Prodrugs for colon-restricted delivery: Design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors
Fig 6
Unbound concentration (ng/mL for plasma; ng/g for colon) of 1 at 3 and 11 h after PO dosing of a 30 mg/kg dose equivalent of prodrugs 2 and 7–14.
Compounds 2, 12, and 13 were dosed as mixtures of isomers (ratio of a:b = 82:18 for 2; 43:57 for 12; and 70:30 for 13). Cmpd 2 is reported as the mean of two separate studies. *Dose = 35 mg/kg, ^Dose = 20 mg/kg. Cellular EC50 corrected for binding in 10% FBS (22 ng/mL) is represented by the horizontal blue line. Tmax = plasma Tmax.