Pharmacokinetics and Bioequivalence of XC8 10 mg and 40 mg Tablets in Fasted Volunteers

NCT05558462 | Completed

• 1 other identifier: XC8-05-04-2022
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

Comparative study of the pharmacokinetics of XC8, film-coated tablets, 10 mg and XC8, film-coated tablets, 40 mg, when administered once in equal doses (40 mg) on an empty stomach in healthy volunteers.

Conditions

Influenza; Respiratory Viral Infection

Outcome Measures

Primary Outcomes (11)

• Pharmacokinetics - Cmax

  Maximum plasma concentration (Cmax)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - tmax

  Time to reach Cmax (tmax)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - AUC0-t

  Area under the plasma concentration-time curve from time 0 to t (AUC0-t)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - AUC0-inf

  Area under the plasma concentration-time curve from time 0 to infinity (AUC0-inf)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - AUCextr

  Extrapolated AUC, defined as (AUC0-inf - AUC0-t)/AUC0-inf

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - t1/2

  Elimination half-life (t1/2)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - kel

  Elimination constant (kel)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - MRT

  Mean residence time (MRT)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Bioequivalence - ratio of Cmax

  Ratio of geometric mean Cmax after intake of R or T (with 90% confidence intervals)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Bioequivalence - ratio of AUC0-t

  Ratio of geometric mean AUC0-t after intake of R or T (with 90% confidence intervals)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

• Bioequivalence - ratio of AUC0-inf

  Ratio of geometric mean AUC0-inf after intake of R or T (with 90% confidence intervals)

  From 0 to 24 hours (Day 1-2 and Day 8-9)

Secondary Outcomes (43)

• Safety and Tolerability: adverse event (AE) number and frequency

  From the screening (and signing informed consent form) to Day 14 of the study or to an early termination visit within the time frame of the study (from Day 0 to Day 14)

• Safety and Tolerability: serious adverse event (SAE) number and frequency

  From the screening (and signing informed consent form) to Day 14 of the study or to an early termination visit within the time frame of the study (from Day 0 to Day 14)

• Safety and Tolerability: vital signs - systolic blood pressure (SBP)

  Screening, from Day 0 to Day 2, from Day 7 to Day 9, and/or on early termination visit within the time frame of the study (from Day 0 to Day 14)

• Safety and Tolerability: vital signs - diastolic blood pressure (DBP)

  Screening, from Day 0 to Day 2, from Day 7 to Day 9, and/or on early termination visit within the time frame of the study (from Day 0 to Day 14)

• Safety and Tolerability: vital signs - respiratory rate (RR)

  Screening, from Day 0 to Day 2, from Day 7 to Day 9, and/or on early termination visit within the time frame of the study (from Day 0 to Day 14)

Study Arms (2)

RT-sequence

EXPERIMENTAL

Group 1 (12 volunteers, RT sequence) will take 4 tablets of XC8, 10 mg, in Period 1 and 1 tablet of XC8, 40 mg, in Period 2

Drug: XC8

TR-sequence

EXPERIMENTAL

Group 2 (12 volunteers, sequence TR) will take 1 tablet of XC8, 40 mg, in Period 1 and 4 tablets of XC8, 10 mg, in Period 2.

Drug: XC8

Interventions

XC8 DRUG

A single dose of R or T drug in each of 2 periods of the study in fasted conditions

RT-sequence; TR-sequence

Eligibility Criteria

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

You may qualify if:

• Voluntary and handwritten informed consent form signed by a healthy volunteer to participate in the study prior to any of the study procedures;
• Men and women between the ages of 18 and 45 years (inclusive) of Caucasian race;
• Verified diagnosis "healthy" (absence of abnormalities according to clinical, laboratory, instrumental methods of examination, stipulated by the protocol);
• Blood pressure (BP): systolic blood pressure (SBP) of 99 to 129 mmHg (inclusive), diastolic blood pressure (DBP) of 70 to 89 mmHg (inclusive);
• Heart rate (HR) from 60 to 89 beats/min (inclusive);
• Respiratory rate (HR) from 12 to 20 per minute (inclusive);
• Body temperature from 36°C to 36.9°C (inclusive);
• Body mass index (BMI) of 18.5 kg/m2 ≤ BMI ≤ 30 kg/m2, with a body weight of ≥ 55 kg for men and ≥ 45 kg for women;
• Consent to use adequate methods of contraception throughout the study and for 30 days after completion; for women of preserved reproductive potential, a negative urine pregnancy test result.

You may not qualify if:

• A history of allergy;
• Drug intolerance to the active substance XC8 (N-\[2-(1H-imidazol-4-yl)-ethyl\]-6-oxo-δ-lactam) and/or excipients contained in the studied drug in the anamnesis;
• Chronic diseases of the kidneys, liver, gastrointestinal tract (GIT), cardiovascular, lymphatic, respiratory, nervous, endocrine, musculoskeletal, genitourinary and immune systems, as well as skin, blood and vision;
• History of gastrointestinal surgery (except appendectomy at least 1 year prior to screening);
• Diseases/conditions that, in the opinion of the investigator, may affect absorption, distribution, metabolism or excretion of the investigational drugs;
• Acute infectious disease less than 4 weeks prior to screening;
• Taking medications that significantly affect hemodynamics and medications that affect liver function (barbiturates, omeprazole, cimetidine, etc.) less than 2 months prior to screening;
• Regularly taking an medicine less than 2 weeks before screening and taking a single medicine less than 7 days before screening;
• Donating blood or plasma less than 3 months before screening;
• Use of hormonal contraceptives (in women) less than 2 months before screening;
• The use of depot injections of any drug less than 3 months before screening;
• Pregnancy or lactation; positive urine pregnancy test for women of preserved reproductive potential;
• Women of preserved reproductive potential with a history of unprotected intercourse within 30 days prior to study drug administration with an unsterilized partner;
• Participation in another clinical trial less than 3 months prior to screening or concurrently with the present study;
• Smoking more than 10 cigarettes per day currently, or a history of smoking the specified number of cigarettes during the 6 months prior to screening; disagreement to abstain from smoking for the duration of the hospital stay;

Sponsors & Collaborators

• Valenta Pharm JSC: lead

Study Sites (1)

I.M. Sechenov First Moscow State Medical University

Moscow, 119991, Russia

Location

MeSH Terms

Conditions

Influenza, Human

Condition Hierarchy (Ancestors)

Respiratory Tract Infections; Infections; Orthomyxoviridae Infections; RNA Virus Infections; Virus Diseases; Respiratory Tract Diseases

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 14, 2022
• First Posted: September 28, 2022
• Study Start: August 22, 2022
• Primary Completion: November 11, 2022
• Study Completion: December 7, 2022
• Last Updated: October 10, 2023

Record last verified: 2023-10

Locations

RU (1)