Phase I Sequential Dose Escalation Study of Pharmacokinetics, Safety and Tolerability After Single Dose (225 Mg-450 mg) Oral Administration of BILR 355 (SDS) Plus Low-dose Ritonavir in Healthy Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 48
- 主要终点
- CL/F (Apparent clearance of the analyte in plasma following extravascular administration)
研究概览
简要总结
The primary objective was to explore the relative bioavailability of increasing doses of BILR 355 BS, as a sodium dodecyl sulfate-containing solid formulation (SDS), in combination with ritonavir 100 mg and to explore the dose-concentration proportionality of increasing doses.
A secondary objective was to explore the effect of food on the pharmacokinetics of BILR 355 (SDS)
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
- 18 Years 至 60 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Males or females who met the inclusion/exclusion criteria, females who are not pregnant nor nursing, and who agreed to use a double-barrier method of birth control (condoms or diaphragm plus spermicide) throughout the trial (alone or in addition to other methods of birth control such as oral contraceptives)
- •Healthy HIV negative adult volunteers
- •Age ≥18 and ≤60 years
- •BMI ≥18.5 and BMI ≤29.9 kg/m2
- •Ability to give signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local regulations
排除标准
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Surgery of gastrointestinal tract (except appendectomy)
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- •History of relevant orthostatic hypotension, fainting spells or blackouts
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
- •Intake of drugs with a long half-life (>24 hours) within at least one month prior to study drug administration and during the trial
- •Use of drugs within 10 days prior to administration or during the trial which might reasonably influence the results of the trial
- •Participation in another trial with an investigational drug within two months prior to administration or during the trial
- •Current smoker
- •Alcohol abuse (more than 60 g/day)
- •Drug abuse (positive urine test for illicit prescription or non-prescription drugs or drugs of abuse)
- •Blood donation (more than 100 mL within four weeks prior to study drug administration or during the trial)
- •Excessive physical activities (within one week prior to study drug administration or during the trial)
- •Any laboratory value outside the reference range that is of clinical relevance at screening, according to the judgment of the investigator
- •Inability to comply with dietary regimen required by the protocol
- •Infected with hepatitis B or hepatitis C viruses (defined as either being hepatitis B surface antigen, or hepatitis C antibody positive)
- •Pregnant or lactating females
研究组 & 干预措施
BILR 355 (dose escalation) + Ritonavir
escalating dose groups, for food effect evaluation lowest dose group (D1) with high fat meal breakfast after wash-out period
干预措施: BILR 355 - D1 (Drug)
BILR 355 (dose escalation) + Ritonavir
escalating dose groups, for food effect evaluation lowest dose group (D1) with high fat meal breakfast after wash-out period
干预措施: BILR 355 - D2 (Drug)
BILR 355 (dose escalation) + Ritonavir
escalating dose groups, for food effect evaluation lowest dose group (D1) with high fat meal breakfast after wash-out period
干预措施: BILR 355 - D3 (Drug)
BILR 355 (dose escalation) + Ritonavir
escalating dose groups, for food effect evaluation lowest dose group (D1) with high fat meal breakfast after wash-out period
干预措施: BILR 355 - D4 (Drug)
BILR 355 (dose escalation) + Ritonavir
escalating dose groups, for food effect evaluation lowest dose group (D1) with high fat meal breakfast after wash-out period
干预措施: Ritonavir (Drug)
BILR 355 (dose escalation) + Ritonavir
escalating dose groups, for food effect evaluation lowest dose group (D1) with high fat meal breakfast after wash-out period
干预措施: high fat breakfast (Other)
结局指标
主要结局
CL/F (Apparent clearance of the analyte in plasma following extravascular administration)
时间窗: up to 120 hours after drug administration
t½ (Terminal half-life of the analyte in plasma)
时间窗: up to 120 hours after drug administration
Tmax (Time from dosing to the maximum concentration of the analyte in plasma)
时间窗: up to 120 hours after drug administration
AUC0-inf (Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
时间窗: up to 120 hours after drug administration
AUC0-tz (Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point)
时间窗: up to 120 hours after drug administration
Cmax (Maximum measured concentration of the analyte in plasma)
时间窗: up to 120 hours after drug administration
次要结局
- Number of patients with adverse events(up to 10 days after last dose administration)