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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 value was calculated using VD=(Cl*t1/2)/0.693) | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| ENTRECTINIB (has an active metabolite)
| ENTRECTINIB | ANTINEOPLASTIC | ORAL | Cmax 3.13 MICROMOLAR Tmax 5 HOUR VD 551 LITER PPB 99 PERCENT Cl 19.6 LITER / HOUR HT 20 HOUR | TROPOMYOSIN RECEPTOR TYROSINE KINASES INHIBITOR (TRK) TRKA TRKB AND TRKC PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ROS1 ANAPLASTIC LYMPHOMA KINASE (ALK) PDB 5FTO (CRYSTAL STRUCTURE OF THE ALK KINASE DOMAIN IN COMPLEX WITH ENTRECTINIB) LIGAND CODE = YMX (link to the list of PDB complexes) Download experimental 3D coordinates of YMX with added hydrogens | High affinity nerve growth factor receptor UNIPROT P04629 NTRK1 -- ALK tyrosine kinase receptor UNIPROT Q9UM73 ALK 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 value was calculated using VD=(Cl*t1/2)/0.693) | Primary Target and PDB code of Protein-Drug complex | Targets from DrugCentral | Links | |||
| M ENTRECTINIB (is an active metabolite)
| ENTRECTINIB | ANTINEOPLASTIC | - | Cmax 1.25 MICROMOLAR VD 81.1 LITER PPB 99 PERCENT Cl 52.4 LITER / HOUR HT 40 HOUR | TROPOMYOSIN RECEPTOR TYROSINE KINASES INHIBITOR (TRK) TRKA TRKB AND TRKC PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ROS1 ANAPLASTIC LYMPHOMA KINASE (ALK) | High affinity nerve growth factor receptor UNIPROT P04629 NTRK1 -- ALK tyrosine kinase receptor UNIPROT Q9UM73 ALK more at DrugCentral | EMA | |||
