This study is divided into two parts, including Part I: a randomized, open-label,positive drug-controlled, single ascending dose (SAD) study, a food effect (FE) study,and Part II: a randomized, double-blind, placebo-controlled, multiple ascending dose(MAD) study.
Part I: Single Ascending Dose (SAD) and Food Effect (FE) Study Combined SAD and FE Study
(N=42): The SAD portion is integrated with the FE study, comprising 5 dose groups: 20 mg,
80 mg, 160 mg, 300 mg, and 600 mg. The trial commences with the low-dose group and in a
sequential manner. As subjects in a given dose group of CX2101A complete their safety
assessments, the investigator evaluates whether the low-dose group has met the
dose-escalation termination criteria. If not, the trial escalates to the next dose level.
SAD Study Enrollment: The SAD study aims to enrolls a total of 42 healthy subjects. The
20 mg dose group will enroll 4 subjects, while the 80 mg, 160 mg, and 600 mg dose groups
will each enroll 8 subjects. These subjects will be randomly assigned to receive either
CX2101A enteric-coated tablets or intravenous remdesivir in a 3:1 ratio.
FE Study for the 300 mg Dose Group: The 300 mg dose group will concurrently conduct a
study of food effect on the pharmacokinetics (PK) of CX2101A enteric-coated tablets. This
study plans to enroll 14 subjects, who will be randomly assigned to receive either
CX2101A enteric-coated tablets (12 subjects) or intravenous remdesivir (2 subjects). In
the first period, all 14 subjects will receive a single dose under fasting conditions
according to the randomization schedule and will have blood samples collected. The 12
subjects receiving CX2101A enteric-coated tablets will undergo a 7-day washout period
with a potential adjustment based on PK data from prior dose groups before proceeding to
the second period, where they will receive the drug under fed conditions, complete blood
sample collection, and undergo safety assessments.
Part II: Multiple Ascending Dose (MAD) Study MAD Study Design: The MAD study will include
2 dose groups, 100 mg and 300 mg. It plans to enroll 20 healthy adult subjects, with 10
subjects in each dose group. These subjects will be randomly assigned to receive either
CX2101A enteric-coated tablets (8 subjects) or CX2101A placebo (2 subjects). The study
will involve continuous dosing for 5 days. If the subjects in the first dose group
complete their safety assessments and the investigator determines that the
dose-escalation termination criteria have not been met, the study will escalate to the
next dose level.
Drug: Remdesivir
Intravenous remdesivir 100 mg
Drug: CX2101A
CX2101A enteric-coated tablet
Drug: Placebo
CX2101A placebo enteric-coated tablet
Inclusion Criteria:
1. Healthy volunteers aged between 18 and 55 years old (including 18 and 55 years old),
regardless of gender.
2. For male volunteers, the body weight should be ≥ 50.0 kg, and for female volunteers,
the body weight should be ≥ 45.0 kg. The body mass index (BMI) = body weight (kg) /
height² (m²), and it should be within the range of 19.0 to 28.0 kg/m². Women of
childbearing potential (WOCBP) or the female partners of male subjects should be
willing to have no plans for childbearing from 2 weeks before the screening until 3
months after the last administration of the investigational medicinal product, and
voluntarily adopt effective contraceptive measures (including one or more
non-pharmacological contraceptive measures), and have no plans for sperm donation or
egg donation.
3. No history of major diseases, and the results of physical examination, vital signs,
12-lead electrocardiogram, chest X-ray examination and laboratory tests during the
screening period are normal, or although slightly beyond the normal reference value
range, they are judged by the investigator to have no clinical significance.
4. The subject should be able to maintain good communication with the investigator,
comply with various requirements of the clinical trial, and voluntarily sign the
informed consent form.
Exclusion Criteria:
1. Diseases with abnormal clinical manifestations that occurred before screening or are
currently occurring and need to be excluded, including but not limited to those in
the nervous/mental system, respiratory system, cardiovascular and cerebrovascular
system, digestive system (any history of gastrointestinal diseases that affect drug
absorption), hematological and lymphatic system, urinary system, endocrine system,
and immune system.
2. Acute diseases that occurred from the screening stage to before the administration
of the investigational medicinal product and are judged by the investigator to
possibly affect the research results.
3. Subjects who cannot tolerate intravenous puncture or those with a history of syncope
judged by the investigator to be of clinical significance.
4. Subjects with difficulty in swallowing.
5. Subjects who are judged by the investigator to possibly or definitely have an
allergic reaction to the investigational drug, remdesivir (including similar drugs),
or any of its excipients; or subjects with an allergic constitution judged by the
investigator to be of clinical significance (a history of severe allergies to
multiple drugs and foods) or a history of allergic diseases.
6. Subjects who have undergone surgery before screening and are judged by the
investigator to possibly affect the absorption, distribution, metabolism, and
excretion of the drug, or subjects with severe surgical sequelae, or subjects who
plan to undergo surgery during the study period.
7. Subjects who donated blood or had massive blood loss (≥ 400 mL), donated ≥ 2 units
of component blood, or received a blood transfusion within 3 months before the first
administration of the trial, or those who plan to donate blood during the trial.
8. Subjects who received any investigational drug in a clinical study or participated
in any interventional clinical study within 3 months before the first administration
of the trial.
9. Subjects who smoked an average of more than 5 cigarettes per day within 3 months
before the first administration of the trial, or those who cannot stop using any
tobacco products during the trial.
10. Subjects who consumed an average of more than 14 units of alcohol per week within 3
months before the first administration of the trial (1 unit of alcohol ≈ 360 mL of
beer or 45 mL of spirits with an alcohol content of 40% or 150 mL of wine), or those
who cannot stop using any alcohol-containing products during the trial, or those
with a positive alcohol breath test before the administration of the trial.
11. Subjects who consumed an excessive amount of tea, coffee, and/or caffeine-containing
beverages on average per day (more than 8 cups on average, 1 cup ≈ 250 mL) within 3
months before the first administration of the trial, or those who cannot stop
consuming tea, coffee, and/or caffeine-containing beverages during the trial.
12. Subjects who used any prescription drugs, over-the-counter drugs, traditional
Chinese patent medicines, Chinese herbal medicines, vitamins, or health foods within
28 days before screening or within 5 drug half-lives (whichever is longer).
13. Female subjects who are pregnant or breastfeeding, or those with a positive
blood/urine pregnancy test (only for WOCBP) at any time before the first
administration.
14. Positive results or results exceeding the upper limit of the reference range for the
four hemodialysis tests: hepatitis B surface antigen (HBsAg), quantitative hepatitis
C (HCV) antibody, quantitative human immunodeficiency virus (HIV) antibody, or
treponema pallidum antibody.
15. Subjects with a positive urine drug screening (morphine, tetrahydrocannabinolic
acid, methamphetamine, methylenedioxymethamphetamine, ketamine) or those with a
history of drug abuse or drug use within the past 5 years before the trial.
16. Subjects who consumed or drank pitaya, mango, pomelo, carambola, or foods or
beverages prepared from them, or foods or beverages containing xanthine, caffeine,
or alcohol (including chocolate, tea, coffee, cola, cocoa, etc.), or other special
diets that affect the absorption, distribution, metabolism, and excretion of the
drug within 72 hours before the first administration.
17. Subjects with special dietary requirements, lactose intolerance, or those who cannot
accept the unified diet.
18. Subjects who, according to the investigator's judgment, are not suitable to
participate in this trial.
Zhejiang Xiaoshan Hospital
Hangzhou, Zhejiang, China
Not Provided