SB-681323 is a p38 MAP kinase inhibitor and is currently under development by GlaxoSmithKline. This will be an open label study conducted at one site. Six healthy male subjects will be enrolled to ensure at least four fully evaluable subjects. Each subject will receive a single 10mg/ 50 µCurie oral dose of \[14C\]SB-681323. Urine and faecal samples will be collected until 216 h after dosing but subjects may be discharged after 168 h if 90% of the dose is recovered and/or \<1% of the dose is excreted in a 24 h period. Blood and plasma will be collected at various sample times after dosing to measure parent drug and total drug-related material. Samples of urine, faeces and plasma will be transferred into separate study to characterise and quantify metabolites in these matrices. Safety will be assessed by adverse event monitoring, vital signs, ECG and clinical laboratory tests.
This will be an open label study conducted at one site. Six healthy male subjects will be enrolled to ensure at least four fully evaluable subjects. Each subject will receive a single 10mg/ 50 µCurie oral dose of \[14C\]SB-681323. Urine and faecal samples will be collected until 216 h after dosing but subjects may be discharged after 168 h if 90% of the dose is recovered and/or \<1% of the dose is excreted in a 24 h period. Blood and plasma will be collected at various sample times after dosing to measure parent drug and total drug-related material. Samples of urine, faeces and plasma will be transferred into separate study to characterise and quantify metabolites in these matrices. Safety will be assessed by adverse event monitoring, vital signs, ECG and clinical laboratory tests.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
4
\[14C\] SB-681323 oral solution, is available as a powder which will be made into a solution of 0.1 milligram/milliliter (0.5 microcurie) \[14C\] SB-681323 in dextrose and water for injection on the day prior to dosing. For a 10 milligram/50 microcurie oral dose of \[14C\]SB-681323, 100 milliliters of 0.1 milligram/milliliter (0.5 microcurie/milliliter \[14C\] SB-681323 oral solution will be dosed.
GSK Investigational Site
Tranent, West Lothian, United Kingdom
Urinary and faecal cumulative excretion as a percentage of the total radioactive dose administered over time.
Time frame: 168 Hours
AUC(0-8), Cmax, AUC(0-t), tmax and t½ of total radioactivity and SB8681323 in plasma following oral dosing.- Blood:Plasma ratio of total radioactivity.- AEs, ECG, vital signs and clinical laboratory tests (including LFTs).
Time frame: 216 Hours
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