Fig. 4: Oral exposure of AZ’6421 in enabling formulations.
From: Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC
a PK experiment using 0.5 mg/kg AZ’6421 in 95% SBE-β-CD (30% w/v) in purified water as i.v. leg and 1 mg/kg AZ’6421 in SF as p.o. leg. b Plasma exposure of AZ’6421 at 100 mg/kg in a range of enabling formulations (EF) in mice. c Dose linearity investigation of EF3 showing 28% relative bioavailability at a 100 mg/kg dose in mice. d Dose linearity investigation of EF5 showing 33% relative bioavailability at a 100 mg/kg dose in mice. e Dose normalised exposure (Cmax and AUC) of AZ’6421 in a range of enabling formulations. (*) AUC0-6 (data BLQ beyond 6 hours).
