ALK-POSITIVE NSCLC
Conditions
Brief summary
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.
Detailed description
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
Interventions
DRUGEnsartinib
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.
Sponsors
Betta Pharmaceuticals Co., Ltd.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
A subject will be eligible for study participation if he meets the following criteria: 1. healthy male volunteers between the ages of 18 to 50 years old, inclusive; 2. Body weight \>=50 kg, Body mass index (body weight(kg)/hight2(m2)) between 19 and 26 kg/m2 (inclusive); 3. Normal physical findings, clinical laboratory values, vital signs and 12-lead ECG, or any abnormality that is non-clinically significant; 4. Male subjects of reproductive potential with partners will be instructed to, and must be willing to practice a highly effective method of birth control for the duration of the study and continuing 1 year after discontinuing treatment with the investigational product. Highly effective methods of birth control include using condom, contraceptive sponge, contraceptive gel, contraceptive film, intrauterine device, oral or injectable contraceptive pill, hypodermic implants or others; 5. Must understand, and voluntarily sign the informed consent, comply with the requirements of the study
Exclusion criteria
A subject will not be eligible for study participation if he meets any of the
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Radioactivity concentration of each urine samples | Day1-Day15 | Use liquid scintillation counter to evaluate Radioactivity concentration of each urine（DPM/ml） sample |
| Radioactivity concentration of each plasma sample | Day1-Day15 | Use liquid scintillation counter to evaluate Radioactivity concentration of each plasma（DPM/ml) sample |
| Radioactivity concentration of each feces sample | Day1-Day15 | Use liquid scintillation counter to evaluate Radioactivity concentration of each feces（DPM/g） sample |
| Total recovery of radioactivity in urine and feces | Day1-Day15 | Calculate the total radioactivity in urine and feces based on the radioactivity concentration of each sample. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Plasma drug concentrations | Day1-Day15 | To determine the plasma concentrations of Ensartinib with validated LC-MS/MS method for obtaining its pharmacokinetics parameters; |
| Number of participants with treatment-related adverse events as assessed by CTCAE v4.03 | Day1-Day15 | According to CTCAE v4.03, the number and frequency of adverse events after a single dose of test drug were assessed. |
Countries
China
Contacts
Primary ContactFeng Shao
Backup ContactSufeng Zhou
Outcome results
None listed