TABLE 1

Mean (CV%) plasma pharmacokinetic parameters of radioactivity, ozanimod, and its metabolites after single oral dose of 1 mg [14C]ozanimod HCl

PK Parameter (Unit)RadioactivityOzanimodCC112273RP101988RP101075RP101124
Cmax (pg/ml)1560a (7.3%)185 (22.0%)337 (10.2%)240 (21.9%)18.9 (18.1%)69.8 (27.4%)
Tmax (h)b10.00 (8.00–24.00)8.00 (6.00–12.18)18 (12–36)8.00 (6.00–12.18)8.00 (6.00–12.18)24.00 (24.00–36.02)
AUClast (pg.h/ml)116000c (11.8%)5400 (29.8%)31000 (8.20%)4810 (30.2%)376 (30.3%)3480 (27.3%)
AUC (pg.h/ml)NR5690 (28.5%)NR5630 (28.5%)NR4220 (21.5%), n = 5
t1/2 (h)98.61 (13.3%)20.78 (15.4%)195 (52.8%), n = 415.29 (17.4%)22.89 (48.2%) n = 427.79 (18.6%) n = 5
CL/F (l/h)NA192 (36.9%)NANANANA
Vz/F (l)NA5590 (26.6%)NANANANA
  • CL/F, apparent total clearance; NA, not applicable; NR, not reportable; Vz/F, apparent volume of distribution.

  • a Picogram equivalent per milliliter.

  • b Median (range).

  • c Picogram equivalent hour per milliliter.