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. 2022 Apr 5;15(4):450. doi: 10.3390/ph15040450

Table 5.

Metabolism of tracers based on clinically approved TKIs.

Tracer Animal Metabolism Method
[18F]Gefitinib Scid/Scid mice Intact tracer in plasma:
>97% at 120 min		 Radio-TLC [84]
[11C]Gefitinib ddY mice Intact tracer in plasma:
93 ± 3.3% at 30 min		 Radio-HPLC [85]
C3H/HeMsNrsf mice 86.2 ±1.5% at 60 min Radio-HPLC [83]
[11C]Erlotinib FVB/N wild-type mice
Abcb1a/b(-/-)Abcg2(-/-) mice		 Intact tracer in plasma:
80 ± 9% at 25 min
54 ± 12% at 25 min		 Radio-TLC [87]
BALB/c nude CAnN.Cg-Foxn1nu/Crl Intact tracer in plasma:
>95% at 25 min		 Radio-TLC [88]
NSCLC patients
 Intact tracer in plasma:
54 ± 2% at 60 min
43 ± 7% at 60 min		 Radio-HPLC [89]
Healthy human volunteers Intact tracer in plasma:
96.4 ± 1.3% at 40 min		 Solid-phase extraction [90]
[18F]Afatinib BALB/c mice Intact tracer in plasma:
83.3 ± 1.3% at 45 min		 Radio-HPLC [91]
NSCLC patients Intact tracer in plasma:
30% at 75 min		 Radio-HPLC [92]
[11C]Osimertinib Healthy human volunteers Intact tracer in plasma:
73 ± 8% at 30 min		 Radio-HPLC [93]