A Phase 1 Study to Evaluate the Effect of BCX7353 on the Single Dose Pharmacokinetics of the P-gp Substrate Digoxin and the BCRP Substrate Rosuvastatin and the Effect of the P-gp Inhibitor Cyclosporine on the Single Dose Pharmacokinetics of BCX7353
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 54
- 试验地点
- 1
- 主要终点
- AUCinf of probe substrate
研究概览
简要总结
This is an open-label, three part study to evaluate the effect of BCX7353 on drug transporters as well as the effect of an inhibitor of drug transport on BCX7353.
详细描述
This is a single center, open-label, fixed-sequence, drug interaction study to evaluate the effect of BCX7353 on the pharmacokinetics of the P-gp substrate digoxin and the BCRP substrate rosuvastatin, as well as the effect of the P-gp inhibitor cyclosporine on the pharmacokinetics of BCX7353.
It is planned that 54 subjects will be enrolled into 3 cohorts of 18 subjects each. Cohort 1 will evaluate the effects of multiple doses of BCX7353 on single-dose pharmacokinetics of digoxin. Cohort 2 will evaluate the effect of multiple doses of BCX7353 on the pharmacokinetics of rosuvastatin. Cohort 3 will evaluate the effect of a single dose of cyclosporine on the pharmacokinetics of BCX7353. Cohorts may be dosed in parallel or in any order.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- None
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
- •written informed consent
- •acceptable birth control measures for male subjects and women of childbearing potential
- •creatinine clearance of at least 80 mL/min by Cockcroft-Gault equation
- •complies with all required study procedures and restrictions
排除标准
- •clinically significant medical history, current medical or psychiatric condition
- •clinically significant ECG finding, vital sign measurement or laboratory/urinalysis abnormality at screening or baseline
- •current use, or use of any prescribed or over the counter medication, vitamins or herbal products within 14 days of Day 1
- •use of medication that is known to inhibit or induce metabolic enzymes or transporters within 30 days of dosing
- •participation in any other investigational drug study within 90 days of screening
- •recent or current history of alcohol or drug abuse
- •regular recent use of tobacco or nicotine products
- •positive serology for HBV, HCV, or HIV
- •pregnant or nursing
- •donation or loss of greater than 400 mL of blood within the previous 3 months
- •history of severe hypersensitivity to any medicinal product
- •for subjects enrolled in cohort 1, current use of antibiotics or probiotics, or use within 6 months prior to Day 1
研究组 & 干预措施
Cohort 1
Day 1: Digoxin 0.25 mg oral dose Day 11-18: BCX7353 350 mg oral dose Day 19: Digoxin 0.25 mg oral dose and BCX7353 350 mg oral dose Day 20-21: BCX7353 350 mg oral dose
干预措施: BCX7353 (Drug)
Cohort 1
Day 1: Digoxin 0.25 mg oral dose Day 11-18: BCX7353 350 mg oral dose Day 19: Digoxin 0.25 mg oral dose and BCX7353 350 mg oral dose Day 20-21: BCX7353 350 mg oral dose
干预措施: Digoxin (Drug)
Cohort 1
Day 1: Digoxin 0.25 mg oral dose Day 11-18: BCX7353 350 mg oral dose Day 19: Digoxin 0.25 mg oral dose and BCX7353 350 mg oral dose Day 20-21: BCX7353 350 mg oral dose
干预措施: BCX7353 + digoxin (Drug)
Cohort 2
Day 1: Rosuvastatin 10 mg oral dose Day 7-14: BCX7353 350 mg oral dose Day 15: Rosuvastatin 10 mg oral dose and BCX7353 350 mg oral dose Day 16: BCX7353 350 mg oral dose
干预措施: BCX7353 (Drug)
Cohort 2
Day 1: Rosuvastatin 10 mg oral dose Day 7-14: BCX7353 350 mg oral dose Day 15: Rosuvastatin 10 mg oral dose and BCX7353 350 mg oral dose Day 16: BCX7353 350 mg oral dose
干预措施: Rosuvastatin (Drug)
Cohort 2
Day 1: Rosuvastatin 10 mg oral dose Day 7-14: BCX7353 350 mg oral dose Day 15: Rosuvastatin 10 mg oral dose and BCX7353 350 mg oral dose Day 16: BCX7353 350 mg oral dose
干预措施: rosuvastatin + BCX7353 (Drug)
Cohort 3
Day 1: BCX7353 350 mg oral dose Day 14: single oral dose of Cyclosporine 600 mg and BCX7353 350 mg
干预措施: BCX7353 (Drug)
Cohort 3
Day 1: BCX7353 350 mg oral dose Day 14: single oral dose of Cyclosporine 600 mg and BCX7353 350 mg
干预措施: Cyclosporine + BCX7353 (Drug)
结局指标
主要结局
AUCinf of probe substrate
时间窗: plasma pharmacokinetic parameters are based on blood sampling over a 48 - 72 hour period
Cmax of probe substrate
时间窗: plasma pharmacokinetic parameters are based on blood sampling over a 48 - 72 hour period
AUClast of probe substrate
时间窗: plasma pharmacokinetic parameters are based on blood sampling over a 48 - 72 hour period
次要结局
- physical examination findings(absolute and change from baseline through end of study, approximately 30 days)
- adverse events(absolute and change from baseline through end of study, approximately 30 days)
- vital signs(absolute and change from baseline through end of study, approximately 30 days)
- laboratory analyses(absolute and change from baseline through end of study, approximately 30 days)
- electrocardiograms(absolute and change from baseline throughend of study, approximately 30 days)