Blonanserin

Blonanserin
Clinical data

Trade names	Lonasen
Routes of administration	Oral
ATC code	none
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	55%.
Metabolism	CYP3A4
Biological half-life	12 h
Excretion	59% (urine), 30% (faeces)
Identifiers
IUPAC name 2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
CAS Number	132810-10-7
PubChem CID	125564
ChemSpider	111697
UNII	AQ316B4F8C
KEGG	D01176
ChEMBL	CHEMBL178803
ECHA InfoCard	100.211.656
Chemical and physical data
Formula	C₂₃H₃₀FN₃
Molar mass	367.50 g/mol
3D model (Jmol)	Interactive image
SMILES Fc1ccc(cc1)c2cc(nc3c2CCCCCC3)N4CCN(CC)CC4

Blonanserin (Lonasen) is a relatively new atypical antipsychotic (approved by PMDA in January 2008) 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.

The use of atypical antipsychotics as a first-line treatment for schizophrenia is controversial. The National Institute of Mental Health’s CATIE trials suggest that atypical antipsychotics are not significantly more effective against negative symptoms of schizophrenia than typical antipsychotics. Blonanserin contradicts these findings by demonstrating more efficacy in treating negative symptoms than the related typical antipsychotic haloperidol. Despite its suggested advantages, blonanserin does not meet the criteria for Lipinski’s rule, indicating it may not have effective pharmacological or biological activity and predicting that it would not be successful in the clinical trial phases of drug development. Blonanserin is approved for treatment of schizophrenia in Japan and South Korea. Blonanserin is not approved for the same use by the FDA.

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