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Table 3 Pharmacokinetic parameters (mean ± SD) of laquinimod in MS patients following repeated daily administration for 21 days

From: Safety and in vivo immune assessment of escalating doses of oral laquinimod in patients with RRMS

Dose (mg)

n

t max a (h)

C max (ng/mL)

C min (ng/mL)

AUC0–24 (ng h/mL)

Dose -normalized

C max

AUC0–24h

0.9

10

0.99 (0.25–2.00)

639.6 ± 114.9

469.5 ± 103.4

12,245.8 ± 2075.4

710.6 ± 127.6

13,606.5 ± 2306.0

1.2

12

0.75 (0.25–4.00)

779.2 ± 115.7

565.7 ± 121.0

15,075.2 ± 2757.6

649.4 ± 96.4

12,562.7 ± 2298.0

1.5

12

1.00 (0.50–24.00)

1207.8 ± 210.8

904.0 ± 189.5

22,974.0 ± 3756.6

805.2 ± 140.6

15,316.0 ± 2504.4

1.8

11

0.50 (0.25–3.00)

1449.4 ± 325.4

1076.7 ± 274.3

28,042.7 ± 6495.5

805.2 ± 180.8

15,579.3 ± 3608.6

2.1

11

2.00 (0.50–6.00)

1712.1 ± 385.8

1310.5 ± 356.0

33,741.2 ± 8133.4

815.3 ± 183.7

16,067.2 ± 3873.1

2.4

10

0.50 (0.50–2.00)

1892.3 ± 526.3

1389.3 ± 512.9

35,470.0 ± 11,100.2

788.5 ± 219.3

14,779.2 ± 4625.1

2.7

10

1.00 (0.5–2.00)

1826.2 ± 313.4

1364.5 ± 186.7

35,274.5 ± 5973.0

676.4 ± 116.1

13,064.6 ± 2212.2

  1. AUC 0–24 area under the plasma concentration-time curve from 0 to 24 h postdose, C max maximum plasma concentration, C min minimum plasma concentration, t max time to maximum plasma concentration
  2. aMedian (range) is provided for t max