This is a single-center, open-label, single-dose phase I study to investigate the absorption, metabolism and excretion of \[14C\] Ensartinib 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 4-6 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 200 mg (100 μCi) of \[14C\]Ensartinib 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
TREATMENT
Masking
NONE
Enrollment
6
A novel, potent ALK inhibitor.The ALK inhibitor ensartinib has been validated in potency and selectivity assays indicating that it is more selective and up to 10 times more potent than competitive ALK inhibitors. Ensartinib has been active in animal models of non-small cell lung cancer (NSCLC) and neuroblastoma, a childhood cancer. Importantly, ensartinib has shown activity in models with ALK mutations that confer resistance to other small molecule ALK inhibitors.
Jiangsu Province Hospital Affiliated to Nanjing Madical University of Medicine
Nanjing, Jiangsu Provence, China
RECRUITINGRadioactivity concentration of each plasma sample
Use liquid scintillation counter to evaluate Radioactivity concentration of each plasma(DPM/ml) sample
Time frame: Day1-Day15
Radioactivity concentration of each urine samples
Use liquid scintillation counter to evaluate Radioactivity concentration of each urine(DPM/ml) sample
Time frame: Day1-Day15
Radioactivity concentration of each feces sample
Use liquid scintillation counter to evaluate Radioactivity concentration of each feces(DPM/g) sample
Time frame: Day1-Day15
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: Day1-Day15
Plasma drug concentrations
To determine the plasma concentrations of Ensartinib with validated LC-MS/MS method for obtaining its pharmacokinetics parameters;
Time frame: Day1-Day15
Number of participants with treatment-related adverse events as assessed by CTCAE v4.03
According to CTCAE v4.03, the number and frequency of adverse events after a single dose of test drug were assessed.
Time frame: Day1-Day15
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