NCT05489744

Human Mass Balance and Biotransformation Study of [14C]Afuresertib

In Vivo Absorption, Metabolism, Excretion (AME) Clinical Study of [14C]Afuresertib in Healthy Chinese Male Adults - Human Mass Balance and Biotransformation Study of [14C]Afuresertib

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 6 (actual)
• Sponsor: Laekna Limited · Industry
• Sex: Male
• Age: 18 Years – 45 Years
• Healthy volunteers: Accepted

Summary

This study adopts a single-center, single-dose, non-randomized, open-label design with a proposed enrollment of 6-10 healthy male subjects. After a single oral dose of approximately 125 mg/150 µCi \[14C\]Afuresertib tablets, blood, urine and fecal specimens are collected from each subject at defined time points/periods during the trial, and PK parameters, recovery, and excretion routes of \[14C\]Afuresertib in plasma are calculated by measuring the total radioactivity. The main metabolic and elimination pathways and characteristics of Afuresertib in human, as well as circulating metabolites with close to or higher than 10% of plasma total radioactivity exposure, are also identified by plasma, urine, and fecal radioactive metabolite profiles and major metabolite structure.

Detailed description

This study includes two stages: Stage I: The subjects are subject to the screening examination from D-7 to D-2. Two healthy adult male subjects selected from those who pass the examination are admitted to the clinical research center after qualification against the inclusion and exclusion criteria on D-2, and receive the baseline examination on D-1. After admission, they are trained on medication, urine and feces collection and other procedures to ensure that they can perform related operations in accordance with the protocol and operating manual for biospecimen analysis for mass balance and biotransformation study. Random urine and feces specimens (-24 h to 0 h) are collected on D-1 and the subjects are deprived of food for at least 10 h and water for 1 h before dosing. On the morning of the first day of the study, blood specimens are collected within 1 h before dosing, and the investigational product is taken orally on an empty stomach with 240 mL of warm water. The subjects are deprived of food for 4 h and water for 1 h after dosing. All urine and feces specimens excreted within the specified time intervals of 0-504 h and blood specimens sampled at specified time points before and within 0-504 h after dosing are collected. Phased testing is adopted in this study to determine whether specimen collection may be terminated in advance or the collection time needs to be prolonged based on the test results. If the specimen collection time exceeds 504 h, the collection should be extended at an interval of 24 h (urine, feces) or an integer multiple interval of 24 h (plasma) until the criteria for termination of specimen collection specified in the protocol are met. Meanwhile, the safety monitoring is continued until the completion date of the specimen collection. Stage II: According to the results of the Stage I study, the necessarily for plan adjustment (dosing regimen, biospecimen collection, etc.) is evaluated, and another 4-8 subjects will be selected if necessary.

Conditions

• Healthy Volunteer

Interventions

Type	Name	Description
DRUG	[14C]Afuresertib	Suspension containing approximately 125 mg of Afuresertib (containing 150 µCi of \[14C\]Afuresertib) is administered orally on an empty stomach, with approximately 240 mL of water for suspending and drug taking.

Timeline

• Start date: 2022-08-06
• Primary completion: 2022-10-21
• Completion: 2022-10-21
• First posted: 2022-08-05
• Last updated: 2023-05-15

Locations

1 site across 1 country: China