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. 2024 Jun 3;42(23):2747–2756. doi: 10.1200/JCO.24.00708

TABLE A7.

Pharmacokinetics Result of Osimertinib and AZD5104

Visit Category Statistic Osimertinib, nM AZ5104, nM
T790M– T790M+ All T790M– T790M+ All
C3D1 Free plasma concentration, nM No.
Geometric mean (CV%)
Range		 48
19.07 (84.46)
1.00-74.20		 1
29.20		 49
19.24 (83.70)
1.00-74.20		 48
3.03 (81.91)
0.22-20.22		 1
42.30		 49
3.04 (80.84)
0.22-20.22
CSF concentration, nM No.
Geometric mean (CV%)
Range		 36
4.55 (105.37)
0.46-47.70		 1
0.41		 37
4.58 (103.49)
0.46-47.70		 36
0.30 (97.81)
0.08-5.98		 1
0.41		 37
0.30 (96.19)
0.08-5.98
Free plasma metabolite-to-parent ratio No.
Ratio (CV%)
Range		 NA NA NA 48
0.16 (64.87)
0.09-0.55		 1
0.11		 49
0.16 (34.84)
0.09-0.55
CSF metabolite-to-parent ratio No.
Ratio (CV%)
Range		 NA NA NA 36
0.07 (52.85)
0.037-0.290		 1
0.07		 37
0.066 (52.02)
0.037-0.290
CSF-to-free plasma ratio No.
Ratio (CV%)
Range		 36
22.25 (63.34)
3.80-64.29		 1
20.44		 37
22.20 (62.47)
3.80-64.29		 36
10.21 (53.05)
3.29-29.57		 1
12.21		 37
10.25 (52.32)
3.29-29.57
C6D1 Free plasma concentration, nM No.
Geometric mean (CV%)
Range		 41
21.87 (59.73)
3.91-69.96		 NA 41
21.87 (59.73)
3.91-69.96		 41
3.34 (71.11)
0.64-19.51		 NA 41
3.34 (71.11)
0.64-19.51
CSF concentration, nM No.
Geometric mean (CV%)
Range		 30
4.81 (88.16)
0.84-21.70		 1
2.74		 31
4.72 (87.25)
0.84-21.70		 30
0.29 (72.75)
0.11-1.35		 1
0.22		 31
0.29 (71.58)
0.11-1.35
Free plasma metabolite-to-parent ratio No.
Ratio (CV%)
Range		 NA NA NA 41
0.15 (24.51)
0.09-0.30		 0 41
0.15 (24.51)
0.09-0.30
CSF metabolite-to-parent ratio No.
Ratio (CV%)
Range		 NA NA NA 30
0.06 (48.09)
0.03-0.19		 1
0.078		 31
0.06 (47.46)
0.03-0.19
CSF-to-free plasma ratio No.
Ratio (CV%)
Range		 30
22.12 (80.14)
4.73-82.29		 NA 30
22.12 (80.14)
4.73-82.29		 30
9.33 (59.57)
3.78-29.41		 NA 30
9.33 (59.57)
3.78-29.41

Abbreviations: CSF, cerebrospinal fluid; CV, Coefficient of Variation; NA, not available.