e-Drug3D

1437

AMBRISENTAN


INN
AMBRISENTAN

cas 177036-94-1
CLASS

CARDIOVASCULAR
ANTIHYPERTENSIVE
ENDOTHELIN RECEPTOR ANTAGONIST
TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH)
AMBRISENTAN IS A SUBSTRATE OF P-GP

ROUTE (list)

ORAL

ATC code

C02KX02
C02KX52

PK parameters

Tmax 1.5 HOUR
Cl 1.71 LITER / HOUR
PPB 99 PERCENT
t1/2 9 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER


Target

TARGET ENDOTHELIN TYPE-A RECEPTOR (ETA) (KI = 0.011 NANOMOLAR)

PDB
8XVK (CRYO-EM STRUCTURE OF ETAR BOUND WITH AMBRISENTAN)

Ligand code = A1D5J (link to the list of PDB complexes)

Download experimental 3D coordinates of A1D5J with added hydrogens

DrugCentral

Endothelin-1 receptor UNIPROT P25101 EDNRA

Download SDF file Benzenepropanoic acid, .alpha.-[(4,6-dimethyl-2-pyrimidinyl)oxy]-.beta.-methoxy-.beta.-phenyl-, (.alpha.S)-

Formula:
C22H22N2O4

Calculated chemical properties:

MW 377.41
NB_atoms 28
XLogP 2.18
PSA 64.513
NB_HD 0
NB_HA 6
fsp3 0.23
Lipinski(0=no;1=yes) 1

FDA
NDA 022081 (label) INN (AMBRISENTAN) LETAIRIS (GILEAD) APPROVAL= AP YEAR= 2007
NDA 208252 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (WATSON LABS INC) APPROVAL= AP YEAR= 2019
NDA 208354 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (SIGMAPHARM LABS LLC) APPROVAL= AP YEAR= 2019
NDA 208441 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (MYLAN) APPROVAL= AP YEAR= 2019
NDA 209509 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (PH HEALTH) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 210058 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (ZYDUS PHARMS) APPROVAL= AP YEAR= 2019
NDA 210715 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (CIPLA) APPROVAL= AP YEAR= 2019
NDA 210784 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (SUN PHARM) APPROVAL= AP YEAR= 2019
NDA 210701 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (APOTEX) APPROVAL= AP YEAR= 2022
NDA 216531 (pdf not found) INN (AMBRISENTAN) AMBRISENTAN (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2022

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL