e-Drug3D

1801

ROLAPITANT

INN
ROLAPITANT

cas 552292-08-7

CLASS

NERVOUS SYSTEM
TREATMENT OF NAUSEA AND VOMITING INDUCED BY CANCER CHEMOTHERAPY
SUBSTANCE P/NEUROKININ 1 (NK1) RECEPTOR ANTAGONIST

ROUTE (list)

ORAL INTRAVENOUS

ATC code

A04AD14

PK parameters

Tmax 4 HOUR
Cmax 1.9 MICROMOLAR
VD 460 LITER
Cl 0.96 LITER / HOUR
PPB 99.8 PERCENT
t1/2 176 HOUR

Target

TARGET P/NEUROKININ-1 (NK1) RECEPTOR

DrugCentral

Substance-P receptor UNIPROT P25103 TACR1

Download SDF file

1,7-Diazaspiro[4.5]decan-2-one, 8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-, (5S,8S)-

Formula:
C25H26F6N2O2

Calculated chemical properties:

MW 500.48
NB_atoms 35
XLogP 5.73
PSA 50.86
NB_HD 2
NB_HA 4
fsp3 0.48
Lipinski(0=no;1=yes) 0

FDA
NDA 206500 (label) INN (ROLAPITANT HYDROCHLORIDE) VARUBI (TERSERA) APPROVAL= AP YEAR= 2015 NEWMOLECULARENTITY
NDA 208399 (label) INN (ROLAPITANT HYDROCHLORIDE) VARUBI (TERSERA) APPROVAL= AP YEAR= 2017 DISCONTINUED