. 2017 Oct 23;57(3):315–333. doi: 10.1007/s40262-017-0608-3

Table 10.

Projected steady-state plasma and brain tramiprosate exposures following oral administration of ALZ-801 tablet 265 mg twice-daily in humans

Parameters	Tramiprosate exposure
Plasma AUC₁₂	34.8 μΜ h
Projected brain AUC₁₂	13.9 μM h (¹⁴C method)^a
Projected brain average concentration (C _ss,av)	550 nM (¹⁴C method)^a
Projected multiple excess of brain drug concentration versus soluble Aβ	> 5000- to 15,000-fold

^aBased on 19% single dose and approximately 40% steady-state brain penetration based on ¹⁴C method. Multiple excess of drug exposure analyses based on CSF soluble Aβ concentrations of 0.035–0.1 nM [23, 24, 28], and comparable levels in brain parenchyma as per published human microdialysis data [21, 22]

AUC ₁₂ area under the concentration–time curve from time zero to 12 h, Css,av average concentration at steady state