Table S1 Clinical Bioanalysis Summary Information for Study A

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Table S1 Clinical bioanalysis summary information for study A

Test compound / Fostamatinib disodium
Analytical matrices / Plasma (K2-EDTA)
Urine
Semen
Analytes / R406
R406 N-glucuronide
R788
Internal standard (IS) / R940406-d9
[2-H, 13-C] R788
Validated methods / R406 plasma
R788 plasma
R406 urine
R406 N-glucuronide urine
R406 semen
Lower limit of quantification / R406 plasma: 0.250 ng/mL
R788 plasma: 0.500 ng/mL
R406 urine: 1.000 ng/mL
R406 N-glucuronide urine: 10.000 ng/mL
R406 semen: 0.250 ng/mL
Validated range / R406 plasma: 0.250–250 ng/mL
R788 plasma: 0.500–250 ng/mL
R406 urine: 1.000–1000 ng/mL
R406 N-glucuronide urine: 10.000–5000 ng/mL
R406 semen: 0.250–250 ng/mL
Quality control (QC) levels / R406 plasma: 0.750, 25.000, 200, 5000 (dilution QC) ng/mL
R788 plasma: 1.50, 25.000, 200 ng/mL
R406 urine: 3.000, 100, 800 ng/mL
R406 N-glucuronide urine: 30, 500, 4000, 50,000 (dilution QC) ng/mL
R406 semen: 0.750, 25.000, 200 ng/mL
Analytical technique/method of detection / R406 plasma: Liquid-liquid extraction,LC-MS/MS
R788 plasma: Protein precipitation,LC-MS/MS
R406 urine: Liquid-liquid extraction,LC-MS/MS
R406 N-glucuronide urine: Dilution with methanol,LC-MS/MS
R406 semen: Liquid-liquid extraction,LC-MS/MS
Total number of samples analyzed / R406 plasma: 1658
R788 plasma: 586
R406 urine: 312
R406 N-glucuronide urine: 312
R406 semen: 6
Sample storage conditions / In a freezer set to maintain approximately –70°C (–60 to –80°C)

LC-MS/MSliquid chromatography coupled with tandem mass spectrometry

Table S2 Clinical bioanalysis summary information for study B

Test compound / Fostamatinib disodium
Analytical matrices / R406: plasma (K2-EDTA), DBS (K2-EDTA), whole
blood (K2-EDTA), urine (fortified with CHAPS
solution)
R406 N-glucuronide: urine (fortified with CHAPS
solution)
Analytes / Plasma, DBS, whole blood: R406
Urine: R406 and R406 N-glucuronide
Internal standard (IS) / R406-d9
Validated methods / R406 plasma
R406 DBS
R406 whole blood
R406 urine
R406 N-glucuronide urine
Lower limit of quantification / R406 plasma: 2.500 ng/mL
R406 DBS: 2.500 ng/mL
R406 whole blood: 2.500 ng/mL
R406 urine: 1.000 ng/mL
R406 N-glucuronide urine: 10.000 ng/mL
Validated range / R406 plasma: 2.500–2500 ng/mL
R406 DBS: 2.500–2500 ng/mL
R406 whole blood: 2.500–2500 ng/mL
R406 urine: 1.000–1000 ng/mL
R406 N-glucuronide urine: 10.000–5000 ng/mL
Quality control (QC) levels / R406 plasma: 7.500, 250, 2000, 20,000 ng/mL (dilution QC)
R406 DBS: 7.500, 250, 2000, 20,000 ng/mL (dilution QC)
R406 whole blood: 7.500, 250, 2000, 20,000 ng/mL (dilution QC)
R406 urine: 3.000, 100, 800 ng/mL
R406 N-glucuronide urine: 30.000, 500, 4000, 50,000 ng/mL (dilution QC)
Analytical technique/method of detection / R406 plasma: liquid-liquid extraction, LC-MS/MS
R406 DBS: liquid-liquid extraction, LC-MS/MS
R406 whole blood: liquid-liquid extraction, LC-MS/MS
R406 urine: liquid-liquid extraction, LC-MS/MS
R406 N-glucuronide urine: direct dilution, LC-MS/MS
Total number of samples analyzed / R406 plasma: 1056
R406 DBS: 744 FS-DBS, 1056 PD-DBS
R406 whole blood: 1056
R406 urine: 168
R406 N-glucuronide urine: 168
Sample storage conditions / R406 plasma: –60 to –80°C
R406 DBS: room temperature
R406 whole blood: –60 to –80°C
R406 urine: –60 to –80°C
R406 N-glucuronide urine: –60 to –80°C

CHAPS 3-[(3-cholamidopropyl) dimethylammonio]-1-propane sulphonate, FS-DBS finger stick-drawn dried blood spot samples, PD-DBS pipette-drawn dried blood spot samples

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