An Open-Label Phase 1 Study to Determine the Pharmacokinetics, Metabolism, and Routes of Excretion of (14C) Radiolabeled PCI-32765 in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 6
- 主要终点
- Area under the concentration-time curve (AUC) of ibrutinib
研究概览
简要总结
The purpose of this study is to investigate the absorption, the metabolic pathways and the excretion of ibrutinib in healthy male adult participants after administration of a single oral dose of 50 mg to 140 mg (5 mg/mL solution) of unlabeled ibrutinib admixed with 14C ibrutinib.
详细描述
This is an open-label (all people know the identity of the intervention), single-center, single-dose study in healthy male participants. Six men will be enrolled to allow a minimum of 4 participants to complete the study. All participants will receive a single oral solution dose of 50 to 140 mg ibrutinib containing 1480 kBq (40 µCi) of 14C labeled ibrutinib, constituting a total radiation burden of approximately 0.916 mSv (ICRP risk category IIa). The duration of the study is approximately 73 days including screening period of 28 days, treatment period of 15 days, and follow-up period of 30 days. Safety will include adverse events, laboratory safety, 12 lead electrocardiogram, physical examination, and vital signs.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 30 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Participant must sign an informed consent document indicating they understand the purpose of and procedures required for the study, including DNA analysis, and are willing to participate in the study
- •Must agree to use an adequate contraception method as deemed appropriate by the investigator (eg, vasectomy, double-barrier, partner using effective contraception) during the study and for 3 months after receiving the study drug
- •Must agree to not donate sperm during the study and for 3 months after receiving the study drug
- •Blood pressure (after the participant is supine for 5 minutes) between 90 and 140 mmHg systolic, inclusive, and no higher than 90 mmHg diastolic
- •Non-smoker (not smoked for 6 months prior to screening)
排除标准
- •History of or current clinically significant medical illness including cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders, lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease
- •Clinically significant abnormal values for hematology, coagulation and platelet function, clinical chemistry or urinalysis at screening as deemed appropriate by the investigator
- •Clinically significant abnormal physical examination, vital signs or 12 lead electrocardiogram (ECG) at screening as deemed appropriate by the investigator
- •History of clinically significant allergies, especially known hypersensitivity or intolerance to β-lactam antibiotics or sulfonamides
- •Known allergy to heparin or history of heparin induced thrombocytopenia
研究组 & 干预措施
Ibrutinib
All participants will receive a single oral solution dose of 50 mg to 140 mg -ibrutinib containing 1480 kBq (40 µCi) of 14C-labeled ibrutinib, with a total radiation burden of approximately 0.916 mSv.
干预措施: Ibrutinib (Drug)
结局指标
主要结局
Area under the concentration-time curve (AUC) of ibrutinib
时间窗: Predose, Day 1 (0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 hours), Day 2 (24 hours), Day 3 (48 hours), Day 4 (72 hours)
Pharmacokinetic parameter AUC of ibrutinib will be determined.
Amount excreted into the urine (Ae) of ibrutinib
时间窗: Day -1, Day 1 over intervals 0-2, 2-4, 4-8, 8-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 hours, Days 9-15
Pharmacokinetic parameter Ae of ibrutinib will be determined by multiplying the urinary volume with the urinary concentration.
Time to reach the maximum concentration (tmax) of ibrutinib
时间窗: Predose, Day 1 (0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 hours), Day 2 (24 hours), Day 3 (48 hours), Day 4 (72 hours)
Pharmacokinetic parameter tmax of ibrutinib will be determined.
Maximum concentration (Cmax) of ibrutinib
时间窗: Day 1 (Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 hours), Day 2 (24 hours), Day 3 (48 hours), Day 4 (72 hours)
Pharmacokinetic parameter Cmax of ibrutinib will be determined.
次要结局
- Number of patients with adverse events(Up to 73 days)