Human Mass Balance and Biotransformation Study of [14C]Afuresertib
Condition: Healthy Volunteer
Study type: Interventional
Phase: Phase 1

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.
    

Intervention name(s): [14C]Afuresertib
Intervention type(s): Drug
Intervention description(s): 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.
Other intervention name(s): [14C]LAE002
Intervention model: Single Group Assignment
Masking: None (Open Label)
Primary purpose: Other
Keywords: Mass balance