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 ATC L01XE56
ANTINEOPLASTIC A TROPOMYOSIN RECEPTOR TYROSINE KINASES INHIBITOR (TRK) TRKA, TRKB, AND TRKC PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ROS1 INHIBITOR ANAPLASTIC LYMPHOMA KINASE (ALK) INHIBITOR ALSO INHIBITS JAK2 AND TNK2 TREATMENT OF METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
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 inhibitor P04629 (NTRK1_HUMAN) ANSM (in French) Dailymed Drugs.com
SIDER side effects
Chemical Probes Portal
ChEMBL BindingDB DrugBank
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 ATC L01XE56
ANTINEOPLASTIC A TROPOMYOSIN RECEPTOR TYROSINE KINASES INHIBITOR (TRK) TRKA, TRKB, AND TRKC PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ROS1 INHIBITOR ANAPLASTIC LYMPHOMA KINASE (ALK) INHIBITOR ALSO INHIBITS JAK2 AND TNK2 TREATMENT OF METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
- 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 inhibitor P04629 (NTRK1_HUMAN) ANSM (in French) Dailymed Drugs.com
SIDER side effects
Chemical Probes Portal
ChEMBL BindingDB DrugBank