An Open Label, Balanced, Randomized, Two-Treatment, Two-Sequence, Four-Period, Full Replicate, Crossover, Single Dose, Oral Comparative Bioavailability Study of XS004 (Dasatinib) 100 mg Film-Coated Tablets, Formulation G of Xspray Pharma AB, Sweden, and SPRYCEL® (Dasatinib) 140 mg Film-Coated Tablets of Bristol-Myers Squibb Company, Princeton, NJ 08543 USA in Healthy, Adult Subjects Under Fasting Conditions
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 110
- 试验地点
- 1
- 主要终点
- Area Under the Plasma Concentration-Time Curve from Zero to the Last Measurable Concentration (AUC0-t) of XS004 and SPRYCEL®
研究概览
简要总结
An open label, single-center, balanced, randomized, two-treatment, two-sequence, four-period, full replicate, crossover, single dose, Phase I, oral comparative bioavailability study in healthy, adult participants (male subjects and female subjects of non-childbearing potential) under fasting conditions with a screening period of 21 days prior to enrollment. In each study period, 21 blood samples were collected from each participant to analyze the pharmacokinetic profile of the test as well as the reference drug.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Other
- 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
- •Healthy males (sterile or using contraception) or females of non-childbearing potential 18 and 55 years of age
- •Acceptable medical history, physical examination, laboratory investigations within 21 days prior to enrollment
- •Clinical laboratory values were within the laboratory's stated normal range. If not within this range, they must be without clinical significance, as determined by the Investigator
- •The subject is able to communicate meaningfully with study personnel and is anticipated to be able to comply fully with study procedures
排除标准
- •Any history of impairment of cardiovascular, pulmonary, hepatic, renal, gastrointestinal, endocrine, immunological, dermatological, neurological, psychiatric disease or disorder
- •Participated in any other clinical study or donated blood in last 90 days
- •Positive screens for serum hepatitis B surface antigen (HbsAg), hepatitis C antibody (HepC) or human immunodeficiency virus (HIV)
- •Female subjects demonstrating a positive pregnancy screen, currently breastfeeding or using hormone replacement therapy within three months prior to dosing of test product
研究组 & 干预措施
XS004 - Period 1
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 100 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel and in accordance with the randomization schedule.
干预措施: Dasatinib ASD 100 mg (Drug)
SPRYCEL - Period 1
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 140 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel, and in accordance with the randomization schedule.
干预措施: Dasatinib 140 MG [Sprycel] (Drug)
XS004 - Period 2
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 100 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel and in accordance with the randomization schedule.
干预措施: Dasatinib ASD 100 mg (Drug)
SPRYCEL - Period 2
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 140 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel, and in accordance with the randomization schedule.
干预措施: Dasatinib 140 MG [Sprycel] (Drug)
XS004 - Period 3
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 100 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel and in accordance with the randomization schedule.
干预措施: Dasatinib ASD 100 mg (Drug)
SPRYCEL - Period 3
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 140 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel, and in accordance with the randomization schedule.
干预措施: Dasatinib 140 MG [Sprycel] (Drug)
XS004 - Period 4
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 100 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel and in accordance with the randomization schedule.
干预措施: Dasatinib ASD 100 mg (Drug)
SPRYCEL - Period 4
At the clinic, after an overnight fast of at least 10 hours, a single oral dose of 140 mg tablet was administered to each participant in a sitting posture with about 240 mL of drinking water in the presence of the principal investigator and quality assurance personnel, and in accordance with the randomization schedule.
干预措施: Dasatinib 140 MG [Sprycel] (Drug)
结局指标
主要结局
Area Under the Plasma Concentration-Time Curve from Zero to the Last Measurable Concentration (AUC0-t) of XS004 and SPRYCEL®
时间窗: For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.
The pharmacokinetic parameters (AUC 0-t) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
Maximum Observed Plasma Concentration (Cmax) of XS004 and SPRYCEL®
时间窗: For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.
The pharmacokinetic parameters (Cmax) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
Area Under the Plasma Concentration-Time Curve from Zero Extrapolated to Infinity (AUC0-inf) of XS004 and SPRYCEL®
时间窗: For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.
The pharmacokinetic parameters (AUC 0-inf) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
次要结局
- Time of Maximum Observed Plasma Concentration (Tmax) of XS004 and SPRYCEL®(For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.)
- Lower Limit on Time for Elimination Rate Constant (Kel_lower) of XS004 and SPRYCEL®(For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.)
- Area Under the Plasma Concentration-Time Curve (Percent Extrapolation) of XS004 and SPRYCEL®(For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.)
- Elimination Rate Constant (Kel) of XS004 and SPRYCEL®(For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.)
- Upper Limit on Time for Elimination Rate Constant (Kel_upper) of XS004 and SPRYCEL®(For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.)
- Terminal Half-Life (T1/2) of XS004 and SPRYCEL®(For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.)