A Phase 1 Open-Label, Randomized, Parallel-Group Study in Healthy Subjects to Investigate the Effect of Different Storage Conditions of a Long-Acting Nanosuspension of Rilpivirine on the Single-Dose Plasma Pharmacokinetics of Rilpivirine After Intramuscular Injection
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 61
- 主要终点
- Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Time (AUC [0-last])
研究概览
简要总结
The purpose of this study is to compare the single-dose pharmacokinetics of rilpivirine (RPV) after intramuscular (IM) injection of rilpivirine long-acting parenteral formulation (RPV-LA) and 'aged' RPV-LA, in healthy adult participants.
详细描述
This is a phase 1 randomized (study medication is assigned by chance), open-label (all people know the identity of the intervention), parallel-group, sequential study in healthy adult participants to investigate the effect of different storage conditions for RPV-LA on the single-dose pharmacokinetics of rilpivirine (RPV) after intramuscular injection. A total of 60 healthy adult participants will be enrolled in this study. The study will consist of 2 treatment sessions in a fixed sequential order : session 1 of up to day 8, all participants will receive a single oral dose of rilpivirine 25 milligram (mg) tablet on day 1, session 2 will consists of 2 treatment groups. The participants will be randomized in session 2 on Day 1 in a 1:1 ratio to Treatments A and B. Each treatment group will receive one IM injection of RPV LA on Day 1 of session 2. Session 1 and 2 will be separated by a washout period of at least 14 days. The total study duration for each participant will be approximately 6.5 months. Safety will be monitored throughout the study.
研究设计
- 研究类型
- Interventional
- 分配方式
- 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
- •Each participant must sign an Informed Consent Form (ICF) indicating that he or she understands the purpose of, and procedures required for, the study and are willing to participate in the study
- •Participant must be willing and able to adhere to the prohibitions and restrictions specified in this protocol
- •Participant must be healthy on the basis of a medical evaluation that reveals the absence of any clinically significant abnormality and includes a physical examination, medical history, vital signs, Electrocardiogram (ECG), and the results of blood biochemistry, hematology and coagulation tests and a urinalysis performed at Screening
- •A female participant of childbearing potential must have a negative serum (beta-human chorionic gonadotropin [beta-hCG]) at Screening and a negative urine pregnancy test on day 1
- •Participant must be non-smoking for at least 3 months prior to selection
排除标准
- •Female participant who is breastfeeding at Screening
- •Participants with a history of any illness that, in the opinion of the investigator, might confound the results of the study or pose an additional risk in administering study drug to the participant or that could prevent, limit or confound the protocol specified assessments. This may include, but is not limited to, renal dysfunction, significant cardiac, vascular, pulmonary, gastrointestinal, endocrine, neurologic, hematologic, rheumatologic, psychiatric, neoplastic, or metabolic disturbances
- •Has known allergies, hypersensitivity, or intolerance to rilpivirine (RPV) or its excipients
- •Has a history of drug allergy such as, but not limited to, sulfonamides and penicillins, or drug allergy witnessed in previous studies with experimental drugs
- •Having donated or lost more than 1 unit of blood (500 milliliter [mL]) within 60 days or more than 1 unit of plasma within 7 days before the first dose of study drug
研究组 & 干预措施
Rilpivirine Long-Acting Parenteral Formulation (RPV-LA)
Participants will receive oral tablet of rilpivirine 25 milligram (mg) once on Day 1 of session 1 and intramuscular (IM) injection of rilpivirine long-acting parenteral formulation 600 mg once on day 1 of session 2.
干预措施: Rilpivirine (RPV) (Drug)
Rilpivirine Long-Acting Parenteral Formulation (RPV-LA)
Participants will receive oral tablet of rilpivirine 25 milligram (mg) once on Day 1 of session 1 and intramuscular (IM) injection of rilpivirine long-acting parenteral formulation 600 mg once on day 1 of session 2.
干预措施: Rilpivirine Long-Acting Parenteral Formulation (RPV-LA) (Drug)
Aged RPV-LA
Participants will receive oral tablet of rilpivirine 25 milligram (mg) once on Day 1 of session 1 and IM injection of aged rilpivirine long-acting parenteral formulation 600 mg once on day 1 of session 2.
干预措施: Rilpivirine (RPV) (Drug)
Aged RPV-LA
Participants will receive oral tablet of rilpivirine 25 milligram (mg) once on Day 1 of session 1 and IM injection of aged rilpivirine long-acting parenteral formulation 600 mg once on day 1 of session 2.
干预措施: Aged RPV-LA (Drug)
结局指标
主要结局
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Time (AUC [0-last])
时间窗: In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose
The AUC (0-last) is the area under the plasma concentration-time curve for rilpivirine from time zero to last quantifiable time.
Maximum Observed Plasma Concentration (Cmax)
时间窗: In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose
The Cmax is the maximum observed plasma concentration of rilpivirine.
Area Under the Plasma Concentration-Time Curve From Time Zero (Day 1) to Day 28 (AUC[0-d28])
时间窗: In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120 and 168 hours post-dose
The AUC (0-d28) is the area under the plasma concentration-time curve for rilpivirine from time zero to day 28.
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC[0-infinity])
时间窗: In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose
The AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of AUC(last) and C(last)/lambda(z); wherein AUC(last) is area under the plasma concentrationtime curve from time zero to last quantifiable time, C(last) is the last observed quantifiable concentration, and lambda(z) is elimination rate constant.
次要结局
- Number of Participants With Adverse Events(Up to 180 Days)
- Time to reach the maximum observed plasma concentration (Tmax)(In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose)
- Elimination Rate Constant (Lambda [z]) of rilpivirine(In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose)
- Apparent Terminal Half-life (t[1/2]) of rilpivirine(In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose)