CDEK
← All drugs Report issue

blonanserin

Trade name: Lonasen

Small moleculeexperimental

Blonanserin, sold under the brand name Lonasen, is a relatively new atypical antipsychotic commercialized by Dainippon Sumitomo Pharma in Japan and Korea for the treatment of schizophrenia. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As with many second-generation (atypical) antipsychotics it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics such as haloperidol. — Wikipedia

Clinical trial activity

4 trials · 4 clinical orgs · 0 marketing orgs

Phase 1
0
Phase 2
3
Phase 3
3
Phase 4
1

Earliest trial started Feb 1, 2012 (NCT01516424)

Timeline

2010s

  1. Jan 1, 2012

    Earliest Phase 3 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

  • Dopamine D3 receptorANTAGONIST

    Dopamine D3 receptor antagonist

    Also has high affinity for 5-HT6 receptors. Low affinity for 5-HT2C, adrenergic α1, histamine H1, muscarinic (M1) receptors and 5-HT1A receptors. Blonanserin has lower affinity for 5-HT2 receptors (Ki = 0.812 nM) compared to D2 receptors (Ki = 0.142 nM), its active metabolite, AD-6048, has highest affinity for D3 receptors.

  • Dopamine D2 receptorANTAGONIST

    Dopamine D2 receptor antagonist

    Also has high affinity for 5-HT6 receptors. Low affinity for 5-HT2C, adrenergic α1, histamine H1, muscarinic (M1) receptors and 5-HT1A receptors. Blonanserin has lower affinity for 5-HT2 receptors (Ki = 0.812 nM) compared to D2 receptors (Ki = 0.142 nM), its active metabolite, AD-6048, has highest affinity for D3 receptors.

  • Serotonin 2a (5-HT2a) receptorANTAGONIST

    Serotonin 2a (5-HT2a) receptor antagonist

    Also has high affinity for 5-HT6 receptors. Low affinity for 5-HT2C, adrenergic α1, histamine H1, muscarinic (M1) receptors and 5-HT1A receptors. Blonanserin has lower affinity for 5-HT2 receptors (Ki = 0.812 nM) compared to D2 receptors (Ki = 0.142 nM), its active metabolite, AD-6048, has highest affinity for D3 receptors.

  • Dopamine D3 receptorINHIBITOR

    DRD3 inhibitor

  • Dopamine D2 receptorINHIBITOR

    DRD2 inhibitor

Chemistry & pharmacology

Loading structure…

SMILES

CCN1CCN(c2cc(-c3ccc(F)cc3)c3c(n2)CCCCCC3)CC1
Mol. weight
367.51 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta(b)pyridine
  • ad 5423
  • ad-5423
  • ad-5423
  • blonanserin
  • blonanserin
  • blonanserin
  • blonanserin
  • blonanserin
  • blonanserin
  • blonanserin
  • blonanserin
  • blonanserin
  • cycloocta(b)pyridine, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-
  • dsp-5423p
  • lonasen
  • lonasen

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT03784222Phase 4Jan 22, 2019Peking University, Sumitomo
NCT02335658Phase 3Dec 1, 2014Sumitomo Dainippon
NCT02287584Phase 3Aug 1, 2014Sumitomo Dainippon
NCT01516424Phase 3Feb 1, 2012Jiao Tong University, Sumitomo
Showing 4 of 4 trials
Page 1 / 1

Organizations

Research & Development (4)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
SumitomoFor profit2222012
Sumitomo DainipponFor profit2212014
Jiao Tong UniversityAcademic/Hospital1012012
Peking UniversityAcademic/Hospital1012019
4 organizations
Page 1 / 1