COVID-19 PneumoniaPhase 1NCT05685719
A Study to Evaluate the Relative Bioavailability of STI-1558 and the Effect of Itraconazole and Rifampin on the Pharmacokinetics of STI-1558
A Phase 1 study testing STI-1558, Itraconazole and Rifampin in people with COVID-19 Pneumonia, run by Zhejiang ACEA Pharmaceutical Co. Ltd. at 1 site in China.
Trial summary
This is an open-label study. This study includes 2 parts, in which part 1 is a relative BA study, Part 2 is a DDI study. Part 1 and Part 2 could be performed in parallel. Read more about this study
- Who is it for?
- Ages 18 to 45 yearsHealthy volunteers can take part
- Conditions the study is for
- COVID-19 Pneumonia
- What is being tested?
- STI-1558, Itraconazole and Rifampin
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 37 participants
- Where
- 1 siteChina
- Study dates
- 4 Jan 2023to 3 Nov 2023
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 45 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Subjects are fully informed of the study and are willing to participate in the study and sign the informed consent document prior to any procedure.
- Healthy male and female subjects, aged 18 to 45 years (both inclusive).
- Body mass index (BMI) is between 19 and 24 kg/m2 (both inclusive), and body weight of female subjects ≥ 45 kg, body weight of male subjects ≥ 50 kg.
- Health status is good, the medical history, vital signs, physical examination, 12- lead ECG, laboratory tests (hematology, blood glucose, blood biochemistry, urinalysis, coagulation test), thyroid function (TSH, FT3, FT4) and serum virology test results are normal or abnormal with no clinical significance (NCS) during the screening period.
- Female subjects of child-bearing potential must agree to use highly effective contraceptive methods from the screening period to 30 days after the last dose of the study drug, (See Appendix 2 Contraceptive Methods).
- Male subjects considered fertile must agree to not plan to father a child, not donate sperm, and take effective contraceptive methods from the screening period to 30 days after the last dose of the study drug, (See Appendix 2 Contraceptive Methods).
- Subjects who are able to communicate well with PI, as well as understand and adhere to the requirements of this study.
Who cannot join
- Difficulties in venous blood collection or history of dizziness when encountering blood or needles.
- Known or suspected pregnancy, or breastfeeding.
- Has a clinically relevant intolerance or allergy to drugs, or are known or suspected to have hypersensitivity to any ingredient in the STI-1558.
- Only for Part 2: Known or suspected hypersensitivity to any ingredient in formulations of itraconazole and/or rifampicin (See the product label for the relevant information).
- Has received an experimental agent (vaccine, drug, biologic, device, blood product or medication) within 1 month or 5 times half-life (whichever is longer) before the first dose of study drug.
- Has a history of gastrointestinal (such as duodenal ulcer, alimentary tract hemorrhage, etc.), liver or kidney disease, or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs as determined by the Principal Investigator (PI, or designee).
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- Has a medical history of other significant diseases (including but not limited to respiratory, circulatory, digestive, hematological, endocrinological, immunological, dermatological, mental and nervous systems, facial diseases and other related diseases).
- Has a major surgery within 3 months before the first dose of the study drug or plans to undergo surgery during the study.
- Has a history of febrile illness within 14 days before the first dose of the study drug.
- Has values above the 1.5 × upper limits of normal (ULN) at screening or Day -1 for the following laboratory measures: alanine aminotransferase (ALT), aspartate aminotransferase (AST), and/or total bilirubin.
- QTcF interval is prolonged at screening or Day -1 (male: QTcF interval ≥ 450 ms, female: QTcF interval ≥ 470 ms).
- Vaccinated within 14 days before the first dose of the study drug or plans to be vaccinated during the study.
- Use of BCRP substrates within 7 days before the first dose of the study drug (see Appendix 3).
- Use of CYP3A4 strong inducers or inhibitors, or CYP1A2 strong inducers within 7 days before the first dose of the study drug (see Appendix 3).
