[14C] Study on Mass Balance and Biotransformation of STI-1558 in Healthy Chinese Adult Male Subjects
Condition: COVID-19
Study type: Interventional
Phase: Phase 1

Summary: 
      This trial adopts a single-center, single-dose, single-period, non-randomized, open-label
      study design. It is planned to enroll 6~8 healthy male subjects, and each subject receives
      single oral administration of drug solution containing 600mg/approximately 100µCi
      [14C]STI-1558 under fasting conditions on trial D1. The whole blood, plasma, urine and stool
      samples are collected at specified time points/intervals during the trial. The
      pharmacokinetic parameters of the total radioactivity in plasma and whole blood, the material
      concentration ratios of the total radioactivity in plasma and whole blood, and the material
      balances are obtained by testing the total radioactivity of [14C]STI-1558 in plasma, whole
      blood, urine and feces. Meanwhile, using isotope tracer and mass spectrometry techniques, the
      main pathways and characteristics of metabolism and elimination of STI-1558 in humans are
      obtained through the quantification of radioactive metabolite profiles and the structure
      identification of the main metabolites in plasma, urine and feces of the subjects. The entire
      duration of trial is expected to be 5 months.
    

Detailed description: 
      The experiment was carried out in two steps :

      Step 1 : Two qualified male subjects were enrolled in the study. After screening, the
      qualified subjects were admitted to the clinical research center after the D-2 was again
      verified by the inclusion and exclusion criteria. After admission, they were trained in
      medication, urine and feces collection procedures to ensure that they could perform relevant
      operations according to the program and SOP requirements. D-1 began to collect random urine
      samples ( -24 h~0 h ) and D-2 began to collect random fecal samples ( -48 h~0 h ). Subjects
      tested D1 morning fasting oral test drugs. All urine and feces samples excreted within the
      specified time interval of 0~336 h and blood samples at the specified time point of 0~168 h
      were collected. The test adopts the method of phased detection. According to the test
      results, it is judged whether the collection of blood, urine and feces samples can be
      terminated in advance or the collection needs to be continued. If the study finds that the
      collection time of biological samples exceeds the planned time ( i.e., blood 168 h, urine and
      feces 336 h ), the collection will be continued at an interval of 24 h ( or according to the
      researcher 's judgment, the integer multiple of 24 h ) until the judgment criteria for the
      termination of sample collection specified in the scheme are met. Safety monitoring continued
      until sample collection was completed.

      Step 2 : 4-6 qualified male subjects were selected and blood, urine and feces samples were
      collected at the specified time points / intervals. The operation is the same as the first
      step. According to the test results of the first step test, determine whether the test
      process needs to be adjusted.

      Criteria for terminating collection:

      Excreta : The total radioactivity of biological samples ( urine + feces ) collected from each
      subject exceeded 90 % of the dose, and the total radioactivity of biological samples ( urine
      + feces ) collected for two consecutive days was less than 1 % of the dose ; radioactive
      blood samples : plasma radioactive concentration < 3 times plasma background value.

      Finally, whether the subjects should terminate the collection of the corresponding samples
      was determined by the researchers based on the results of the radioactive test, the safety
      results and the actual situation, and the opinions of the sponsors.

      All subjects were required to complete the test procedure according to the program
      requirements during their stay in the clinical research center. The subjects who met the
      radioactive recovery conditions were collected in the laboratory examination samples, and no
      clinically significant abnormalities were found in the clinical observation, and the group
      could be confirmed by the researchers. If the abnormality is found to have clinical
      significance, the subjects will need to remain in the research center for observation or
      after the comprehensive evaluation of the researchers, agree to leave the research center and
      return to the hospital for regular review ( according to the requirements of the researchers
      ), follow-up until the normal or abnormal level is returned to normal or not clinically
      significant or acceptable to the researchers.
    

Intervention name(s): [14C]STI-1558
Intervention type(s): Drug
Intervention description(s): Fasting oral administration of 600 mg [ 14C ] STI-1558 ( about 100 μCi ) solution.
Intervention model: Single Group Assignment
Masking: None (Open Label)
Primary purpose: Treatment