[14C] Mass Balance Clinical Trial of Azvudine in Healthy Male Subjects

NCT07002281 | Completed Phase 1

• 1 other identifier: GQ-FNC-111
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

Azvudine(FNC)，a nucleoside reverse transcriptase inhibitor, make itself a better candidate to be co-formulated in other anti-HIV therapies, thus to improve patient's compliance. FNC is a broad-spectrum RNA virus inhibitor that inhibits the novel coronavirus RNA-dependent RNA polymerase (RdRp). This trial uses a single-center, open-label, single-dose adaptive design aimed at investigating the pharmacokinetic characteristics of total radioactivity of \[14C\]-labeled Azvudine in whole blood and plasma of healthy male subjects, to quantitatively analyze the total radioactivity in exhaled gas and excreta of healthy male subjects after oral administration of \[14C\]Azvudine suspension, to obtain data on the mass balance in the human body, and to determine the main excretion routes. Biological sample collection and safety examination will be performed in this trial.

Conditions

Healthy

Keywords

Azvudine

Outcome Measures

Primary Outcomes (6)

• Pharmacokinetics (PK): Maximum Concentration (Cmax) of total radioactive material in whole blood and plasma

  Up to 96 hours post-dose

• Pharmacokinetics (PK): Time to Maximum Concentration (Tmax) of total radioactive material in whole blood and plasma

  Up to 96 hours post-dose

• Pharmacokinetics (PK): Area Under the Concentration curve (AUC) of total radioactive material in whole blood and plasma

  Up to 96 hours post-dose

• Pharmacokinetics (PK): Elimination half-life (t1/2) of total radioactive material in whole blood and plasma

  Up to 96 hours post-dose

• The total radioactivity allocation ratio

  Up to 96 hours post-dose

• The total radioactivity and the percentage to the total administered dose

  Up to 168 hours post-dose

Secondary Outcomes (6)

• Pharmacokinetics (PK): Maximum Concentration (Cmax) of Azvudine and its metabolites in plasma

  Up to 96 hours post-dose

• Pharmacokinetics (PK): Time to Maximum Concentration (Tmax) of Azvudine and its metabolites in plasma

  Up to 96 hours post-dose

• Pharmacokinetics (PK): Area Under the Concentration curve (AUC) of Azvudine and its metabolites in plasma

  Up to 96 hours post-dose

• Pharmacokinetics (PK): Elimination half-life (t1/2) of Azvudine and its metabolites in plasma

  Up to 96 hours post-dose

• Percentage of Azvudine metabolites in plasma to total exposed AUC

  Up to 96 hours post-dose

Study Arms (1)

Healthy male subjects

EXPERIMENTAL

Drug: [14C]Azvudine suspension

Interventions

[14C]Azvudine suspension DRUG

A single oral dose of 3 mg/100 μCi of \[14C\]Azvudine suspension is given orally on an empty stomach.

Healthy male subjects

Eligibility Criteria

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

You may qualify if:

• Healthy adult male subjects aged 18\~45 years old;
• Body mass index (BMI) within the range of 18.0-30.0 (including the critical value) (BMI = weight (kg) / height 2 (m2)), the weight should be ≥ 50.0kg;
• Subjects who are judged by the investigator to be in good health, with normal results of physical examination, vital signs, electrocardiogram, and laboratory examinations or abnormal but without clinical significance;
• Subjects who have no fertility plan during the study period and within 1 year after the end of the trial and agree to take effective non-drug contraceptive measures during the trial (except for those who have taken permanent contraceptive measures, such as vasectomy, etc.), and have no sperm donation plan;
• Subjects who are willing to follow the visits, study treatments, laboratory tests, and other study-related procedures and requirements specified in the study protocol, understand and sign the informed consent form.

You may not qualify if:

• Those who are allergies, with a history of drug or food allergies, especially those who are allergic to any of the ingredients in this product and excipients;
• Those who are positive for human immunodeficiency virus (HIV) antibody, hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV-Ab), or treponema pallidum antibody;
• Those who cannot tolerate venipuncture blood collection and/or have a history of blood sickness and needle sickness;
• Those who have a history of mental illness, family history of mental illness, or chronic or serious diseases of the central nervous system, cardiovascular, liver, kidney, lung, metabolic, blood, bone and other systems;
• Serum aspartate aminotransferase (AST) or alanine aminotransferase (ALT) \> 1.5 times the upper limit of normal (ULN);
• Glomerular filtration rate\< 90 mL/min/1.73m2;
• Patients with long QT syndrome or its family history, or QTcF interval (Fridericia's correction) \> 450 ms; Intraventricular block or left and right bundle branch block and/or QRS\>120 ms; Frequent ventricular ectopic beats (1 premature ventricular contraction occurred on any 10-second ECG during the screening period≥); or abnormal resting heart rate (\>100 bpm);
• Previous or current swallowing dysfunction, active gastrointestinal diseases (such as chronic constipation or diarrhea, irritable bowel syndrome, inflammatory bowel disease) or other diseases that significantly affect drug absorption, distribution, metabolism and excretion;
• Hemorrhoids or perianal disease accompanied by regular/hematochezia;
• Those who have donated blood within 3 months before screening, or have lost ≥ 200 ml of blood, or plan to donate blood during the study period;
• Those who have been vaccinated with the new crown vaccine within 2 weeks before screening or other vaccines within 3 months before screening or plan to be vaccinated during the trial;
• Intake of \> 6 servings of coffee, tea, cola, energy drinks, or other caffeinated products per day within 3 months prior to screening (one serving ≈ 120 mg of caffeine); or ingestion of foods or drinks containing high levels of caffeine, xanthines, alcohol, flavonoids (such as: grapefruit (juice), grapefruit (juice), orange (juice), etc.) within 24 hours before administration;
• Use of any drug that inhibits or induces hepatic drug metabolism enzymes within 1 month before administration (such as: inducers - barbiturates, carbamazepine, phenytoin, glucocorticoids, omeprazole; Inhibitors - SSRIs antidepressants, cimetidine, diltiazem macrolides, nitroimidazoles, sedative-hypnotics, verapamil, fluoroquinolones, antihistamines, etc.);
• Have used any prescription drugs, over-the-counter drugs, Chinese herbal medicines, and health care products within 14 days before administration;
• Those who have participated in other clinical trials within 3 months before screening;

Sponsors & Collaborators

• Henan Genuine Biotech Co., Ltd.: lead

Study Sites (1)

Beijing Jishuitan Hospital

Beijing, China

Location

Study Design

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

Study Record Dates

• First Submitted: May 13, 2025
• First Posted: June 3, 2025
• Study Start: July 22, 2024
• Primary Completion: October 10, 2024
• Study Completion: March 20, 2025
• Last Updated: June 3, 2025

Record last verified: 2025-05

Locations

CN (1)