- Any marketed medication (prescription and nonprescription) within 14 days or 5 times the half-life (whichever is longer) before the first dose of study drug. (Excluding oral contraceptives, or topical ointments at the discretion of the PI (or designee)).
- A known history of drug abuse within 2 years before the screening; or positive drug abuse test on Day -1.
- Blood donation or blood loss of more than 400 mL within 3 months before the screening (excluding menstrual blood loss of women).
- Weekly alcohol consumption of more than 14 units of alcohol (1 unit of alcohol = 360 mL of beer or 45 mL of spirit with the alcohol content of 40% or 150 mL of wine) in any week within the past 3 months before screening; or intake of alcohol- containing products within 48 hours before the first dose of the study drug, or cannot abstain from any alcohol product during the study, or positive breath alcohol test on Day -1.
- Smoking history (≥ 5 cigarettes per day) within 3 months before the screening, or cannot abstain from any tobacco products during the study.
- Excessive drinking of tea, coffee, or caffeine-containing beverage (at least 8 cups per day, 1 cup=250 mL) within 3 months before screening; intake of rich caffeine- or xanthine-containing food or drinks (e.g., coffee, tea, chocolate, cola drinks) within 48 hours before the first dose of the study drug.
- Intake of food, juice, or drink containing grapefruit, lime, cinchona peel, or quinine within 48 h before the first dose of the study drug.
- The results of serum virology test are positive or exceed the upper limit of the reference range, including: hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV) antibody, human immunodeficiency virus (HIV) antibody, or treponema pallidum antibody (TP-Ab).
- Subjects who are judged as not eligible to participate in this study by the PI (or designee).
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Study to Evaluate the Relative Bioavailability of Different Strengths of STI-1558 Capsules and the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and Inducer (Rifampin) on the Pharmacokinetics of STI-1558 in Healthy Volunteers
This is an open-label study. This study includes 2 parts, in which part 1 is a relative BA study, Part 2 is a DDI study. Part 1 and Part 2 could be performed in parallel.
- Conditions
- COVID-19 Pneumonia
- Being tested
- STI-1558, Itraconazole, Rifampin
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
STI-1558Drug
An oral small molecule prodrug that effectively inhibits the SARS-CoV-2 main protease (Mpro).
ItraconazoleDrug
A strong CYP3A4 inhibitor
RifampinDrug
A strong CYP3A4 inducer
| Study group | Role | What they receive |
|---|---|---|
| Part 1: TR | Experimental | Subjects will take a single dose of test product 200mg/capsule on Day 1 of the study, then reference product 100mg/capsule on Day 8 of the study. Receives: Drug: STI-1558 |
| Part 1: RT | Experimental | Subjects will take a single dose of reference product 100mg/capsule on Day 1 of the study, then test product 200mg/capsule on Day 8 of the study. Receives: Drug: STI-1558 |
| Part 1: Group 1 | Experimental | Subjects will take a single dose of STI-1558 200mg/capsule on Day 1. Starting from Day 4, subjects will orally take 200mg of itraconazole, q.d, for 6 consecutive days (Day 4 to Day 9). The 5th dose (Day 8) of itraconazole will be co-administered with STI-1558 (200 mg/capsule × 3 capsules) to subjects. Receives: Drug: STI-1558; Drug: Itraconazole |
| Part 1: Group 2 | Experimental | Subjects will take a single dose of STI-1558 200mg/capsule on Day 1. Starting from Day 4, subjects will orally take 600mg of rifampin, q.d, for 9 consecutive days (Day 4 to Day 12). The 8th dose (Day 11) of rifampin will be co-administered with STI-1558 (200 mg/capsule × 3 capsules) to subjects. Receives: Drug: STI-1558; Drug: Rifampin |
What is being measured
The primary outcome is the main question the study is designed to answer.
Comparison of Area Under the Curve (AUC) from time 0 to last time point(AUC0-t) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
To compare AUC0-t of a single 600mg dose of two different oral strength of STI-1558（200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules）in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Measured: Up to 2 weeks.
