TABLE 5

Correlation of PK parametersa in human volunteersb and IC50s

CompoundCmax (μg/ml)tmax (h)t1/2 (h)AUC (μg ml−1 h)Cmax/IC50c ratioAUC/IC50c ratio
R-PZQ0.162.671.550.87843.5
S-PZQ0.522.551.462.990.090.5
R-trans-4-OH-PZQ1.312.721.708.800.312.1
S-trans-4-OH-PZQ0.783.051.915.60NAdNAd
  • a tmax, time to Cmax; t1/2, half-life; AUC, area under the curve.

  • b Adapted from reference 16 (oral dose of 23.3 mg/kg).

  • c IC50s from adults after 72 h.

  • d NA, not applicable (no IC50).