A Definitive Bioequivalence Study of a New Boceprevir (SCH 503034) Tablet Formulation Compared to the Current Capsule Form in Healthy Male and Female Subjects.
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 177
- 主要终点
- Area Under the Concentration Curve (AUC) From Hour 0 to the Final Quantifiable Sample (AUCtf) for Boceprevir Tablets Versus Capsules in Fed State
研究概览
简要总结
This is a single-dose, randomized, cross-sectional comparison study examining the relative safety and resulting blood level profiles after administration of a new boceprevir tablet formulation versus its current capsule formulation for treatment of chronic hepatitis C. In Part 1 of the study participants will receive boceprevir tablets and capsules under fed conditions. In Part 2 of the study a new group of participants will receive boceprevir tablets and capsules under fasted conditions.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 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
- 是
入选标准
- •Subjects must be willing to give written informed consent for the trial and able to adhere to dose and visit schedules.
- •Subjects must be willing to give written informed consent for pharmacogenetic
- •testing, and able to adhere to applicable visit schedules.
- •Subjects of either gender and of any race between the ages of 18 and 65
- •years, inclusive, having a Body Mass Index (BMI) between 18 and 32,
- •inclusive. BMI = weight (kg)/height (m)^
- •(Individuals with values outside (or
- •indicate lower or higher) of these ranges may be enrolled if clinically
- •acceptable to the investigator and sponsor.)
- •Subjects' clinical laboratory tests (complete blood count [CBC], blood chemistry, and urinalysis) must be within normal limits or clinically acceptable to the investigator and within an allowed expanded range supplied by sponsor. However, subject's liver function test results (ie, aspartate aminotransferase [AST], alanine aminotransferase [ALT]) must not be elevated above normal limits at Screening and on Day -
- •No rescreening of liver function tests will be allowed.
- •Subjects must be free of any clinically significant disease that would interfere with the study evaluations.
- •The Screening 12 lead electrocardiogram [ECG] conduction intervals must be within gender specific normal range (e.g, ECG QTcB,measure in males ≤430 msec and QTcB measure in females ≤450 msec, PR interval ≤200 msec).
- •Vital sign measurements (taken after ~3 minutes in a sitting position) must be
- •within the following ranges: (Individuals with values outside of these ranges
- •may be enrolled if clinically acceptable to the investigator and sponsor.)
- •oral body temperature, between 35.0°C and 37.5°C
- •systolic blood pressure, 90 to 140 mm Hg
- •diastolic blood pressure, 45 to 90 mm Hg
- •pulse rate, 40 to 100 bpm
- •Female subjects must be:
- •postmenopausal (defined as 12 months with no menses, age > 40
- •years and with a follicle-stimulating hormone [FSH] level of >40 u/mL, and serum E2 < 73 pmol/L), or
- •surgically sterilized at least 3 months prior to baseline (eg, documented
- •hysterectomy or tubal ligation), or
- •premenopausal and if unsterilized must have used a medically
- •accepted method of contraception for 3 months (or abstained from
- •sexual intercourse) prior to the screening period, and agree to use a
- •medically accepted method of contraception during the trial (including
- •the screening period prior to receiving trial medication) and for
- •2 months after stopping the trial medication. An acceptable method of
- •contraception includes one of the following:
- •i. stable oral, transdermal, injectable, or sustained-release vaginal
- •hormonal contraceptive regimen without breakthrough uterine
- •bleeding for 3 months prior to Screening; in addition, during
- •study use of condom and/or spermicide (when marketed in the
- •ii. intrauterine device (inserted at least 2 months prior to Screening
- •visit); in addition, during study use of condom and/or spermicide
- •(when marketed in the country).
- •iii. condom (male or female) with spermicide (when marketed
- •within the country),
- •iv. diaphragm or cervical cap with spermicide (when marketed
- •within the country) and condom (male),
- •Non-vasectomized men must agree to use a condom with spermicide or abstain from sexual intercourse, during the trial and for 1 month after stopping the medication.
排除标准
- •Female subjects who are pregnant, intend to become pregnant (within
- •3 months of ending the study), or are breastfeeding.
- •Subjects who, in the opinion of the investigator, will not be able to participate optimally in the study.
- •Any surgical or medical condition which might significantly alter the
- •absorption, distribution, metabolism or excretion of any drug. The investigator
- •should be guided by evidence of any of the following, and be discussed with
- •the sponsor prior to enrollment into the trial:
- •history or presence of inflammatory bowel disease, ulcers,
- •gastrointestinal or rectal bleeding;
- •history of major gastrointestinal tract surgery such as gastrectomy,
- •gastroenterostomy, or bowel resection;
- •history of pancreatic injury or pancreatitis;
- •history or presence of liver disease or liver injury;
- •history or presence of impaired renal function as indicated by clinically
- •significant elevation in creatinine, blood urea nitrogen [BUN]/urea, urinary albumin, or
- •clinically significant urinary cellular constituents ; or
- •history of urinary obstruction or difficulty in voiding.
