A 3-Treatment, 3-Period, 6-Sequence Randomized Crossover Single-Dose Study Evaluating the Bioequivalence of High-Load and Low-Load Oral Tablet Formulations of Apx001 and the Effect of Food on the Absorption of Apx001 From the High-Load Tablet In Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 18
- 试验地点
- 1
- 主要终点
- Maximum Observed Plasma Concentration (Cmax)
研究概览
简要总结
A study to learn about the bioequivalence (the biochemical similarity of two medicines that share the same active ingredient and desired outcome for patients) of the study medicine called APX001 in healthy participants.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 65 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Body mass index (BMI) between 18.0 and 32.0 kg/m2, inclusive.
- •Minimum body weight of 50 kg.
- •Screening hematology, clinical chemistry, coagulation, and urinalysis consistent with overall good health and having an estimated glomerular filtration rate (eGFR) >80 mL/min, based on creatinine clearance calculation by the Cockcroft-Gault formula.
排除标准
- •Having any uncontrolled or active major systemic disease including, but not limited to: cardiovascular, pulmonary, gastrointestinal, metabolic, urogenital, neurological, immunological, psychiatric, or neoplastic disorder with metastatic potential.
- •History or presence of neurological disorders including abnormal movements or seizures.
- •History or presence of malignancy within the past year. Subjects who have been successfully treated with no recurrence of basal cell carcinoma of the skin or carcinoma in-situ of the cervix may be enrolled.
- •Significant and/or acute illness or chronic infection, as judged by the investigator, including, but not limited to: upper airway infection, urinary tract infection, or skin infection within 30 days prior to the first study drug administration.
- •Taking any drug or herbal CYP3A modulator (e.g., erythromycin; St. John's Wort) within 4 weeks (or 5 half-lives, whichever is longer) or any other nutrients known to modulate CYP3A activity (e.g., grapefruit juice; Seville orange) within 2 weeks prior to the first admission.
研究组 & 干预措施
APX001 Treatment A
Oral tablet with a 25% drug load (low-load) in fasted participants
干预措施: APX001 (Drug)
APX001 Treatment A
Oral tablet with a 25% drug load (low-load) in fasted participants
干预措施: APX001A (Drug)
APX001A Treatment B
Oral tablet with a high drug load in fasted participants
干预措施: APX001 (Drug)
APX001A Treatment B
Oral tablet with a high drug load in fasted participants
干预措施: APX001A (Drug)
APX001A Treatment C
Oral tablet with a high drug load in participants that are not fasted.
干预措施: APX001 (Drug)
APX001A Treatment C
Oral tablet with a high drug load in participants that are not fasted.
干预措施: APX001A (Drug)
结局指标
主要结局
Maximum Observed Plasma Concentration (Cmax)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Time to Reach Maximum Observed Plasma Concentration (Tmax)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Apparent Total clearance, Calculated as Dose/AUCinf (CL/F)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Apparent Volume of Distribution at Terminal Phase (Vz/F)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Apparent Terminal Elimination Rate Constant (λz)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Number of Participants With Treatment Emergent Treatment-Related Adverse Events (AEs)
时间窗: Baseline through Day 14
Number of Participants With Change From Baseline in Laboratory Tests Results
时间窗: Baseline through Day 14
Number of Participants With Clinically Significant Change in Vital Signs
时间窗: Baseline through Day 14
Number of Participants With Clinically Significant Findings in Electrocardiogram (ECG) Abnormalities
时间窗: Baseline through Day 14
Number of Participants With Abnormalities in Physical Examinations
时间窗: Baseline through Day 14
Percentage of Area Under the Curve Extrapolated to Infinity (%AUCextra)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Plasma Decay Half-Life (t1/2)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Area Under the Curve From Time Zero to 24 hours (AUC0-24)
时间窗: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
次要结局
未报告次要终点