This is a single-center, non-randomized, open-label, single-dose, Phase I clinical studyto evaluate the mass balance and biotransformation, safety and tolerability of WPV01 inhealthy adult chinese male participants following a single oral administration of [14C]WPV01.
This trial is planned to enroll 6-8 healthy Chinese male subjects. Each subject is
administered a single oral dose containing 600 mg/approximately 100 µCi [14C]WPV01
suspension on the first day of the trial in fasting condition.
Whole blood, plasma, urine and fecal samples are collected at defined time points/periods
during the test. The whole blood/plasma partition ratio, pharmacokinetic parameters of
total radioactivity in plasma, recovery and excretion pathway data of [14C]WPV01 are
calculated by measuring the total radioactivity. The major metabolic elimination pathways
and characterization of WPV01 in the human body, as well as circulating metabolites that
are close to or above 10% of total plasma radioactivity exposure, are obaitned from
structural characterization of plasma, urine and fecal radio-metabolite profiles and
major metabolites.
All excreted urine and fecal samples are collected at specified time intervals from 0 to
336h post-dose and and blood samples are collected at specified time points from 0 to
144h post-dose.
Drug: [14C]-WPV01
Single oral dose of 600 mg [14C]-WPV01
Inclusion Criteria:
- Healthy adult males
- Participants aged ≥18 years and ≤55 years old
- Body weight: Body mass index (BMI) between 19.0 and 26.0 kg/m2 (including borderline
values), body weight no less than 50.0 kg.
- Voluntarily participate in the clinical trial and sign the informed consent
- Able to communicate well with the investigator and able to complete the trial in
accordance with the protocol
Exclusion Criteria:
- Participants who have abnormalities and clinical significance after comprehensive
physical examination, vital signs, routine laboratory tests, thyroid function, chest
CT, abdominal ultrasound, etc.
- Participants whose 12-lead electrocardiogram test results show corrected QT interval
≥450 msec
- Participants who is positive for Hepatitis B Surface Antigen, Hepatitis C Antibody,
HIV Antibody and Syphilis Antibody
- Participants who have used any drug that inhibits or induces hepatic drug
metabolizing enzymes within 30 days prior to the screening period
- Participants who have used any prescription medication, over-the-counter medication,
herbal or dietary supplements, such as vitamins, calcium supplements, within 14 days
prior to the screening period
- Participants who have a history of any clinically serious disease or
disease/condition that, in the opinion of the investigator, may affect the results
of the test, including, but not limited to, a history of circulatory, respiratory,
endocrine, neurological, gastrointestinal, urological, or hematological,
immunological, psychiatric, and metabolic disorders
- Participants who have any condition that may affect drug absorption, e.g.,
gastrectomy, cholecystectomy, gastric bypass, duodenotomy, colectomy, history of
inflammatory bowel disease
- Participants who have history of organic heart disease, heart failure, myocardial
infarction, angina pectoris, unexplained arrhythmia, ventricular tachycardia,
atrioventricular block, QT prolongation syndrome, or symptoms of QT prolongation
syndrome, and a family history of the disease (as evidenced by genetic
predisposition or by the death of a close family member from a cardiac cause at a
young age).
- Participants who have undergone major surgery within 6 months prior to the screening
period or whose surgical incisions have not completely healed; major surgery
includes, but is not limited to, any surgery with significant risk of hemorrhage,
prolonged general anesthesia, or incisional biopsy or significant traumatic injury
- Participants who have specific allergic history, such as those with a known history
of allergy to two or more substances; or those who, in the judgment of the
investigator, may be allergic to the test drug or its excipients
- Participants who have perianal disease with regular/ongoing blood in stool,
irritable bowel syndrome, inflammatory bowel disease
- Participants who have habitual constipation or diarrhea
- Participants who are alcohol abusers or regularly drink alcohol in the 6 months
prior to the screening period, i.e., more than 14 units of alcohol per week (1 unit
= 360 mL of beer or 45 mL of spirits at 40% alcohol by volume or 150 mL of wine); or
an alcohol breath test result of >0 mg/dL at the time of the screening period
- Participants who smoked >5 cigarettes per day in the 3 months prior to the screening
period or habitually used nicotine-containing products and were unable to quit
during the trial period
- Participants who are substance abusers or use soft drugs (e.g., marijuana) in the 3
months prior to the screening period or use of hard drugs (e.g., cocaine,
amphetamines, phenylcyclohexylpiperidine, etc.) in the 1 year prior to the screening
period; or a positive urine drug test at the screening period
- Participants who consume grapefruit juice or excessive amounts of tea, coffee and/or
caffeinated beverages that cannot be stopped during the trial period
- Participants who are exposed to radiation for prolonged periods of time; or who have
had significant radiation exposure (≥2 chest/abdominal CTs, or ≥3 other types of
X-rays) or participated in radiopharmaceutical labeling tests within 1 year prior to
testing
- Participants who are with a history of needle and blood sickness, those who have
difficulty in blood collection or cannot tolerate venipuncture blood collection
- Participation in any other clinical trial (including clinical trials such as drugs
and devices) within 3 months prior to the screening period
- Participants who have vaccinated within 1 month prior to screening or scheduled to
be vaccinated during the trial period
- Participants who plan to have children or donate sperm during the trial and within 1
year after completion of the trial, or who do not agree that the subject and his/her
spouse should use strict contraception during the trial and within 1 year after
completion of the trial
- Participants who have had blood loss or donated up to 400 mL of blood within 3
months prior to the screening period, or those who have received a blood transfusion
within 1 month
- Participants who, in the opinion of the investigator, have any factors that make
participation in this trial inappropriate
Shandong Provincial Qianfoshan Hospital
Jinan 1805753, Shandong 1796328, China
Wei Zhao, Principal Investigator
Qianfoshan Hospital