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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
AVAPRITINIB

AVAPRITINIB


ATC L01EX18

ANTINEOPLASTIC
A TYROSINE KINASE INHIBITOR PDGFRA AND PDGFRA D842 MUTANTS AND KIT
TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST)

ORAL

Cmax 1.63 MICROMOLAR

Tmax 3 HOUR

VD 1200 LITER

PPB 98.8 PERCENT

Cl 19.5 LITER / HOUR

HT 44.5 HOUR

SOLUBILITY LOWER THAN 0.001 MILLIGRAM PER MILLILITER

PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA)
MAST STEM CELL GROWTH FACTOR RECEPTOR (KIT)

PDB 8PQG (C-KIT T670I MUTATED KINASE DOMAIN IN COMPLEX WITH AVAPRITINIB)

LIGAND CODE = 9JI (link to the list of PDB complexes)

Download experimental 3D coordinates of 9JI with added hydrogens

Mast,stem cell growth factor receptor Kit UNIPROT P10721 KIT -- Platelet-derived growth factor receptor alpha UNIPROT P16234 PDGFRA

more at DrugCentral

EMA

ANSM (in French)

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Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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