asenapine
Trade name: saphris
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
Earliest trial started Oct 1, 2002 (NCT01101464)
Timeline
2000s
- Jan 1, 2002
Earliest Phase 2 Sponsor(trial)
- Jan 1, 2003
Earliest Phase 3 Sponsor(trial)
- Aug 13, 2009
Organon — Earliest FDA Approval
- Aug 13, 2009
Organon — NDA Organization
- Aug 13, 2009
Forest Laboratories — NDA Secondary Org
- Aug 13, 2009
Allergan — Marketing Organization
- Aug 13, 2009
GlaxoSmithKline — NDA Secondary Org
- Aug 13, 2009
AbbVie — Marketing Organization
2010s
- Jan 1, 2010
Earliest Phase 1 Sponsor(trial)
- Aug 11, 2017
Alembic — Marketing Organization
- Jul 17, 2018
Sigmapharm Laboratories — Marketing Organization
- Oct 11, 2019
Hisamitsu Pharmaceutical Co., Inc. — Marketing Organization
- Oct 11, 2019
Hisamitsu Pharmaceutical Co., Inc. — NDA Secondary Org
2020s
- Dec 10, 2020
Esteve Labs — Marketing Organization
Indications
Mechanism of action
- Serotonin 2a (5-HT2a) receptorANTAGONIST
HTR2A antagonist
- Dopamine D2 receptorANTAGONIST
DRD2 antagonist
- Unspecified targetOTHER
Unknown
Approval history
- approvedAug 13, 2009
Chemistry & pharmacology
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
Sources
- ChEMBLCHEMBL3187365 ↗
- WikipediaAsenapine ↗
- NCATSJKZ19V908O ↗
- ChEMBLCHEMBL3544974 ↗
- ChEMBLCHEMBL1201756 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02876900 | Phase 3 | Aug 1, 2016 | Noven Therapeutics |
| NCT02181803 | Phase 1 | Aug 1, 2014 | Merck |
| NCT02072954 | Phase 2/Phase 3 (Phase 3) | Nov 1, 2013 | Accutest Research Laboratories (I) Pvt. Ltd., Amneal Pharmaceuticals |
| NCT01968161 | Phase 4 | Oct 1, 2013 | Centre de Recherche de l'Institut Universitaire en Santé Mentale de Québec |
| NCT01807741 | Phase 2 | Sep 1, 2013 | Merck, University of Cincinnati, University of Louisville |
| NCT01948024 | Phase 1 | Jul 1, 2013 | Advanced Pharma CR, LLC, Atlanta Center for Medical Research, bioRASI, LLC, Collaborative Neuroscience Network, Compass Research, Evolution Research Group, New Hope Clinical Research, Sun Pharmaceuticals |
| NCT01617187 | Phase 3 | Dec 1, 2012 | Merck |
| NCT01617200 | Phase 3 | Dec 1, 2012 | Forest Laboratories |
| NCT01765829 | Phase 3 | Nov 1, 2012 | Government of Spain, Universidad Carlos III Madrid |
| NCT01670019 | Phase 4 | Oct 1, 2012 | Duke University, Merck |
| NCT01684657 | Phase 3 | Sep 1, 2012 | Merck, University of California, Irvine |
| NCT01587118 | Phase 4 | Jun 1, 2012 | Forest Laboratories, Merck, Tuscaloosa Research & Education Advancement Corporation (TREAC) |
| NCT01549041 | Phase 4 | Apr 1, 2012 | Duke University, Merck |
| NCT00764478 | Phase 3 | Apr 1, 2012 | Merck |
| NCT01400113 | Phase 4 | Apr 1, 2012 | Schering-Plough, St. Joseph Hospital Health Center, University of Arizona |
| NCT01395992 | Phase 3 | Apr 1, 2012 | Forest Laboratories |
| NCT01396291 | Phase 3 | Dec 1, 2011 | Forest Laboratories |
| NCT01460290 | Phase 4 | Oct 1, 2011 | Case Western Reserve University |
| NCT01349907 | Phase 3 | Jun 1, 2011 | Merck |
| NCT01244815 | Phase 3 | Jun 1, 2011 | Merck |
Organizations
Research & Development (32)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 37 | 32 | 4 | 2002 |
| Forest Laboratories | For profit | 4 | 3 | 2 | 2011 |
| Pfizer | For profit | 4 | 0 | 1 | 2004 |
| Duke University | Academic/Hospital | 2 | 2 | 1 | 2012 |
| Accutest Research Laboratories (I) Pvt. Ltd. | For profit | 1 | 0 | 1 | 2013 |
| Advanced Pharma CR, LLC | For profit | 1 | 0 | 1 | 2013 |
| Amneal Pharmaceuticals | For profit | 1 | 1 | 1 | 2013 |
| Atlanta Center for Medical Research | For profit | 1 | 0 | 1 | 2013 |
| bioRASI, LLC | For profit | 1 | 1 | 1 | 2013 |
| Case Western Reserve University | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Centre de Recherche de l'Institut Universitaire en Santé Mentale de Québec | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Collaborative Neuroscience Network | For profit | 1 | 0 | 1 | 2013 |
| Compass Research | For profit | 1 | 0 | 1 | 2013 |
| Evolution Research Group | For profit | 1 | 0 | 1 | 2013 |
| Government of Spain | Government | 1 | 1 | 1 | 2012 |
| Johns Hopkins University | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Meiji Seika Pharma Co., Ltd. | For profit | 1 | 0 | 1 | 2010 |
| National Institute of Mental Health (NIMH) | Government | 1 | 0 | 1 | 2009 |
| New Hope Clinical Research | For profit | 1 | 0 | 1 | 2013 |
| Noven Therapeutics | For profit | 1 | 1 | 1 | 2016 |
Marketing (12)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| AbbVie | For profit | MKTG | Aug 13, 2009 |
| Alembic | For profit | SYN | Dec 10, 2020 |
| Alembic | For profit | MKTG | Aug 11, 2017 |
| Allergan | For profit | MKTG | Aug 13, 2009 |
| Esteve Labs | For profit | MKTG | Dec 10, 2020 |
| Forest Laboratories | For profit | NDA2 | Aug 13, 2009 |
| GlaxoSmithKline | For profit | NDA2 | Aug 13, 2009 |
| Hisamitsu Pharmaceutical Co., Inc. | For profit | MKTG | Oct 11, 2019 |
| Hisamitsu Pharmaceutical Co., Inc. | For profit | SYN | Oct 11, 2019 |
| Hisamitsu Pharmaceutical Co., Inc. | For profit | NDA2 | Oct 11, 2019 |
| Organon | For profit | NDA | Aug 13, 2009 |
| Sigmapharm Laboratories | For profit | MKTG | Jul 17, 2018 |