Blonanserin

Blonanserin was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 25, 2008. It was developed and marketed as Lonasen® by Dainippon Sumitomo Pharma in JP.

Blonanserin acts as a mixed 5-HT2A (Ki=0.812 nM) and D2 receptor (Ki=0.142 nM) antagonist and also exerts some blockade of α1-adrenergic receptors (Ki = 26.7 nM). It lacks significant affinity for numerous other sites including the 5-HT1A, 5-HT3, D1, α2-adrenergic, β-adrenergic, H1, and mACh receptors and the monoamine transporters, though it does possess low affinity for the sigma receptor (IC50 = 286 nM). It is indicated for the treatment of schizophrenia.

Lonasen® is available as tablet and powder for oral use, containing 2 mg, 4 mg or 8 mg for tablet or 2% for powder of free Blonanserin. In general, the recommended dose for adults is 4 mg at a time, twice a day after meals. Then, increase the dose in incremental steps.

Index：

General Information

Update Date：2016-05-16

Drug Name：
Blonanserin
Research Code：
AD-5423
Trade Name：
Lonasen®
MOA：
Serotonin receptor antagonist; Dopamine receptor antagonist
Indication：
Schizophrenia
Status：
Approved
Company：
Dainippon Sumitomo (Originator) , Dainippon Sumitomo
Sales：
$104.8 Million (Y2015);
$104.7 Million (Y2014);
$125.7 Million (Y2013);
$134.1 Million (Y2012);
$122.8 Million (Y2011);
ATC Code：
N05
Approved Countries or Area

Update Date：2015-07-29

Approval Date Approval Type Trade Name Indication Dosage Form Strength Company Review Classification
2009-12-02 New strength Lonasen Schizophrenia Tablet 8 mg Dainippon Sumitomo
2008-01-25 Marketing approval Lonasen Schizophrenia Powder 2% Dainippon Sumitomo
2008-01-25 Marketing approval Lonasen Schizophrenia Tablet 2 mg/4 mg Dainippon Sumitomo
More
Chemical Structure

Update Date：2015-08-27

Molecular Weight 367.5
Formula C23H30FN3
CAS No. 132810-10-7 (Blonanserin);
Chemical Name 2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
Blonanserin （Free Acid/Base）Parameters：
MW HD HA FRB* PSA* cLogP*
367.5 0 3 3 19.4 5.779±0.592
*：Calculated by ACD/Labs software V11.02.
Related Patents

Update Date：2015-08-31

No. Major Technical Classification Publication No. Patent No. Legal Status Filling Date Estimated Expiry Date
1 Formulation CN101500570A CN101500570B Granted 2007/6/7 2027/6/7
2 Formulation CN101541311A CN101541311B Granted/abandoned 2007/10/25 2013/10/25
3 Formulation CN102458406A Withdrawn 2010/6/16
4 Formulation CN103347522A Examination 2012/2/1
5 Formulation CN103338771A Examination 2012/2/1
More
Synthesis & Impurities

Update Date：2015-09-07


1. US5021421A.

2. JP2013216655A.

 

 

 

 

Impurity database is being updated！