Article Figures & Data
Figures
- FIGURE 1.
Schematic of clinical study design.
- FIGURE 2.
(Left) Elacridar plasma concentrations in ng/mL for increasing oral dose of elacridar (0, 10, 25, and 50 mg/kg). (Right) Erlotinib brain-to-plasma ratios at same increasing doses of elacridar in WT mice (n = 4). Group of Abcb1a/b;Abcg2 knockout mice was used as positive controls (n = 5).
- FIGURE 3.
(Left) Representative summation images of Abcb1a/b;Abcg2 knockout mouse (bottom) and WT mouse (top). Arrows indicate brain. (Right) 11C-erlotinib percentage injected dose (%ID) per gram of brain determined ex vivo in knockout and WT mice. Erlotinib brain penetration was significantly higher in knockout mice (n = 2 per group).
- FIGURE 4.
11C-erlotinib PET before (top) and after (bottom) elacridar for subject 4.
- FIGURE 5.
11C-erlotinib whole-brain activity as SUV vs. time (in minutes) for patients before and after administration of elacridar (n = 5).
- FIGURE 6.
11C-erlotinib brain VT ratio vs. elacridar exposure (n = 5).
Tables
- TABLE 1
K1, K2, and VT of Brain 11C-Erlotinib Before and After Elacridar Administration in Cancer Patients (n = 5)
11C-erlotinib before elacridar 11C-erlotinib after elacridar Patient no. K1 K2 VT K1 K2 VT VT ratio 1 0.012 0.030 0.395 0.011 0.036 0.312 0.790 2 0.015 0.090 0.167 0.013 0.066 0.198 1.186 3 —* —* —* 0.014 0.080 0.179 —* 4 0.010 0.060 0.160 0.017 0.076 0.221 1.381 5 0.12 0.100 0.128 0.014 0.123 0.116 0.906 Mean ± SD 0.012 ± 0.002 0.070 ± 0.032 0.213 ± 0.123 0.014 ± 0.002 0.076 ± 0.031 0.205 ± 0.071 1.066 ± 0.268 ↵* Data were excluded because peak uptake was missed during first scan.
Ratio is based on patients evaluable in both scans.
Supplemental Data
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