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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 the equation t1/2 = VD / Cl * 0.693 was usedPrimary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
NIROGACESTAT

NIROGACESTAT


ATC L01XX81

ANTINEOPLASTIC
GAMMA SECRETASE INHIBITOR
TREATMENT OF PROGRESSING DESMOID TUMORS
BLOCKS PROTEOLYTIC ACTIVATION OF THE NOTCH RECEPTOR

ORAL

Cmax 1.03 MICROMOLAR

Tmax 1.5 HOUR

F 19 PERCENT

VD 1430 LITER

PPB 99.6 PERCENT

Cl 45 LITER / HOUR

HT 23 HOUR

SOLUBILITY SIGNIFICANTLY DECREASES AT PH HIGHER THAN 6.0

GAMMA SECRETASE

PDB 8KCT (CRYO-EM STRUCTURE OF HUMAN GAMMA-SECRETASE IN COMPLEX WITH NIROGACESTAT)

LIGAND CODE = O6U (link to the list of PDB complexes)

Download experimental 3D coordinates of O6U with added hydrogens

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more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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