A Bioequivalence Trial of Fasting Single Oral STI-1558 Capsule in Healthy Chinese Subjects

NCT06044233 | Completed Phase 1

• 1 other identifier: MPR-COV-105CN
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

Brief Summary

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. 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.

Conditions

COVID-19

Outcome Measures

Primary Outcomes (3)

• Comparison of maximum observed concentration(Cmax) profiles of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  To compare Cmax of 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) in healthy adult , human subjects under fasting conditions, to establish relative bioavailability.

  Up to 2 weeks

• Comparison of Area Under the Curve (AUC) from time 0 to last time point(AUC0-t) profiles of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  To compare AUC0-t of 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) in healthy adult , human subjects under fasting conditions, to establish relative bioavailability.

  Up to 2 weeks

• Comparison of AUC from time 0 extrapolated to infinity(AUC0-inf ) profiles of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  To compare AUC0-inf of 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) in healthy adult , human subjects under fasting conditions, to establish relative bioavailability.

  Up to 2 weeks

Secondary Outcomes (4)

• Comparison of Tmax of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  Up to 2 weeks

• Comparison of t1/2 of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  Up to 2 weeks

• Comparison of λz of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  Up to 2 weeks

• Comparison of %AUCex of two different kinds of oral STI-1558 to determine the Relative Bioavailability

  Up to 2 weeks

Study Arms (2)

TR group

EXPERIMENTAL

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).

Drug: STI-1558

RT group

EXPERIMENTAL

Subjects in the RT group will take the reference preparation (R) 200 mg/ pill × 1 pill on day 1 (D1) and the test preparation (T) 200 mg/ pill × 1 pill on day 8 (D8).

Drug: STI-1558

Interventions

STI-1558 DRUG

STI-1558 test preparation and reference preparation

Also known as: An oral small molecule prodrug that effectively inhibits the SARS-CoV-2 main protease (Mpro).

RT group; TR group

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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;
• Healthy adult males or females aged 18-45 years (including the threshold) at the time of signing the ICF;
• 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;
• 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);
• 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;
• 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;
• The subject is able to communicate well with the investigator (or designee) and understands and complies with the requirements of the study.

You may not qualify if:

• Patients who have difficulty in venous blood collection or have a history of needle fainting or blood fainting;
• Pregnant or lactating;
• Allergic constitution or allergic to any ingredient in STI-1558 capsule preparation;
• 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.);
• 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;
• 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);
• 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;
• Within 14 days prior to screening and screening of patients with a history of fever;
• QT interval prolongation: QTcF \> 450 msec (male); QTcF \> 470 msec (female);
• 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;
• Within 7 days before screening and screening of patients who have used BCRP substrate drugs;
• Those who have used CYP3A4 inhibitor, strong inducer, or CYP1A2 inhibitor within 7 days prior to screening and those who have been screened;
• 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);
• Had a history of drug abuse within 2 years prior to screening, or tested positive for drug abuse upon admission (D-1);
• Patients with a history of blood donation or blood loss (excluding female menstrual blood loss) exceeding 400 mL within 3 months before screening;

Sponsors & Collaborators

• Zhejiang ACEA Pharmaceutical Co. Ltd.: lead

Study Sites (1)

Zhejiang Xiaoshan Hospital

Hangzhou, China

Location

MeSH Terms

Conditions

COVID-19

Interventions

STI-1558

Condition Hierarchy (Ancestors)

Pneumonia, Viral; Pneumonia; Respiratory Tract Infections; Infections; Virus Diseases; Coronavirus Infections; Coronaviridae Infections; Nidovirales Infections; RNA Virus Infections; Lung Diseases; Respiratory Tract Diseases

Study Officials

• Chen Jian, master

  Zhejiang Hospital

  STUDY CHAIR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 15, 2023
• First Posted: September 21, 2023
• Study Start: September 28, 2023
• Primary Completion: October 23, 2023
• Study Completion: November 8, 2023
• Last Updated: December 13, 2023

Record last verified: 2023-12

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)