e-Drug3D
880
BOSENTAN
INN
BOSENTAN
cas 147536-97-8
CLASS
CARDIOVASCULAR
ENDOTHELIN RECEPTOR (ET-A AND ET-B) ANTAGONIST
ANTIHYPERTENSIVE
TREATMENT OF PULMONARY ARTERIAL HYPERTENSION
ROUTE (list)
ORAL
ATC code
C02KX01
PK parameters
F 50 PERCENT
Tmax 4 HOUR
VD 18 LITER
Cl 4 LITER / HOUR
PPB 98 PERCENT
t1/2 5 HOUR
Solubility
POORLY SOLUBLE IN WATER
TARGET ENDOTHELIN RECEPTOR
ENDOTHELIN-1 RECEPTOR
ENDOTHELIN-1 RECEPTOR
PDB
5XPR (HUMAN ENDOTHELIN RECEPTOR TYPE-B IN COMPLEX WITH ANTAGONIST BOSENTAN)
Ligand code = K86 (link to the list of PDB complexes)
Download experimental 3D coordinates of K86 with added hydrogens
Endothelin-1 receptor UNIPROT P25101 EDNRA
Endothelin B receptor UNIPROT P24530 EDNRB
Formula:
C27H29N5O6S
Calculated chemical properties:
MW 551.62
NB_atoms 39
XLogP 4.20
PSA 131.052
NB_HD 2
NB_HA 11
fsp3 0.26
Lipinski(0=no;1=yes) 0
NB_atoms 39
XLogP 4.20
PSA 131.052
NB_HD 2
NB_HA 11
fsp3 0.26
Lipinski(0=no;1=yes) 0
FDA
NDA 021290 (label) INN (BOSENTAN) TRACLEER (ACTELION) APPROVAL= AP YEAR= 2001
NDA 209279 (label) INN (BOSENTAN) TRACLEER (ACTELION) APPROVAL= AP YEAR= 2017
NDA 205699 (pdf not found) INN (BOSENTAN) BOSENTAN (PH HEALTH) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206002 (pdf not found) INN (BOSENTAN) BOSENTAN (ALVOGEN PINE BROOK) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206987 (pdf not found) INN (BOSENTAN) BOSENTAN (NATCO PHARMA LTD) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 207110 (pdf not found) INN (BOSENTAN) BOSENTAN (WATSON LABS INC) APPROVAL= AP YEAR= 2019
NDA 207760 (pdf not found) INN (BOSENTAN) BOSENTAN (ZYDUS PHARMS) APPROVAL= AP YEAR= 2019
NDA 208695 (pdf not found) INN (BOSENTAN) BOSENTAN (HIKMA) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 209324 (pdf not found) INN (BOSENTAN) BOSENTAN (SUN PHARM) APPROVAL= AP YEAR= 2019
NDA 209742 (pdf not found) INN (BOSENTAN) BOSENTAN (AMNEAL PHARMS CO) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 205173 (pdf not found) INN (BOSENTAN) BOSENTAN (MYLAN) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 210342 (pdf not found) INN (BOSENTAN) BOSENTAN (CHARTWELL MOLECULAR) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 211461 (pdf not found) INN (BOSENTAN) BOSENTAN (ALEMBIC) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 213154 (pdf not found) INN (BOSENTAN) BOSENTAN (NATCO PHARMA LTD) APPROVAL= AP YEAR= 2025
NDA 213981 (pdf not found) INN (BOSENTAN) BOSENTAN (ZYDUS PHARMS USA INC) APPROVAL= TA YEAR= 2025
NDA 021290 (label) INN (BOSENTAN) TRACLEER (ACTELION) APPROVAL= AP YEAR= 2001
NDA 209279 (label) INN (BOSENTAN) TRACLEER (ACTELION) APPROVAL= AP YEAR= 2017
NDA 205699 (pdf not found) INN (BOSENTAN) BOSENTAN (PH HEALTH) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206002 (pdf not found) INN (BOSENTAN) BOSENTAN (ALVOGEN PINE BROOK) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206987 (pdf not found) INN (BOSENTAN) BOSENTAN (NATCO PHARMA LTD) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 207110 (pdf not found) INN (BOSENTAN) BOSENTAN (WATSON LABS INC) APPROVAL= AP YEAR= 2019
NDA 207760 (pdf not found) INN (BOSENTAN) BOSENTAN (ZYDUS PHARMS) APPROVAL= AP YEAR= 2019
NDA 208695 (pdf not found) INN (BOSENTAN) BOSENTAN (HIKMA) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 209324 (pdf not found) INN (BOSENTAN) BOSENTAN (SUN PHARM) APPROVAL= AP YEAR= 2019
NDA 209742 (pdf not found) INN (BOSENTAN) BOSENTAN (AMNEAL PHARMS CO) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 205173 (pdf not found) INN (BOSENTAN) BOSENTAN (MYLAN) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 210342 (pdf not found) INN (BOSENTAN) BOSENTAN (CHARTWELL MOLECULAR) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 211461 (pdf not found) INN (BOSENTAN) BOSENTAN (ALEMBIC) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 213154 (pdf not found) INN (BOSENTAN) BOSENTAN (NATCO PHARMA LTD) APPROVAL= AP YEAR= 2025
NDA 213981 (pdf not found) INN (BOSENTAN) BOSENTAN (ZYDUS PHARMS USA INC) APPROVAL= TA YEAR= 2025