Official Title
A Randomized, Open, Two-sequence, Two-cycle, Double-cross Design Bioequivalence Trial of Fasting Single Oral STI-1558 Capsule in Healthy Chinese Subjects
Brief Summary

This study is a randomized, open, single-dose, two-sequence, two-cycle, double-crossdesign bioequivalence study.32 eligible subjects will be randomly assigned to TR group and RT group in a 1:1 ratio.Subjects in the TR group will take the test preparation (T) 200 mg/ pill × 1 pill on day1 (D1) and the reference preparation (R) 200 mg/ pill × 1 pill on day 8 (D8). Thesequence of medication in RT group is reversed from TR group. Wash for at least 7 daysbetween doses.Screening was performed within 28 days prior to initial dosing, and all eligible subjectswere admitted to the clinical research Center 1 day prior to Cycle 1 dosing (D-1) anddischarged on day 10 of the study (D10) after completing Cycle 2 PK blood collection,corresponding safety examination, and evaluation. On the 14th day of the study (± 1 day),the clinical research center was returned for follow-up to further evaluate the safetyand tolerability of the subjects.

Detailed Description

This study is a randomized, open, single-dose, two-sequence, two-cycle, double-cross
design bioequivalence study.

32 eligible subjects will be randomly assigned to TR group and RT group in a 1:1 ratio.
Subjects in the TR group will take the test preparation (T) 200 mg/ pill × 1 pill on day
1 (D1) and the reference preparation (R) 200 mg/ pill × 1 pill on day 8 (D8). The
sequence of medication in RT group is reversed from TR group. Wash for at least 7 days
between doses.

The trial drug STI-1558 should be taken with approximately 240 ml of water after fasting
overnight for at least 10h. Except for drinking water, water should be prohibited for at
least 1h before and after administration, and fasting should be at least 4h after
administration. Test drugs (T and R) must be swallowed whole and not chewed, crushed or
separated. In order to ensure the subject's compliance with the medication procedure, the
staff should check the subject's mouth after taking the medication.

Screening was performed within 28 days prior to initial dosing, and all eligible subjects
were admitted to the clinical research Center 1 day prior to Cycle 1 dosing (D-1) and
discharged on day 10 of the study (D10) after completing Cycle 2 PK blood collection,
corresponding safety examination, and evaluation. On the 14th day of the study (± 1 day),
the clinical research center was returned for follow-up to further evaluate the safety
and tolerability of the subjects.

Completed
COVID-19

Drug: STI-1558

STI-1558 test preparation and reference preparation
Other Name: An oral small molecule prodrug that effectively inhibits the SARS-CoV-2 main protease (Mpro).

Eligibility Criteria

Inclusion Criteria:

1. The subject fully understands the purpose, nature, method and possible adverse
reactions of the test, voluntarily becomes a participant, and signs an informed
consent form (ICF) before the start of any procedure;

2. Healthy adult males or females aged 18-45 years (including the threshold) at the
time of signing the ICF;

3. At the time of signing the ICF and on the day of hospitalization, the body mass
index (BMI) is 19-24 kg/m2 (including the threshold), and the weight is not less
than 45 kg for women and not less than 50 kg for men;

4. Good health with normal or abnormal results of history, vital signs, physical
examination, 12-lead ECG, laboratory tests (blood routine, blood glucose, blood
biochemistry, urine routine and coagulation tests) and hemodialysis during the
screening period (NCS);

5. Fertile Women (WOCBP) subjects must consent to the use of one or more effective
contraceptive methods from the screening period to 30 days after the last dose;

6. Fertile male subjects must consent to the use of one or more effective contraceptive
methods within 30 days from the first dose to the last dose;

7. The subject is able to communicate well with the investigator (or designee) and
understands and complies with the requirements of the study.

Exclusion Criteria:

1. Patients who have difficulty in venous blood collection or have a history of needle
fainting or blood fainting;

2. Pregnant or lactating;

3. Allergic constitution or allergic to any ingredient in STI-1558 capsule preparation;

4. Within 1 month prior to screening or within 5 half-lives of the drug (subject to
older age) and those who have been enrolled in other clinical trials (including but
not limited to investigational drugs, vaccines, biologics, devices, blood products,
etc.);

5. Have a history of gastrointestinal (such as duodenal ulcer, gastrointestinal
bleeding), liver or kidney related, or other medical history that the investigator
(or his designee) determines may affect the absorption, distribution, metabolism,
and excretion of oral drugs;

6. Have any clinical history of serious diseases (including but not limited to
respiratory system, circulatory system, digestive system, blood system, endocrine
system, immune system, skin and mucosal system, psychiatric nervous system, ent
department and other related diseases);

7. Those who underwent major surgery within 3 months prior to screening, or did not
fully recover from surgery, or planned to have surgery during the study period;

8. Within 14 days prior to screening and screening of patients with a history of fever;

9. QT interval prolongation: QTcF > 450 msec (male); QTcF > 470 msec (female);

10. Those who were vaccinated within 14 days prior to screening and those who were
screened until check-in or planned to be vaccinated during the study period;

11. Within 7 days before screening and screening of patients who have used BCRP
substrate drugs;

12. Those who have used CYP3A4 inhibitor, strong inducer, or CYP1A2 inhibitor within 7
days prior to screening and those who have been screened;

13. Within 14 days prior to screening or within 5 half-lives of the drug (whichever is
older), and to those who have been admitted to use any other prescription,
over-the-counter or Chinese herbal medicine (other than contraceptive drugs or
topical drugs assessed by the investigator to be applicable);

14. Had a history of drug abuse within 2 years prior to screening, or tested positive
for drug abuse upon admission (D-1);

15. Patients with a history of blood donation or blood loss (excluding female menstrual
blood loss) exceeding 400 mL within 3 months before screening;

16. Those who consumed more than 14 units of alcohol per week in the 3 months prior to
screening (1 unit of alcohol =360 mL beer or 45 mL spirits with 40% alcohol or 150
mL wine), or had consumed alcoholic products within 48 hours prior to the first
dose, or were unable to abstinent during the study period, or tested positive for
alcohol breath test at admission (D-1);

17. Smokers who smoked more than 5 cigarettes per day in the 3 months before screening,
or who could not guarantee no smoking during the trial period;

18. Excessive consumption of tea, coffee or caffeinated beverages (defined as: at least
8 cups per day, 1 cup =250 ml) in the 3 months prior to screening, or intake of
caffeine or xanthine-rich foods or beverages (such as coffee, tea, chocolate, cola,
etc.) within 48 hours prior to the first dose;

19. Consumed food, juice or drink containing grapefruit, lime, cinchona peel or quinine
within 48 hours before screening and until check-in;

20. Positive or above the upper limit of the reference range for four hemodialysis
tests, including hepatitis B surface antigen (HBsAg), hepatitis C (HCV) antibodies,
human immunodeficiency virus (HIV) antibodies or treponema pallidum antibodies;

21. Other circumstances in which the investigator (or his designee) deems it
inappropriate to participate in the study.

Eligibility Gender
All
Eligibility Age
Minimum: 18 Years ~ Maximum: 45 Years
Countries
China
Locations

Zhejiang Xiaoshan Hospital
Hangzhou 1808926, China

Chen Jian, master, Study Chair
Zhejiang Hospital

Zhejiang ACEA Pharmaceutical Co. Ltd.
NCT Number
MeSH Terms
COVID-19
STI-1558