Comparison of AUC from time 0 extrapolated to infinity(AUC0-inf ) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
To compare AUC0-inf of a single 600mg dose of two different oral strength of STI-1558（200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules）in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Measured: Up to 2 weeks.
Comparison of maximum observed concentration(Cmax) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
To compare Cmax of a single 600mg dose of two different oral strength of STI-1558（200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules）in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Measured: Up to 2 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the pharmacokinetics(PK) of STI-1558 by collecting serum at protocol-specified time points: Cmax
Measured: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-t
Measured: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-inf.
Measured: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: Cmax
Measured: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-t
Measured: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-inf
Measured: Up to 3 weeks.
Secondary outcomes (3)
Cmax of AC1115(an active metabolite of STI-1558)
Measured: Up to 2 weeks for part 1 and 3 weeks for part 2.
AUC0-t of AC1115(an active metabolite of STI-1558)
Measured: Up to 2 weeks for part 1 and 3 weeks for part 2.
AUC0-inf of AC1115(an active metabolite of STI-1558)
Measured: Up to 2 weeks for part 1 and 3 weeks for part 2.
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted17 Jan 2023
- Study start4 Jan 2023
- Primary completion15 Mar 2023
- Study completion3 Nov 2023
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for COVID-19 PneumoniaStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 37 participants (actual)
Sponsor and investigators
- Lead sponsor
- Zhejiang ACEA Pharmaceutical Co. Ltd.
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT05685719
- Sponsor's protocol ID
- MPR-COV-102CN
- Status last verified
- Dec 2023
- First submitted
- 21 Dec 2022
- Last updated
- 7 Dec 2023
- Results posted
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- No
Study at a glance
From the registry record, last updated by the sponsor on 7 Dec 2023. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Study to Evaluate the Relative Bioavailability of Different Strengths of STI-1558 Capsules and the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and Inducer (Rifampin) on the Pharmacokinetics of STI-1558 in Healthy Volunteers
- ClinicalTrials.gov ID
- NCT05685719
- Acronym / sponsor ID
- MPR-COV-102CN
- Conditions
- COVID-19 Pneumonia
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 37 participants (actual)
- Lead sponsor
- Zhejiang ACEA Pharmaceutical Co. Ltd.Industry (pharma, biotech, devices)
- Study start
- 4 Jan 2023 (actual)
- Primary completion
- 15 Mar 2023 (actual)
- Study completion
- 3 Nov 2023 (actual)
- First posted
- 17 Jan 2023 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This is an open-label study. This study includes 2 parts, in which part 1 is a relative BA study, Part 2 is a DDI study. Part 1 and Part 2 could be performed in parallel.
Study design
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 4
| Arm | Type | Receives |
|---|---|---|
| Part 1: TR | Experimental | Drug: STI-1558Subjects will take a single dose of test product 200mg/capsule on Day 1 of the study, then reference product 100mg/capsule on Day 8 of the study. |
| Part 1: RT | Experimental | Drug: STI-1558Subjects will take a single dose of reference product 100mg/capsule on Day 1 of the study, then test product 200mg/capsule on Day 8 of the study. |
| Part 1: Group 1 | Experimental | Drug: STI-1558, Drug: ItraconazoleSubjects will take a single dose of STI-1558 200mg/capsule on Day 1. Starting from Day 4, subjects will orally take 200mg of itraconazole, q.d, for 6 consecutive days (Day 4 to Day 9). The 5th dose (Day 8) of itraconazole will be co-administered with STI-1558 (200 mg/capsule × 3 capsules) to subjects. |
| Part 1: Group 2 | Experimental | Drug: STI-1558, Drug: RifampinSubjects will take a single dose of STI-1558 200mg/capsule on Day 1. Starting from Day 4, subjects will orally take 600mg of rifampin, q.d, for 9 consecutive days (Day 4 to Day 12). The 8th dose (Day 11) of rifampin will be co-administered with STI-1558 (200 mg/capsule × 3 capsules) to subjects. |
Who may qualify
- Ages
- 18 to 45 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (7 listed)
- Subjects are fully informed of the study and are willing to participate in the study and sign the informed consent document prior to any procedure.
