asenapine

Trade name: saphris

Small moleculeapproved

Approved

Aug 13, 2009

Asenapine is an antipsychotic drug. The mechanism of action of asenapine, as with other drugs having efficacy in schizophrenia and bipolar disorder, is unknown. Asenapine exhibits high affinity for serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors, dopamine D2, D3, D4, and D1 receptors, α1 and α2-adrenergic receptors, and histamine H1 receptors, and moderate affinity for H2 receptors. In in vitro assays asenapine acts as an antagonist at these receptors. It has been suggested that the efficacy of asenapine in schizophrenia is mediated through a combination of antagonist activity at D2 and 5-HT2A receptors. Asenapine is approved by the FDA for the acute treatment of schizophrenia in adults and for the acute treatment of manic or mixed episodes associated with bipolar I disorder, with or without psychotic features, in adults. — NCATS

Clinical trial activity

48 trials · 32 clinical orgs · 9 marketing orgs

Phase 1
3
Phase 2
37
Phase 3
35
Phase 4
7

Earliest trial started Oct 1, 2002 (NCT01101464)

Timeline

2000s

  1. Jan 1, 2002

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2003

    Earliest Phase 3 Sponsor(trial)

  3. Aug 13, 2009

    Organon — Earliest FDA Approval

  4. Aug 13, 2009

    Organon — NDA Organization

  5. Aug 13, 2009

    Forest Laboratories — NDA Secondary Org

  6. Aug 13, 2009

    Allergan — Marketing Organization

  7. Aug 13, 2009

    GlaxoSmithKline — NDA Secondary Org

  8. Aug 13, 2009

    AbbVie — Marketing Organization

2010s

  1. Jan 1, 2010

    Earliest Phase 1 Sponsor(trial)

  2. Aug 11, 2017

    Alembic — Marketing Organization

  3. Jul 17, 2018

    Sigmapharm Laboratories — Marketing Organization

  4. Oct 11, 2019

    Hisamitsu Pharmaceutical Co., Inc. — Marketing Organization

  5. Oct 11, 2019

    Hisamitsu Pharmaceutical Co., Inc. — NDA Secondary Org

2020s

  1. Dec 10, 2020

    Esteve Labs — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedAug 13, 2009

Chemistry & pharmacology

Loading structure…

SMILES

CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1
Mol. weight
285.77 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Black box warning

Sources

Also known as

  • 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz(2,3-6,7)oxepino(4,5-c)pyrrole
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine
  • asenapine maleate
  • asenapine maleate
  • asenapine maleate
  • asenapine maleate
  • asenapine maleate
  • asenapine maleate
  • asenapine maleate
  • org 5222
  • org 5222
  • org-5222
  • org-5222
  • org-5222
  • org-5222
  • org-5222
  • org-5222
  • saphris
  • saphris
  • saphris
  • saphris
  • saphris
  • sycrest
  • sycrest
  • sycrest

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02876900Phase 3Aug 1, 2016Noven Therapeutics
NCT02181803Phase 1Aug 1, 2014Merck
NCT02072954Phase 2/Phase 3 (Phase 3)Nov 1, 2013Accutest Research Laboratories (I) Pvt. Ltd., Amneal Pharmaceuticals
NCT01968161Phase 4Oct 1, 2013Centre de Recherche de l'Institut Universitaire en Santé Mentale de Québec
NCT01807741Phase 2Sep 1, 2013Merck, University of Cincinnati, University of Louisville
NCT01948024Phase 1Jul 1, 2013Advanced Pharma CR, LLC, Atlanta Center for Medical Research, bioRASI, LLC, Collaborative Neuroscience Network, Compass Research, Evolution Research Group, New Hope Clinical Research, Sun Pharmaceuticals
NCT01617187Phase 3Dec 1, 2012Merck
NCT01617200Phase 3Dec 1, 2012Forest Laboratories
NCT01765829Phase 3Nov 1, 2012Government of Spain, Universidad Carlos III Madrid
NCT01670019Phase 4Oct 1, 2012Duke University, Merck
NCT01684657Phase 3Sep 1, 2012Merck, University of California, Irvine
NCT01587118Phase 4Jun 1, 2012Forest Laboratories, Merck, Tuscaloosa Research & Education Advancement Corporation (TREAC)
NCT01549041Phase 4Apr 1, 2012Duke University, Merck
NCT00764478Phase 3Apr 1, 2012Merck
NCT01400113Phase 4Apr 1, 2012Schering-Plough, St. Joseph Hospital Health Center, University of Arizona
NCT01395992Phase 3Apr 1, 2012Forest Laboratories
NCT01396291Phase 3Dec 1, 2011Forest Laboratories
NCT01460290Phase 4Oct 1, 2011Case Western Reserve University
NCT01349907Phase 3Jun 1, 2011Merck
NCT01244815Phase 3Jun 1, 2011Merck
Showing 20 of 48 trials
Page 1 / 3

Organizations

Research & Development (32)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
MerckFor profit373242002
Forest LaboratoriesFor profit4322011
PfizerFor profit4012004
Duke UniversityAcademic/Hospital2212012
Accutest Research Laboratories (I) Pvt. Ltd.For profit1012013
Advanced Pharma CR, LLCFor profit1012013
Amneal PharmaceuticalsFor profit1112013
Atlanta Center for Medical ResearchFor profit1012013
bioRASI, LLCFor profit1112013
Case Western Reserve UniversityAcademic/Hospital1112011
Centre de Recherche de l'Institut Universitaire en Santé Mentale de QuébecAcademic/Hospital1112013
Collaborative Neuroscience NetworkFor profit1012013
Compass ResearchFor profit1012013
Evolution Research GroupFor profit1012013
Government of SpainGovernment1112012
Johns Hopkins UniversityAcademic/Hospital1112009
Meiji Seika Pharma Co., Ltd.For profit1012010
National Institute of Mental Health (NIMH)Government1012009
New Hope Clinical ResearchFor profit1012013
Noven TherapeuticsFor profit1112016
32 organizations
Page 1 / 2

Marketing (12)

OrganizationOrg typeRelationshipDate
AbbVieFor profitMKTGAug 13, 2009
AlembicFor profitSYNDec 10, 2020
AlembicFor profitMKTGAug 11, 2017
AllerganFor profitMKTGAug 13, 2009
Esteve LabsFor profitMKTGDec 10, 2020
Forest LaboratoriesFor profitNDA2Aug 13, 2009
GlaxoSmithKlineFor profitNDA2Aug 13, 2009
Hisamitsu Pharmaceutical Co., Inc.For profitMKTGOct 11, 2019
Hisamitsu Pharmaceutical Co., Inc.For profitSYNOct 11, 2019
Hisamitsu Pharmaceutical Co., Inc.For profitNDA2Oct 11, 2019
OrganonFor profitNDAAug 13, 2009
Sigmapharm LaboratoriesFor profitMKTGJul 17, 2018