e-Drug3D

1615

MACITENTAN

INN
MACITENTAN

cas 441798-33-0

CLASS

CARDIOVASCULAR
ANTIHYPERTENSIVE
PULMONARY ARTERIAL HYPERTENSION (PAH)
ENDOTHELIN RECEPTOR ANTAGONIST ET-1
PREVENTS THE BINDING OF ET-1 TO ITS RECEPTORS ETA AND ETB

ROUTE (list)

ORAL

ATC code

C02KX04
C02KX54

PK parameters

VD 50 LITER
Cl 2.1 LITER / HOUR (EQN)
PPB 99 PERCENT
t1/2 16 HOUR

Solubility

NOT SOLUBLE IN WATER

Target

TARGET ENDOTHELIN RECEPTOR ET-1

PDB
8XVJ (CRYO-EM STRUCTURE OF ETAR BOUND WITH MACITENTAN)

Ligand code = A1D5I (link to the list of PDB complexes)

Download experimental 3D coordinates of A1D5I with added hydrogens

DrugCentral

Endothelin-1 receptor UNIPROT P25101 EDNRA

Endothelin B receptor UNIPROT P24530 EDNRB

Download SDF file

Sulfamide, N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl-

Formula:
C19H20Br2N6O4S

Calculated chemical properties:

MW 588.28
NB_atoms 32
XLogP 3.57
PSA 116.69
NB_HD 2
NB_HA 10
fsp3 0.26
Lipinski(0=no;1=yes) 0

FDA
NDA 204410 (label) INN (MACITENTAN) OPSUMIT (ACTELION) APPROVAL= AP YEAR= 2013
NDA 211123 (pdf not found) INN (MACITENTAN) MACITENTAN (SUN PHARM INDS) APPROVAL= TA YEAR= 2021
NDA 211224 (pdf not found) INN (MACITENTAN) MACITENTAN (ZYDUS LIFESCIENCES) APPROVAL= AP YEAR= 2021 DISCONTINUED
NDA 211198 (pdf not found) INN (MACITENTAN) MACITENTAN (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 214112 (pdf not found) INN (MACITENTAN) MACITENTAN (RHODES PHARMS) APPROVAL= TA YEAR= 2023
NDA 211195 (pdf not found) INN (MACITENTAN) MACITENTAN (APOTEX) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 211107 (pdf not found) INN (MACITENTAN) MACITENTAN (TORRENT) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 218490 (label) INN (MACITENTAN ; TADALAFIL) OPSYNVI (ACTELION) APPROVAL= AP YEAR= 2024
NDA 211136 (pdf not found) INN (MACITENTAN) MACITENTAN (MSN) APPROVAL= AP YEAR= 2025
NDA 211128 (pdf not found) INN (MACITENTAN) MACITENTAN (ALEMBIC) APPROVAL= AP YEAR= 2025