Table 4.

Pharmacokinetic parameters of neratinib for patients with advanced solid tumors

Dose group, mgStudy day 1, mean ± SD (CV%) [n]
Study day 21, mean ± SD (CV%) [n]
Cmax, ng/mLtmax, ht1/2, hAUC0-24 hr ng·h/mLCmax, ng/mLAUCss, ng·h/mL
405.0 ± 2.2 (44) [3]4.0 (3.0, 5.0) [3]8.2 ± 5.3 (65) [2]43.1 ± 6.57(15) [2]5.8 ± 0.5 (8) [3]76.0 ± NC (NC) [1]
8017.3 ± 7.3 (42) [4]6.5 (2.0, 8.0) [4]14.7 ± 2.7 (18) [2]230 ± 105 (46) [4]32.9 ± 5.3 (16) [4]435 ± 155 (36) [4]
12047.6 ± 33.9 (71) [4]5.0 (3.0, 8.0) [4]16.3 ± 2.4 (15) [3]464 ± 295 (64) [4]52.1 ± 23.1 (44) [4]807 ± 239 (30) [4]
18065.9 ± 34.7 (53) [6]3.0 (2.0, 5.0) [6]16.0 ± 4.6 (29) [6]734 ± 291(40) [6]70.1 ± 33.7 (48) [6]975 ± 633 (65) [6]
24075.9 ± 12.9 (17) [3]4.0 (4.0, 5.0) [3]13.9 ± 1.1 (8) [3]823 ± 291(35) [3]73.5 ± 27.0 (37) [3]939 ± 316 (34) [3]
320118 ± 47.6 (40) [7]4.0 (2.0, 8.0) [7]15.1 ± 2.7 (18) [7]1582 ± 800 (51) [7]119 ± 61.3 (51) [5]1,644 ± 1,014(62) [5]
MTD (320)83.5 ± 51.6 (62) [39]4.0 (2.0, 8.0) [39]14.9 ± 4.1 (27) [38]994 ± 580 (58) [38]85.8 ± 44.8 (52) [31]1,280 ± 739 (58) [31]
40076.5 ± 39.5 (52) [6]5.5 (2.0, 8.0) [6]16.9 ± 4.2 (25) [6]1116 ± 582(52) [6]105 ± 45 (43) [2]1,704 ± 340 (20) [2]
  • Abbreviations: NC, not calculated; CV%, coefficient of variation.