Table 2.

Exposure correlations in vitro/in vivo

Species, strainIn vitro IC50, nmTurnover half-life, minIn vivo IC20, nmIn vivo IC50, nm
Mouse, C57BL/62.7 ± 0.8247 (37–64)1.8 (1.5–2.1)4.7
Guinea pig, DH2.0 ± 1.353 (34–121)0.5 (0.3–0.7)1.8
Mouse, Tg257638 ± 11NANANA
  • In vitro IC50 in primary neurons incubated with AZ-4217 (±SD). Turnover half-life of Aβ40 in brain (kout, estimate and 95% planar confidence interval). No turnover half-life could be determined in Tg2576 due to a single time point effect readout. In vivo IC20 is expressed as free AZ-4217 concentration in brain (estimate and 95% planar confidence interval). Calculated in vivo IC50 for Aβ40 in brain as free AZ-4217 concentration in brain.