A Phase 1, Randomized, Placebo-Controlled Study to Investigate the Safety, Tolerability and Pharmacokinetics of Single and Multiple Oral Doses of APX001, to Investigate the Effect of Food on APX001 and to Investigate the Drug-Drug Interaction Potential of APX001
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 46
- 试验地点
- 2
- 主要终点
- Safety and tolerability of single and multiple oral doses of APX001 as measured by adverse events (AEs), physical examinations (PE), vital signs (VS), laboratory safety tests, urinalysis and 12-lead electrocardiograms (ECG).
研究概览
简要总结
This is a Phase l double-blind, placebo-controlled, randomized study to investigate the safety, tolerability, pharmacokinetics, bioavailability and food effect of single doses of APX001 administered intravenously and orally, followed by an evaluation of the safety, tolerability, pharmacokinetics and drug-drug interaction potential of multiple doses of APX001 administered orally.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Treatment
- 盲法
- Double (Participant, Investigator)
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Women of childbearing potential must agree to avoid pregnancy during the study and to use contraception at least 2 weeks before the start of the study until 3 months after the last dose of study drug.
- •Males with partner(s) of childbearing potential must agree to use appropriate barrier contraception from the screening period until 3 months after the last dose of study drug.
- •Screening hematology, clinical chemistry, coagulation and urinalysis consistent with overall good health.
- •No significantly abnormal findings on physical examination, ECG and vital signs.
- •Willing and able to provide written informed consent.
排除标准
- •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 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.
- •Use of prescription medication within 14 days prior to the first dose of study drug and throughout the study.
- •Use of non-prescription or over-the-counter medications within 7 days prior to the first dose of study drug and throughout the study.
- •Positive results on any of the following Screening laboratory tests: serum pregnancy test, urine alcohol test, urine drugs of abuse, hepatitis B surface antigen, hepatitis C antibody, and human immunodeficiency virus (HIV) antibody.
研究组 & 干预措施
Cohort 1a, Period B
single oral dose, crossover
干预措施: APX001 single oral dose 1 (Drug)
Cohort 1b, Period E
Single oral dose under fasted conditions, crossover
干预措施: Matching placebo control (Drug)
Cohort 1b, Period F
Single oral dose under fed conditions, crossover
干预措施: APX001 single oral dose fed (Drug)
Cohort 3
Multiple oral doses
干预措施: APX001 multiple oral doses 2 (Drug)
Cohort 1a, Period A
single intravenous dose, crossover
干预措施: APX001 single IV dose (Drug)
Cohort 1a, Period A
single intravenous dose, crossover
干预措施: Matching placebo control (Drug)
Cohort 1a, Period B
single oral dose, crossover
干预措施: Matching placebo control (Drug)
Cohort 1a, Period C
single oral dose
干预措施: APX001 single oral dose 2 (Drug)
Cohort 1a, Period C
single oral dose
干预措施: Matching placebo control (Drug)
Cohort 1a, Period D
single oral dose, crossover
干预措施: APX001 single oral dose 3 (Drug)
Cohort 1a, Period D
single oral dose, crossover
干预措施: Matching placebo control (Drug)
Cohort 1b, Period E
Single oral dose under fasted conditions, crossover
干预措施: APX001 single oral dose fasted (Drug)
Cohort 1b, Period F
Single oral dose under fed conditions, crossover
干预措施: Matching placebo control (Drug)
Cohort 2
Multiple oral doses
干预措施: APX001 multiple oral doses 1 (Drug)
Cohort 2
Multiple oral doses
干预措施: Matching placebo control (Drug)
Cohort 3
Multiple oral doses
干预措施: Matching placebo control (Drug)
Cohort 4
Multiple oral doses in presence of CYP probe substrates
干预措施: APX001 single IV dose (Drug)
Cohort 4
Multiple oral doses in presence of CYP probe substrates
干预措施: APX001 multiple oral doses 3 (Drug)
Cohort 4
Multiple oral doses in presence of CYP probe substrates
干预措施: Cytochrome P450 substrates (Drug)
结局指标
主要结局
Safety and tolerability of single and multiple oral doses of APX001 as measured by adverse events (AEs), physical examinations (PE), vital signs (VS), laboratory safety tests, urinalysis and 12-lead electrocardiograms (ECG).
时间窗: 21 days
次要结局
- Pharmacokinetics of single and multiple doses of APX001 as measured by terminal half life (t1/2).(21 days)
- Pharmacokinetics of single and multiple doses of APX001 as measured by maximum observed concentration (Cmax).(21 days)
- Pharmacokinetics of single and multiple doses of APX001 as measured by accumulation ratio.(21 days)
- Pharmacokinetics of single and multiple doses of APX001 as measured by elimination rate constant (Kel).(21 days)
- Pharmacokinetics of single and multiple dose of APX001 as measured by area under the curve (AUC).(21 days)
- Pharmacokinetics of single and multiple doses of APX001 as measured by volume of distribution (Vd).(21 days)