Pharmacokinetics and Bioequivalence of Aterixen 100 mg Tablets and Aterixen 100 mg Film-coated Tablets in Healthy Volunteers

NCT06096571 | Unknown

• 1 other identifier: ХС221-05-05-2022
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

1. 1.Comparative evaluation of the safety of the drug Aterixen 100 mg tablets (Valenta Pharm JSC, Russia) and Aterixen 100 mg film-coated tablets (Valenta Pharm JSC, Russia) administered in single doses under fasting conditions in healthy volunteers, based on AE/SAE (adverse events/serious adverse event) analysis;
2. 2.Comparative assessment of pharmacokinetic parameters and bioavailability of Aterixen 100 mg tablets (Valenta Pharm JSC, Russia) and Aterixen 100 mg film-coated tablets (Valenta Pharm JSC, Russia) administered in single doses under fasting conditions in healthy volunteers.
3. 3.To conclude on the bioequivalence of Aterixen 100 mg tablets (Valenta Pharm JSC, Russia) and Aterixen 100 mg film-coated tablets (Valenta Pharm JSC, Russia) administered in single doses under fasting conditions in healthy volunteers.

Conditions

Viral Infection COVID-19

Outcome Measures

Primary Outcomes (11)

• Pharmacokinetics - Cmax

  Maximum plasma concentration (Cmax)

  From 0 to 12 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - tmax

  Time to reach Cmax (tmax)

  From 0 to 12 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 12 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 12 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - AUCextr

  Extrapolated AUC, area under the concentration-time pharmacokinetic curve, to be calculated as Clast/Kel

  From 0 to 12 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - t1/2

  Elimination half-life (t1/2)

  From 0 to 12 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - Kel

  Elimination constant (Kel)

  From 0 to 12 hours (Day 1-2 and Day 8-9)

• Pharmacokinetics - number of points in terminal logarithmic phase

  Used to estimate Kel

  From 0 to 12 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 12 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 12 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 12 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: adverse event (AE) characteristics

  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)

Experimental: RT-sequence

OTHER

Group 1 (18 volunteers, RT sequence) will take 1 tablet of Aterixen,100 mg as a single dose in the fasting state in Period 1 and 1 tablet of Aterixen,100 mg film-coated tablet as a single dose in the fasting conditions in Period 2

Drug: Aterixen

Experimental: TR-sequence

OTHER

Group 2 (18 volunteers, TR sequence) will take 1 tablet of Aterixen,100 mg film-coated tablet as a single dose in the fasting state in Period 1 and 1 tablet of Aterixen,100 mg as a single dose in the fasting conditions in Period 2

Drug: Aterixen

Interventions

Aterixen DRUG

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

Experimental: RT-sequence; Experimental: 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;
• Healthy male and female caucasian volunteers aged 18 to 45 years (inclusive);
• Verified diagnosis "healthy" (without abnormal findings in the protocol-defined clinical, laboratory, and instrumental test data);
• Blood pressure (BP) levels: 99 to 129 mm Hg, inclusive (systolic, SBP), 70 to 89 mm Hg, inclusive (diastolic, DBP);
• Heart rate (HR) of 60 to 89 bpm, inclusive;
• Respiratory rate (RR) of 12 to 20 breaths per minute, inclusive;
• Body temperature of 36°C to 36.9°C, inclusive;
• Body mass index (BMI) of 18.5 kg/m2 ≤ BMI ≤ 30 kg/m2, where the body weight range is ≥ 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 N1-\[2-(1-Methyl imidazol-4-yl)-ethyl\]perhydroazin-2,6-dione (the active ingredient of Aterixen) and/or excipients contained in the studied drug in the anamnesis;
• History of drug intolerance of N1-\[2-(1-Methyl imidazol-4-yl)-ethyl\]perhydroazin-2,6-dione (the active ingredient of Aterixen) aand/or excipients contained in the studied drug in the anamnesis;
• History of hereditary galactose intolerance, lactase or glucose-galactose malabsorption
• Chronic diseases of the kidneys, liver, gastrointestinal tract (GIT); disease of the circulatory, lymphatic, respiratory, nervous, endocrine, musculoskeletal, urogenital and the immune systems; dermal, hematopoietic, and ophthalmological diseases;
• 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 (including OTC medicinal products, vitamins, dietary supplements, or medicinal herbs);
• 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;

Sponsors & Collaborators

• Valenta Pharm JSC: lead

Study Sites (1)

Limited Liability Company "Research Center Eco-Safety"

Saint Petersburg, 196143, Russia

Location

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: October 13, 2023
• First Posted: October 24, 2023
• Study Start: June 15, 2024
• Primary Completion: December 15, 2024
• Study Completion: December 30, 2024
• Last Updated: March 29, 2024

Record last verified: 2023-10

Locations

RU (1)