A Single Ascending Dose Phase 1 Study to Evaluate the Pharmacokinetics, Safety and Tolerability of a Single Intramuscular Injection of Quarterly Risperidone (QUAR) for Different Formulations and Dose Strengths in Participants With Schizophrenia (QUARTZ Study)
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 58
- 试验地点
- 1
- 主要终点
- λz
研究概览
简要总结
This is a single ascending dose phase 1 study to evaluate the pharmacokinetics (PK), safety, and tolerability of a single intramuscular (IM) injection of quarterly Risperidone (QUAR) for different formulations and dose strengths in participants with schizophrenia.
详细描述
The study will assess the PK, safety and tolerability of QUAR when administered as a single IM injection, in patients with schizophrenia. The study will be conducted with 3 different dose strengths and up to two formulations.
After eligibility confirmation, an oral treatment period follow by a washout period will be performed before QUAR IM administration.
The different cohorts will be administered with one of the following dosages of Risperidone QUAR:
Cohort 1/2: Formulation 1 or 2. Dose level 1 (Gluteal); Cohort 1a/2a: Formulation 1 or 2. Dose level 2 (Gluteal); Cohort 1b/2b: Formulation 1 or 2. Dose level 3 (Gluteal); Cohort 1c/2c: Formulation 1 or 2. Dose level 3 (Deltoid);
The progression to the next cohorts will take place after a clinical safety assessment. Several blood samples for plasma pharmacokinetic (PK) assessments will be obtained pre-dose and post-dose. Safety assessments will be conducted at each pre-specified time points.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Sequential
- 主要目的
- Treatment
- 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
- 否
入选标准
- •Capable of providing informed consent.
- •Male or female aged ≥ 18 years to < 65 years with BMI ≥17.0 to ≤35.0 kg/m2
- •Current diagnosis of schizophrenia, according to the Diagnostic and DSM-5 criteria.
- •Medically stable over the last month, and psychiatrically stable without significant symptom exacerbation over the last three months based on the investigator's judgment
- •currently taking oral risperidone as maintenance therapy
- •Score of ≤ 4 (moderately ill at most) on the Clinical Global Impression - Severity of Illness (CGI-S)
- •If a sexually active female of childbearing potential, using a medically accepted method of birth control.
排除标准
- •Presence of an uncontrolled, unstable, clinically significant medical condition that in the opinion of the investigator could interfere with the interpretation of safety and PK evaluations
- •If female, a positive serum pregnancy test, or planning to become pregnant between signing informed consent and 1 month after the last dose of study drug or is breastfeeding a child.
- •History of neuroleptic malignant syndrome and current or past history of clinically significant tardive dyskinesia.
- •The participant has a primary diagnosis other than schizophrenia diagnosis that is primarily responsible for current symptoms and functional impairment
- •Positive test result for drugs of abuse or alcohol unless the positive finding can be accounted for by documented prescription use.
- •In the investigator's opinion, at imminent risk of committing self-harm or harm to others.
- •Unwilling to discontinue any of the prohibited medications prior to the baseline visit or unable to safely washout such medication without significant destabilization or increased risk of self-harm (suicide).
- •Receipt study drug in another investigational study in the last 90 days.
- •Current participation in any other clinical trial.
研究组 & 干预措施
Cohort 1/2
Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 1 dose.
干预措施: Oral risperidone; QUAR F1/2, Dose 1 - Gluteal (Drug)
Cohort 1a/2a
Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 2 dose.
干预措施: Oral risperidone; QUAR F1/2, Dose 2 - Gluteal (Drug)
Cohort 1b//2b
Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 3 dose.
干预措施: Oral risperidone; QUAR F1/2, Dose 3 - Gluteal (Drug)
Cohort 1c/2c
Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 3 dose.
干预措施: Oral risperidone; QUAR F1/2, Dose 3 - Deltoids (Drug)
结局指标
主要结局
λz
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Terminal elimination rate constant
t1/2
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Terminal elimination half-life
Cmax
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Peak plasma concentration
Tmax
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Time to peak concentration
Cmin
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Minimum plasma concentration
Clast
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Last observed plasma concentration
AUC0-t
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Area under the curve
AUCinf
时间窗: Following QUAR administration until day 196
Area under the curve
AUCextrap
时间窗: Following QUAR administration until day 196
Area under the curve
Vd/F
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Apparent volume of distribution
Cl/F
时间窗: Following Oral and QUAR administration until day 17 or 196 respectively
Apparent total body clearance
次要结局
未报告次要终点