- Healthy male and female subjects, aged 18 to 45 years (both inclusive).
- Body mass index (BMI) is between 19 and 24 kg/m2 (both inclusive), and body weight of female subjects ≥ 45 kg, body weight of male subjects ≥ 50 kg.
- Health status is good, the medical history, vital signs, physical examination, 12- lead ECG, laboratory tests (hematology, blood glucose, blood biochemistry, urinalysis, coagulation test), thyroid function (TSH, FT3, FT4) and serum virology test results are normal or abnormal with no clinical significance (NCS) during the screening period.
- Female subjects of child-bearing potential must agree to use highly effective contraceptive methods from the screening period to 30 days after the last dose of the study drug, (See Appendix 2 Contraceptive Methods).
Key exclusion criteria (23 listed)
- Difficulties in venous blood collection or history of dizziness when encountering blood or needles.
- Known or suspected pregnancy, or breastfeeding.
- Has a clinically relevant intolerance or allergy to drugs, or are known or suspected to have hypersensitivity to any ingredient in the STI-1558.
- Only for Part 2: Known or suspected hypersensitivity to any ingredient in formulations of itraconazole and/or rifampicin (See the product label for the relevant information).
- Has received an experimental agent (vaccine, drug, biologic, device, blood product or medication) within 1 month or 5 times half-life (whichever is longer) before the first dose of study drug.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| STI-1558An oral small molecule prodrug that effectively inhibits the SARS-CoV-2 main protease (Mpro). | Drug | Part 1: Group 1, Part 1: Group 2, Part 1: RT, Part 1: TR |
| ItraconazoleA strong CYP3A4 inhibitor | Drug | Part 1: Group 1 |
| RifampinA strong CYP3A4 inducer | Drug | Part 1: Group 2 |
Primary outcome
Comparison of Area Under the Curve (AUC) from time 0 to last time point(AUC0-t) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
Time frame: Up to 2 weeks.
To compare AUC0-t of a single 600mg dose of two different oral strength of STI-1558（200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules）in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Comparison of AUC from time 0 extrapolated to infinity(AUC0-inf ) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
Time frame: Up to 2 weeks.
To compare AUC0-inf of a single 600mg dose of two different oral strength of STI-1558（200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules）in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Comparison of maximum observed concentration(Cmax) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
Time frame: Up to 2 weeks.
To compare Cmax of a single 600mg dose of two different oral strength of STI-1558（200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules）in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the pharmacokinetics(PK) of STI-1558 by collecting serum at protocol-specified time points: Cmax
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-t
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-inf.
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: Cmax
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-t
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-inf
Time frame: Up to 3 weeks.
3 secondary outcomes
Cmax of AC1115(an active metabolite of STI-1558)
Time frame: Up to 2 weeks for part 1 and 3 weeks for part 2.
AUC0-t of AC1115(an active metabolite of STI-1558)
Time frame: Up to 2 weeks for part 1 and 3 weeks for part 2.
AUC0-inf of AC1115(an active metabolite of STI-1558)
Time frame: Up to 2 weeks for part 1 and 3 weeks for part 2.
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 7 Dec 2023.
- Individual participant dataSharing planned: No
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
The record lists no contact. Use the official record to reach the sponsor.
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing STI-1558, Itraconazole and Rifampin in people with COVID-19 Pneumonia, run by Zhejiang ACEA Pharmaceutical Co. Ltd. at 1 site in China.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 7 inclusion and 23 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 7 Dec 2023. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in China. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Comparison of Area Under the Curve (AUC) from time 0 to last time point(AUC0-t) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability (time frame: Up to 2 weeks.). The study lists 9 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 7 Dec 2023; AzTrials last refreshed its copy on 6 Nov 2026.