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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
ENASIDENIB

ENASIDENIB


ATC L01XX59

ANTINEOPLASTIC
TREATMENT OF ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
ISOCITRATE DEHYDROGENASE-2 (IDH2) INHIBITOR

ORAL

Cmax 27.4 MICROMOLAR

Tmax 4 HOUR

F 57 PERCENT

VD 55.8 LITER

PPB 98.5 PERCENT

Cl 0.74 LITER / HOUR

HT 137 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN WATER (LESS THAN 74 MCG/ML)

ISOCITRATE DEHYDROGENASE-2 (IDH2)

PDB 5I96 (CRYSTAL STRUCTURE OF HUMAN MITOCHONDRIAL ISOCITRATE DEHYDROGENASE (IDH2) R140Q MUTANT HOMODIMER IN COMPLEX WITH AG-221 (ENASIDENIB) INHIBITOR.)

LIGAND CODE = 69Q (link to the list of PDB complexes)

Download experimental 3D coordinates of 69Q with added hydrogens

ENZYME IDHP_HUMAN INHIBITOR P48735EMA

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