This is a single-center, open-label, single-dose phase I study to investigate the absorption, metabolism and excretion of \[14C\] D-0316 in healthy Chinese male subjects. The study will be conducted into two steps:Firstly, 2 subjects are enrolled in to participate in the pilot study to grope for the completion date of plasma, urine and feces sampling on the 3rd day post-dose and onwards. Then, the collection time of blood and excreta samples (urine and feces) from the subsequent 2-4 subjects will be adjusted according to the pilot study
Subjects who had signed informed consent and meet inclusion criteria and no exclusion criteria are admitted to Phase I Clinical Unit two days prior to dosing (D-2). On the morning of Day 1 before dosing, subjects will be transferred to nuclear medical ward. And after an overnight fast of at least 10 h, subjects will receive a single oral dose of 75 mg (50 μCi) of \[14C\]D-0316 as an oral suspension. Then, after two days of the dosing, subjects will be transferred back to Phase I Clinical Unit ward and confined to this unit until blood or excreta sampling and safety monitoring at the designated time points or intervals are complete
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Enrollment
4
Before administration, the drug preparation was placed at room temperature, and 40ml drinking water was added into each bottle to prepare suspension for the subjects to take. 40ml pure water was injected again. After washing the container, the subjects took orally. Repeat the previous step, and then used 160ml purified water. After the administration container was moistened for several times, the subjects took all the moistening lotion. Pay attention not to splash the liquid during mixing outside the bottle
Jiangsu Province Hospital Affiliated to Nanjing Madical University of Medicine
Nanjing, Jiangsu, China
Radioactivity concentration of each plasma sample
Use liquid scintillation counter or accelerator mass spectrometry to evaluate radioactivity concentration of each plasma(DPM/ml) sample
Time frame: Day 1-Day85
Radioactivity concentration of each urine samples
Use liquid scintillation counter or accelerator mass spectrometry to evaluate radioactivity concentration of each urine(DPM/ml) sample
Time frame: Day-1-Day85
Radioactivity concentration of each feces sample
Use liquid scintillation counter or accelerator mass spectrometry to evaluate radioactivity concentration of each feces(DPM/ml) sample
Time frame: Day-1-Day85
Total recovery of radioactivity in urine and feces
Calculate the total radioactivity in urine and feces based on the radioactivity concentration of each sample
Time frame: Day-1-Day85
Identification of metabolites in plasma, urine and fecal samples
LC-MS/MS was used to identify the main metabolites in plasma, urine and feces, and finally to provide the main biotransformation pathway of CM082 in human body
Time frame: Day-1-Day85
Pharmacokinetic parameters of unlabeled D-0316 and metabolite D-0865
To determine the plasma concentrations of D-0316 with validated LC-MS/MS method for obtaining its pharmacokinetics parameters
Time frame: Day-1-Day85
Number of participants with treatment-related adverse events as assessed by CTCAE v4.03
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According to CTCAE v4.03, the number and frequency of adverse events after a single dose of test drug were assessed
Time frame: Day-14-Day85