NCT06627088已完成1 期

A Phase 1, Open-label, Two-part Study of the Absorption, Metabolism, Excretion, and Bioavailability of LY4100511 (DC-853) Following Administration of [14C]-LY4100511 in Healthy Male Participants

DICE Therapeutics, Inc., a wholly owned subsidiary of Eli Lilly and Company1 个研究点分布在 1 个国家目标入组 24 人开始时间: 2024年8月23日最近更新: 2025年1月24日

适应症

干预措施

试验速览

阶段: 1 期
状态: 已完成
发起方
入组人数: 24
试验地点: 1
主要终点: Part A: Pharmacokinetic (PK): Area Under the Concentration from Time 0 to Infinity (AUC0-∞) for TRA

研究概览研究设计入排标准研究组 & 干预措施结局指标研究者研究点记录与标识符相似试验

研究概览

简要总结

The study has two parts, Part A and Part B. The purpose of Part A is to determine the absorption, metabolism, and excretion (AME) of [14C]-LY4100511 and to characterize and determine the metabolites present in plasma, urine, and feces in healthy male participants after a single oral dose of LY4100511. The purpose of Part B is to determine the absolute bioavailability of LY4100511 in humans, to further analyze the rate and routes of excretion, including the mass balance, and to further investigate the pharmacokinetics (PK) of [14C]-LY4100511, LY4100511, and TRA.

研究设计

研究类型: Interventional
分配方式: Non Randomized
干预模型: Parallel
主要目的: Basic Science
盲法: None

入排标准

年龄范围: 18 Years 至 55 Years（Adult）
性别: Male
接受健康志愿者: 是

入选标准

•Body mass index between 18.0 and 32.0 kilogram per square meter (kg/m2), inclusive, and a body weight of ≥50 kilogram (kg)
•In good health and determined by no clinically significant finding from medical history, 12-lead ECG and vital signs measurements, and clinical laboratory evaluations (congenital nonhemolytic hyperbilirubinemia, e.g., suspicion of Gilbert's syndrome based on total and direct bilirubin is not acceptable) at screening and check-in, and from the physical examination at check-in, as assessed by the Investigator or designee
•History of a minimum of 1 bowel movement per day.
•Able to provide a fecal sample between check-in on Day-2 and oral dosing on Day 1.

排除标准

•Have a 12-lead ECG abnormality that, in the opinion of the Investigator
•increases the risks associated with participating in the study
•may confound ECG data analysis
•a QTcF & > 450 msec
•short PR interval & <120 msec or PR interval >220 msec
•second- or third-degree atrioventricular block
•intraventricular conduction delay with QRS 120 msec
•right bundle branch block
•left bundle branch block, or
•Wolff Parkinson-White syndrome.
•Have a current or recent acute, active infection (for example, for at least 30 days before screening and up to check-in, participants must have no symptoms or signs of infection in the absence of any anti-infective treatment).
•Had any malignancy within the past 5 years. Exceptions: successfully treated basal cell skin carcinoma or squamous cell skin carcinoma, with no evidence of recurrence or metastatic disease within the 3 years prior to baseline.
•Are immunocompromised.
•Have inflammatory bowel disease (IBD)

研究组 & 干预措施

Part A LY4100511 (tablet formulation) and [14C]-LY4100511 capsule

Experimental

Participants will receive a single oral dose 1 or dose 2 unlabeled LY4100511 (tablet formulation) administered with a dose 1 [14C]-LY4100511 capsule containing approximately 100 µCi (3.7 MBq) of radioactivity in the fasted state

干预措施: LY4100511 (DC-853) (Drug)

Part A LY4100511 (tablet formulation) and [14C]-LY4100511 capsule

Experimental

干预措施: [14C]-LY4100511 (DC-853) Administered oral dose (Drug)

Part B LY4100511 (tablet formulation) and [14C]-LY4100511

Experimental

Participants will receive a single oral dose 1 or dose 2 unlabeled LY4100511 (tablet formulation) in the fasted state, followed by a single intravenous (IV) dose of of [14C]-LY4100511, containing ≤1 μCi (≤37 kBq) of radioactivity, administered as an infusion.