- •Subject who has a history of any infectious disease within 4 weeks prior to
- •drug administration that in the opinion of the investigator, affects the subject's ability to participate in the trial.
- •Subjects who are positive for hepatitis B surface antigen, hepatitis C
- •antibodies or human immunodeficiency virus [HIV].
- •Subjects who have a positive screen for drugs with a high potential for abuse
- •(during the Screening period or clinical conduct of the trial).
- •Subjects with a history of psychiatric or personality disorders that in the
- •opinion of the investigator and sponsor, affects the subject's ability to
- •participate in the trial.
- •Subjects with a history of alcohol or drug abuse in the past 2 years.- Subjects who have donated blood in the past 60 days.
- •Subjects who have previously received boceprevir.
- •Subjects who are currently participating in another clinical study or have
- •participated in a clinical study (e.g., laboratory or clinical evaluation) within 30 days of baseline.
- •Subjects who are part of the study staff personnel or family members of the
- •study staff personnel.
- •Subjects who have demonstrated allergic reactions (eg, food, drug, atopic
- •reactions or asthmatic episodes) which, in the opinion of the investigator and
- •sponsor, interfere with their ability to participate in the trial.
- •Subjects who smoke more than 10 cigarettes or equivalent tobacco use per
- •Subjects who have a history of malignancy.
- •Subjects who have received any prohibited treatment (prescription and non prescription medication except acetaminophen, potent inhibitors and inducers of cytochrome P3A [CYP3A4], or vitamins and herbals) more recently than the indicated washout period prior to Randomization which, in the opinion of the investigator and sponsor, interferes with their ability to participate in the trial.
研究组 & 干预措施
Boceprevir Tablets then Capsules (fed)
Participants will start therapy with a single dose of boceprevir tablets, orally, in fed condition, and then 4 days later will take a single dose of boceprevir capsules, orally, in fed condition.
干预措施: boceprevir (Drug)
Boceprevir Capsules then tablets (fed)
Participants will start therapy with a single dose of boceprevir capsules, orally, in fed condition, and then 4 days later will take a single dose of boceprevir tablets, orally, in fed condition.
干预措施: boceprevir (Drug)
Boceprevir Tablets then Capsules (fasted)
Participants will start therapy with a single dose of boceprevir tablets, orally, following an overnight fast, and then 4 days later will take a single dose of boceprevir capsules, orally, following an overnight fast.
干预措施: boceprevir (Drug)
Boceprevir Capsules then Tablets (fasted)
Participants on this study arm will start therapy with a single dose of boceprevir capsules, orally, following an overnight fast, and then 4 days later will take a single dose of boceprevir tablets, orally, following an overnight fast.
干预措施: boceprevir (Drug)
结局指标
主要结局
Area Under the Concentration Curve (AUC) From Hour 0 to the Final Quantifiable Sample (AUCtf) for Boceprevir Tablets Versus Capsules in Fed State
时间窗: Predose through 72 hours post-dose
AUC is the measure of total plasma exposure of a drug over a given time period. AUC is derived from the area under the plasma drug concentration-time curve.
Maximum Plasma Concentration (Cmax) of Boceprevir Tablets Versus Capsules in Fed State
时间窗: Predose through 72 hours post-dose
Cmax is the highest plasma drug concentration observed on the plasma concentration-time curve.
AUCtf for Boceprevir Tablets Versus Capsules in Fasted State
时间窗: Predose through 72 hours post-dose
AUC is the measure of total plasma exposure of a drug over a given time period. AUC is derived from the area under the plasma drug concentration-time curve.
Cmax of Boceprevir Tablets Versus Capsules in Fasted State
时间窗: Predose through 72 hours post-dose
Cmax is the highest plasma drug concentration observed on the plasma concentration-time curve.
Half Life (t1/2) of Boceprevir in Fed State
时间窗: Predose through 72 hours post-dose
T1/2 is the time required for a given drug concentration to decrease by 50%.
AUC From Hour 0 to Infinity (AUCinf) in Fed State
时间窗: Predose through 72 hours post-dose
AUC is the measure of total plasma exposure of a drug over a given time period. AUC is derived from the area under the plasma drug concentration-time curve.
AUCinf in Fasted State
时间窗: Predose through 72 hours post-dose
AUC is the measure of total plasma exposure of a drug over a given time period. AUC is derived from the area under the plasma drug concentration-time curve.
t1/2 Boceprevir in Fasted State
时间窗: Predose through 72 hours post-dose
T1/2 is the time required for a given drug concentration to decrease by 50%.
次要结局
未报告次要终点