A Phase 1, Multi-cohort, Open-label Study to Evaluate the Relative Bioavailability of Capsule and Tablet Formulations of TYRA-300-B01, and to Evaluate the Safety, Tolerability, and Food Effect of TYRA-300-B01 Tablets in Healthy Adult Participants
试验速览
- 阶段
- 1 期
- 状态
- 进行中（未招募）
- 入组人数
- 60
- 试验地点
- 1
- 主要终点
- Pharmacokinetics single-dose Cmax
研究概览
简要总结
The purpose of this study is to evaluate the relative bioavailability of capsule and tablet formulations of TYRA-300-B01, and to evaluate the safety, tolerability, and food effect of TYRA-300-B01 tablets in healthy adult participants.
详细描述
This is a Phase 1, multi-cohort trial studying TYRA-300-B01, a novel, potent fibroblast growth factor receptor (FGFR) 3-selective tyrosine kinase inhibitor, in healthy, adult participants. The purpose of this study is to evaluate the relative bioavailability of capsule and tablet formulations of TYRA-300-B01, and to evaluate the safety, tolerability, and food effect of TYRA-300-B01 tablets in healthy adult participants.
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
- 26 Years 至 55 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Males or females of non-childbearing potential, between 18 and 55 years of age
- •In good health, determined by no clinically significant findings from medical history, 12-lead electrocardiogram (ECG), vital signs, and clinical laboratory assessments
- •Body mass index (BMI) 18 to 32 kg/m^2 (inclusive)
- •Cohorts 1 and 2 ethnicity requirements: none
- •Cohort 3 ethnicity requirements: first- or second-generation Japanese participants
排除标准
- •Significant history of any hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, immunologic, musculoskeletal disease, or allergic disease (as determined by the Investigator)
- •Any ocular condition likely to increase the risk of eye toxicity
- •Gastrointestinal disorders that will affect oral administration or absorption of TYRA-300-B01
- •Females of child-bearing potential and males who plan to father a child while enrolled in this study
研究组 & 干预措施
Bioavailability Tablet vs Capsule Formulation
TYRA-300-B01 single oral dose of tablet or capsule crossover followed by twice-daily tablet dosing
干预措施: TYRA-300-B01 (Drug)
Food Effect Tablet Formulation
TYRA-300-B01 single oral dose of tablet in the fed and fasted state
干预措施: TYRA-300-B01 (Drug)
Pharmacokinetic Tablet Formulation
TYRA-300-B01 single oral dose
干预措施: TYRA-300-B01 (Drug)
Pharmacokinetic Mini-Tablet Formulation
TYRA-300-B01 multiple-dose mini-tablet formulation
干预措施: TYRA-300-B01 (Drug)
结局指标
主要结局
Pharmacokinetics single-dose Cmax
时间窗: Up to 48 hours post-dose
maximum plasma concentration (Cmax)
Pharmacokinetics multiple-dose Cmin
时间窗: Up to 24 hours post-dose
average steady-state trough plasma concentration (Cmin)
Pharmacokinetics multiple-dose RAUC
时间窗: Up to 24 hours post-dose
accumulation ratio for AUC
Pharmacokinetics multiple-dose Cmax
时间窗: Up to 24 hours post-dose
maximum steady-state plasma concentration (Cmax)
Pharmacokinetics single dose Tmax
时间窗: Up to 48 hours post-dose
time to reach maximum plasma concentration (Tmax)
Pharmacokinetics single and multiple dose AUC
时间窗: Up to 48 hours post-dose
area under the plasma concentration-time curve (AUC)
Pharmacokinetics single dose CL/F
时间窗: Up to 48 hours post-dose
apparent total clearance (CL/F)
Pharmacokinetics single dose Vz/F
时间窗: Up to 48 hours post-dose
apparent volume of distribution (Vz/F)
Pharmacokinetics single dose t1/2
时间窗: Up to 48 hours post-dose
half-life of TYRA-300
Pharmacokinetics multiple-dose RCmax
时间窗: Up to 24 hours post-dose
accumulation ratio for Cmax (RCmax)
次要结局
- Safety and tolerability(Initiation of study treatment up to 7-days post treatment)