TABLE 2

Pharmacokinetics of cinacalcet and total plasma radioactivity in monkeys and humans after a single oral dose

Values are mean ± S.D.




Dose

Tmax

Cmax

t1/2

AUC0-t
mg/kg h ng/ml h ng · h/ml
Plasma cinacalcet
Monkey (3) 10 4.67 ± 1.15 23.9 ± 10.8 6.59 ± 3.20 209.8 ± 143.4
Monkey (3) 100 13.3 ± 9.24 101.3 ± 29.5 13.0 ± 2.42 2611.1 ± 701.3
Human (5) ∼1a 3.00 ± 0 10.6 ± 2.78 34.3 ± 8.61 116 ± 29.7
Human (5)b ∼1a 2.90 ± 0.89 12.2 ± 5.55 41.0 ± 16.54 129 ± 52.4
h μg Eq/g or ml h μg Eq · h/g
Total plasma radioactivity
Monkey (3) 10 4.67 ± 1.15 8.65 ± 1.94 65.5 ± 19.9 135 ± 20.2
Monkey (3) 100 9.33 ± 2.31 49.5 ± 4.19 65.2 ± 1.93 1442 ± 470
Human (5) ∼1a 2.80 ± 0.44 2.85 ± 0.22 15.7 ± 2.45 54.0 ± 14.87c
Human (5)b
∼1a
2.60 ± 0.54
3.03 ± 0.33
15.8 ± 3.13
45.3 ± 10.48c
  • a 75 mg of total dose.

  • b Smokers.

  • c The corresponding values for blood were 24.6 ± 7.08 and 19.6 ± 5.19 for nonsmokers and smokers, respectively.