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| 1 | INN | Class | Route (list) | PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that the equation t1/2 = VD / Cl * 0.693 was used | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| APROCITENTAN (is an active metabolite)
| APROCITENTAN | CARDIOVASCULAR | ORAL | Cmax 2.38 MICROMOLAR Tmax 4.5 HOUR VD 20 LITER PPB 99 PERCENT Cl 0.3 LITER / HOUR HT 41 HOUR SOLUBILITY INSOLUBLE IN WATER | ENDOTHELIN RECEPTOR ET-1 | - more at DrugCentral | EMA | |||
| 2 | INN | Class | Route (list) | PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that the equation t1/2 = VD / Cl * 0.693 was used | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| MACITENTAN (has an active metabolite)
| MACITENTAN | CARDIOVASCULAR | ORAL | VD 50 LITER PPB 99 PERCENT Cl 2.1 LITER / HOUR (EQN) HT 16 HOUR SOLUBILITY NOT SOLUBLE IN WATER | 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 | Endothelin-1 receptor UNIPROT P25101 EDNRA -- Endothelin B receptor UNIPROT P24530 EDNRB more at DrugCentral | EMA | |||
