e-Drug3D

1802

PIMAVANSERIN

INN
PIMAVANSERIN

cas 706779-91-1

CLASS

NERVOUS SYSTEM
ANTIPSYCHOTIC
TREATMENT OF HALLUCINATIONS AND DELUSIONS ASSOCIATED WITH PARKINSON'S DISEASE PSYCHOSIS
INVERSE AGONIST / ANTAGONIST SEROTONIN 5-HT2A (KI = 0.087 NANOMOLAR) AND 5-HT2C (KI = 0.44 NANOMOLAR)
SIGMA 1 RECEPTOR (KI = 120 NANOMOLAR)

ROUTE (list)

ORAL

ATC code

N05AX17

PK parameters

Tmax 6 HOUR
VD 2173 LITER
PPB 95 PERCENT
t1/2 57 HOUR

Solubility

SOLUBLE IN WATER

Target

TARGET 5-HT2A RECEPTOR
5-HT2C RECEPTOR

PDB
8ZMG (CRYSTAL STRUCTURE OF AN INVERSE AGONIST ANTIPSYCHOTIC DRUG PIMAVANSERIN-BOUND 5-HT2A)

Ligand code = A1L11 (link to the list of PDB complexes)

Download experimental 3D coordinates of A1L11 with added hydrogens

DrugCentral

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file

Urea, N-[(4-fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N'-[[4-(2-methylpropoxy)phenyl]methyl]-

Formula:
C25H34FN3O2

Calculated chemical properties:

MW 427.55
NB_atoms 31
XLogP 4.67
PSA 40.028
NB_HD 1
NB_HA 5
fsp3 0.48
Lipinski(0=no;1=yes) 1

FDA
NDA 207318 (label) INN (PIMAVANSERIN TARTRATE) NUPLAZID (ACADIA PHARMS INC) APPROVAL= AP YEAR= 2016 NEWMOLECULARENTITY
NDA 210793 (label) INN (PIMAVANSERIN TARTRATE) NUPLAZID (ACADIA PHARMS INC) APPROVAL= AP YEAR= 2018
NDA 214750 (pdf not found) INN (PIMAVANSERIN) PIMAVANSERIN (TEVA PHARMS USA) APPROVAL= TA YEAR= 2021
NDA 214782 (pdf not found) INN (PIMAVANSERIN) PIMAVANSERIN (AUROBINDO PHARMA LTD) APPROVAL= TA YEAR= 2022
NDA 214502 (pdf not found) INN (PIMAVANSERIN TARTRATE) PIMAVANSERIN (ZYDUS) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 214925 (pdf not found) INN (PIMAVANSERIN TARTRATE) PIMAVANSERIN (MSN) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 214493 (pdf not found) INN (PIMAVANSERIN TARTRATE) PIMAVANSERIN (ZYDUS) APPROVAL= AP YEAR= 2024 DISCONTINUED