Pimavanserin

Pimavanserin

Systematic (IUPAC) name
N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide
Clinical data
Legal status	?
Routes	Oral
Pharmacokinetic data
Protein binding	94-97%[1]
Half-life	54-56 hours[1]
Identifiers
CAS number	Y 706782-28-7 (tartrate)
ATC code	None
PubChem
ChemSpider	N
UNII	Y
Chemical data
Formula	C25H34FN3O2
Mol. mass	427.553 g/mol
SMILES CC(C)COc3ccc(cc3)CNC(=O)N(C(CC2)CCN2C)Cc(cc1)ccc1F
InChI InChI=1S/C25H34FN3O2/c1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21/h4-11,19,23H,12-18H2,1-3H3,(H,27,30) N Key:RKEWSXXUOLRFBX-UHFFFAOYSA-N N
N

Pimavanserin (ACP-103), marketed under the trade name Nuplazid, is a drug developed by Acadia Pharmaceuticals which acts as an inverse agonist on the serotonin receptor subtype 5-HT_2A, with 40x selectivity over 5-HT_2C, and no significant affinity or activity at 5-HT_2B or dopamine receptors.^[1] As of September 3 2009, pimavanserin has not met expectations for Phase III clinical trials for the treatment of Parkinson's disease psychosis,^[2] and is in Phase II trials for adjunctive treatment of schizophrenia alongside an antipsychotic medication.^[3] It is expected to improve the effectiveness and side effect profile of antipsychotics.^[4][5][6] The results of a clinical trial examining the efficacy, tolerability and safety of adjunctive pimavanserin to risperidone and haloperidol were published in November 2012 and the results showed that pimavanserin potentiated the antipsychotic effects of subtherapeutic doses of risperidone and improve the tolerability of haloperidol treatment by reducing the incidence of extrapyramidal symptoms.^[7]

On September 2, 2014, the United States Food and Drug administration granted Breakthrough Therapy status to Acadia's New Drug Application for pimavanserin.[1]

References