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1 INNClassRoute (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 complexTargets from DrugCentral Links
LORLATINIB

LORLATINIB


ATC L01ED05

ANTINEOPLASTIC
KINASE INHIBITOR
TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
ACTIVITY AGAINST ALK AND ROS1 AS WELL AS TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, AND ACK

ORAL

Cmax 1.42 MICROMOLAR

Tmax 1.2 HOUR

F 81 PERCENT

VD 305 LITER

PPB 66 PERCENT

Cl 11 LITER / HOUR

HT 24 HOUR

SOLUBILITY 0.17 MILLIGRAM PER MILLILITER

ALK
ROS1

PDB 5A9U (HUMAN ANAPLASTIC LYMPHOMA KINASE)

LIGAND CODE = 5P8 (link to the list of PDB complexes)

Download experimental 3D coordinates of 5P8 with added hydrogens

ALK tyrosine kinase receptor UNIPROT Q9UM73 ALK -- Proto-oncogene tyrosine-protein kinase ROS UNIPROT P08922 ROS1

more at DrugCentral

EMA

ANSM (in French)

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SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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