干预措施: LY4100511 (DC-853) (Drug)

Part B LY4100511 (tablet formulation) and [14C]-LY4100511

Experimental

干预措施: [14C]-LY4100511 (DC-853) (Drug)

结局指标

主要结局

Part A: Pharmacokinetic (PK): Area Under the Concentration from Time 0 to Infinity (AUC0-∞) for TRA

时间窗: Up until Day 15

Part A: PK Area Under Concentration from 0 to Last Measurable Concentration (AUC0-tlast) for [14C] LY4100511

时间窗: Up until Day 15

Part A: Total Radioactivity Recovery and Excretion (TRA)

时间窗: Up until Day 15

Total radioactivity recovery and excretion (fet1-t2 and Aet1-t2) in urine and feces (and vomitus, if available)

Part A: Pharmacokinetic (PK): Area Under the Concentration from Time 0 to Infinity (AUC0-∞) for [14C] LY4100511

时间窗: Up until Day 15

Part A: Pharmacokinetic (PK): Area Under the Concentration from Time 0 to Infinity (AUC0-∞) for LY4100511

时间窗: Up until Day 15

Part A: PK Area Under Concentration from 0 to Last Measurable Concentration (AUC0-tlast) for LY4100511

时间窗: Up until Day 15

Part A: PK Area Under Concentration from 0 to Last Measurable Concentration (AUC0-tlast) for TRA

时间窗: Up until Day 15

Part A: PK Maximum Observed Plasma Concentration (Cmax) for [14C] LY4100511

时间窗: Up until Day 15

Part A: PK Maximum Observed Plasma Concentration (Cmax) for LY4100511

时间窗: Up until Day 15

Part A: PK Maximum Observed Plasma Concentration (Cmax) for TRA

时间窗: Up until Day 15

Part A: PK Time to Maximum Observed Plasma Concentration (tmax) for [14C] LY4100511

时间窗: Up until Day 15

Part A: PK Time to Maximum Observed Plasma Concentration (tmax) for LY4100511

时间窗: Up until Day 15

Part A: PK Time to Maximum Observed Plasma Concentration (tmax) for TRA

时间窗: Up until Day 15

Part B: Recovery of TRA in urine and feces

时间窗: Up until Day 6

Part A: PK Terminal Elimination Half Life (t1/2) for [14C] LY4100511

时间窗: Up until Day 15

Part A: PK Terminal Elimination Half Life (t1/2) for LY4100511

时间窗: Up until Day 15

Part A: PK Terminal Elimination Half Life (t1/2) for TRA

时间窗: Up until Day 15

Part A: Urinary Recovery and Excretion of TRA (Aet1-t2)

时间窗: Up until Day 15

Part A: Urinary Recovery and Excretion of [14C] LY4100511 (Aet1-t2)

时间窗: Up until Day 15

Part A: Renal clearance of [14C] LY4100511 (CLR)

时间窗: Up until Day 15

Part B: Pharmacokinetic (PK): absolute bioavailability (Fabs) of LY4100511

时间窗: Up until Day 6

Part B: Recovery of [14C]-LY4100511 in feces (Aet1-t2) following IV dosing

时间窗: Up until Day 6

Part B: Recovery of [14C]-LY4100511 in urine (Aet1-t2) following IV dosing

时间窗: Up until Day 6

Part B: PK Area Under Concentration from 0 to Last Measurable Concentration (AUC0-tlast) of LY4100511 following IV dosing

时间窗: Up until Day 6

Part B: PK Maximum Observed Plasma Concentration (Cmax) of LY4100511following IV dosing

时间窗: Up until Day 6

Part B: PK Time to Maximum Observed Plasma Concentration (tmax) of LY4100511following IV dosing

时间窗: Up until Day 6

Part B: PK Terminal Elimination Half Life (t1/2) following IV dosing

时间窗: Up until Day 6

Part B: PK Clearance (CL) following IV dosing

时间窗: Up until Day 6

Part B: PK renal clearance (CLr) following IV dosing [Time Frame: Up until Day 6]

时间窗: Up until Day 6

次要结局

Number of Participants with One or More Adverse Events (AEs), and Serious Adverse Events (SAEs) considered by the investigator to be related to study drug administration(Up until Day 8)

研究者

发起方

DICE Therapeutics, Inc., a wholly owned subsidiary of Eli Lilly and Company

申办方类型

Industry

责任方

Sponsor

研究点 (1)

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