, Foster AC (April 2006). "Indiplon is a high-affinity positive allosteric modulator with selectivity for alpha1 subunit-containing GABAA receptors" (PDF). The Journal of Pharmacology and Experimental Therapeutics. 317 (1): 369–77. doi:10.1124/jpet.105.096701. PMID 16399882. S2CID 46510829.
  • ^ Lemon MD, Strain JD, Hegg AM, Farver DK (September 2009). "Indiplon in the management of insomnia". Drug Design, Development and Therapy. 3: 131–142. doi:10.2147/dddt.s3207. PMC 2769245. PMID 19920929.
  • ^ a b c Neubauer DN (2010). "Indiplon". In Monti JS, Pandi-Perumal SR, Möhler H (eds.). GABA and Sleep: Molecular, Functional and Clinical Aspects. Springer Science & Business Media. pp. 453–464. ISBN 9783034602266.
  • ^ "San Diego's Neurocrine Biosciences Scores Second Big Deal in Two Days". The Motley Fool. 18 June 2010.
  • ^ "Neurocrine's FDA Nightmare". TheStreet.com. 16 May 2006.
  • ^ "Pfizer Drops Neurocrine Deal". TheStreet.com. 22 June 2006.
  • ^ "Neurocrine stock price plunges 60 percent:FDA's mixed review of sleeping pill Indiplon could threaten Pfizer-Neurocrine partnership". CNN Money. 15 May 2006.
  • ^ a b "Neurocrine Receives Approvable Letter for Indiplon Capsules with Additional Safety and Efficacy Data Required by FDA" (Press release). Neurocrine Biosciences, Inc. 2007-12-13. Retrieved 2007-12-13.
  • ^ a b "Additional Pipeline Projects". Neurocrine. 2012-02-16. Archived from the original on 2012-03-27. Retrieved 2014-06-24.

    • External links[edit]


    Retrieved from "https://en.wikipedia.org/w/index.php?title=Indiplon&oldid=1214852205"
    Categories: 
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