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. Author manuscript; available in PMC: 2014 Jan 21.
Published in final edited form as: J Pharmacokinet Pharmacodyn. 2013 Jan 12;40(2):157–176. doi: 10.1007/s10928-012-9295-8

Table 8.

Single dose lapatinib observed and predicted human half-life (t1/2), maximum concentration (Cmax) and time of maximum concentration (Tmax)

Dose (mg) Observed t1/2 (h) Predicted t1/2 (h) T1/2 PE%c Observed Cmax (nM) Predicted Cmax (nM) Cmax PE%c Observed Tmax (h) Predicted Tmax (h) Tmax PE%c Reference
50 6.0a (4.8–7.5) 10.0 66.7 124 (88–177)d 66 −46.7 3.0 (2.0–6.0)f 3.75 25.0 [4]
100 6.3a (5.6–7.0) 10.0 58.7 213 (148–308)d 132 −38.1 4.0 (2.5–5.9)f 3.75 −6.3 [4]
100 9.6a (8.5–10.7) 10.0 4.2 198 (174–224)e 132 −33.3 4.0 (2.5–8.0)f 3.75 −6.3 [14]
175 8.2a (6.7–9.9) 10.0 22.0 380 (241–599)d 231 −39.3 3.0 (2.0–4.0)f 3.75 25.0 [4]
250 8.8a (6.6–11.7) 10.0 13.6 546 (330–902)d 329 −39.7 4.0 (3.0–6.0)f 3.75 −6.3 [4]
250 10.2a (9.24–11.3) 10.0 −2.0 449 (360–563)e 329 −26.8 4.0 (2.5–6.0)f 3.75 −6.3 [14]
900 12.9b (10.1–18.3) 10.0 −22.5 1,740 (1,194–2,533)d 1,185 −31.9 4.0 (2.0–6.0)g 3.75 −6.3 [13]
1,200 11.5b (10.1–19.5) 10.0 −13.0 1,767 (816–3,833)d 1,581 −10.5 3.5 (2.1–6.0)g 3.75 7.1 [13]
1,600 13.9b (9.6–18.0) 10.0 −28.1 2,647 (1,793–3,903)d 2,107 −20.4 4.0 (2.0–8.0)g 3.75 −6.3 [13]
1,800 15.7b (11.0–133.1) 10.0 −36.3 2,112 (800–5,579)d 2,371 12.3 3.9 (3.0–8.0)g 3.75 −3.8 [13]
a

t1/2 is the terminal half-life geometric mean (95 % confidence interval)

b

t1/2 is the terminal half-life median (95 % confidence interval)

c

PE% is the prediction error

d

Is the geometric mean (95 % confidence interval) of Cmax

e

Is the geometric mean (range) of Cmax

f

Is the median (range) of Tmax

g

Is the median (95 % confidence interval) of Tmax