Phase I Clinical Study on Material Balance of [14C]Zorifertinib in Healthy Adult Male Participants in China

Alpha Biopharma (Jiangsu) Co., Ltd.1 个研究点分布在 1 个国家目标入组 6 人开始时间: 2026年7月6日最近更新: 2026年9月22日

适应症

干预措施

试验速览

阶段: 1 期
状态: 已完成
发起方
入组人数: 6
试验地点: 1
主要终点: Total radioactive recovery and cumulative total radioactive recovery in urine and feces at each time interval

研究概览研究设计入排标准研究组 & 干预措施结局指标研究者研究点记录与标识符相似试验

研究概览

简要总结

This is a single-center, single-dose, open-label, Phase I study to evaluate the mass balance, biotransformation, pharmacokinetic characteristics, excretion pathways, and safety of a single oral 200 mg/5 µCi dose of [14C]Zorifertinib in healthy Chinese adult male participants. The study includes a screening period (Day -14 to Day -1) and a dosing and observation period (Day 1 to Day 14). Blood, urine, and feces samples will be collected to measure radioactivity, drug concentrations, and metabolites. Safety will be assessed by adverse events, vital signs, laboratory tests, 12-lead ECG, and ophthalmic examinations. The target total radioactivity recovery is ≥90% of the administered dose.

研究设计

研究类型: Interventional
分配方式: Na
干预模型: Single Group
主要目的: Basic Science
盲法: None

入排标准

年龄范围: 18 Years 至 45 Years（Adult）
性别: Male
接受健康志愿者: 是

入选标准

•Healthy Chinese males;
•Age at the time of signing the informed consent form: 18-45 years (inclusive);
•Body mass index (BMI) ranging from 19-26 kg/m2 (inclusive), with a body weight of no less than 50 kg;
•Fully understand the purpose and requirements of this study and voluntarily sign the informed consent form;
•Be able to communicate well with the investigators and complete the trial according to the protocol.
•The 14C content in plasma and urine samples obtained during screening are within general environmental 14C background levels. Directly analyzed plasma samples must have values ≤150 pMC, and urine samples containing petroleum-based carbon carriers must have values ≤50 pMC.

排除标准

•Ancillary Examinations:
•Abnormal findings from comprehensive physical examination, vital signs, laboratory tests (hematology, blood biochemistry, coagulation function, urinalysis, routine stool + occult blood, thyroid function), 12-lead ECG, chest X-ray (posteroanterior view), abdominal ultrasound, digital rectal examination, etc., that are judged by the investigator as clinically significant.
•Resting corrected QT interval (Fridericia correction, QTcF = QT/RR1/3) obtained from 12-lead ECG >450 ms in males, or other abnormalities judged by the investigator as clinically significant.
•Positive result for any of the following: hepatitis B surface antigen or hepatitis B e antigen, hepatitis C virus antibody, Treponema pallidum antibody, or human immunodeficiency virus antigen/antibody combination test (HIV-Ag/Ab).
•Abnormal findings from ophthalmic examination (slit lamp, intraocular pressure, fundus photography) that are clinically significant.
•Medication History:
•Use of any drugs that inhibit or induce the drug-metabolizing enzyme CYP3A4 within 30 days prior to the screening period.
•Use of any prescription drugs, over-the-counter drugs, herbal medicines, or food supplements (e.g., vitamins, calcium supplements) within 14 days prior to the screening period.
•Medical and Surgical History:
•History of any clinically serious disease or condition that the investigator believes may affect the trial results, including but not limited to circulatory, respiratory, endocrine, nervous, digestive, urinary, hematologic, immune, psychiatric, or metabolic diseases;
•History of dysphagia or any condition that may affect drug absorption, e.g., gastrectomy, cholecystectomy, gastric bypass, duodenotomy, colectomy, inflammatory bowel disease;
•History of organic heart disease, heart failure, myocardial infarction, angina pectoris, arrhythmia, ventricular tachycardia, clinically symptomatic AV block, long QT syndrome, or family history of long QT syndrome (evidenced by genetic proof or sudden cardiac death of a close relative at a young age);
•Major surgery within 6 months prior to the screening period, or surgical incision not fully healed; Major surgery includes, but is not limited to, any procedure with significant bleeding risk, prolonged general anesthesia, incisional biopsy, or significant traumatic injury;
•Allergic constitution, e.g., known history of allergy to two or more substances; Or judged by the investigator as potentially allergic to the investigational drug;
•Hemorrhoids or perianal diseases with regular/ongoing hematochezia, irritable bowel syndrome, inflammatory bowel disease.
•Lifestyle Habits:
•Habitual constipation or diarrhea;
•Alcoholism or regular alcohol consumption within 6 months prior to screening, i.e., alcohol intake exceeding 14 units per week (1 unit = 360 mL beer, or 45 mL spirit with 40% alcohol, or 150 mL wine), or a breath alcohol test result ≥20 mg/dL at screening, or inability to abstain from alcohol during the trial period;
•Smoking >5 cigarettes per day or habitual use of nicotine-containing products within 3 months prior to screening, or inability to abstain during the trial period;
•Drug abuse or use of soft drugs (e.g., cannabis) within 3 months prior to screening, or use of hard drugs (e.g., amphetamines, phencyclidine) within 1 year prior to screening; Or positive urine screen for drugs of abuse during the screening period;
•Habitual consumption of grapefruit juice or excessive tea, coffee, and/or caffeinated beverages, and inability to abstain during the study period.
•Participation in a radiolabeled drug trial within 1 year prior to screening, or participation in a 14C-labeled breath test within 3 months prior to screening;
•History of needle phobia or blood phobia, difficulty with blood collection, or inability to tolerate venous puncture;
•Participation in any other clinical trial (including drug and device trials) within 3 months prior to the screening period;
•Vaccination within 1 month prior to screening, or planned vaccination during the study period;
•Plan to father a child or donate sperm during the study period or within 1 year after study completion, or disagreement to use strict contraceptive measures (see Appendix 1) for themselves and their partners during the study period and within 1 year after study completion;
•Blood loss or blood donation of ≥400 mL within 3 months prior to screening, or blood transfusion within 1 month;
•Any other factor that, in the investigator's opinion, makes the participant unsuitable for participation in this trial.

研究组 & 干预措施

Single Dose Zorifertinib Group

Experimental

干预措施: [14C]Zorifertinib Oral Formulation (Drug)

结局指标

主要结局

Total radioactive recovery and cumulative total radioactive recovery in urine and feces at each time interval

时间窗: Pre-dose up to 312 hours after dosing, or until termination criteria met

Percentage of total radioactivity exposure (%AUC), percentage of parent drug and its metabolites (%Dose), and metabolite identification

时间窗: Pre-dose up to 312 hours after dosing, or until termination criteria met

Percentage of total radioactivity exposure (%AUC) accounted for by parent drug and its metabolites in plasma. Percentage of administered dose (%Dose) accounted for by parent drug and its metabolites in urine and faeces. Identification of metabolites in plasma, urine, and feces

Peak Plasma Concentration (Cmax)