Bioequivalence Study of GP30101 800 mg (GEROPHARM) Versus PREZISTA® 800 mg (Jonson&Jonson, Russia)

Study Overview
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Brief Summary
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Bioequivalence Study of GP30101 800 mg (GEROPHARM) Versus PREZISTA® 800 mg (Jonson&Jonson, Russia)

Detailed Description
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Study to evaluate the pharmacokinetic parameters, relative bioavailability and bioequivalence of drugs containing darunavir - GP30101 and Prezista® in healthy volunteers after single orally administered dose, under fed conditions A comparative analysis of adverse events aditionally conducted in this study.

Official Title
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Crossover, Open-label, Randomized, Single-dose, Bioequivalence Study of GP30101 Film-coated Tablets (LLC GEROPHARM, Russia) 800 mg Versus Prezista® (Jonson&Jonson, Russia) Film-coated Tablets 800 mg in Healthy Volunteers Under Fed Conditions

Conditions
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Bioequivalence

Intervention / Treatment
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* Drug: GP30101
* Drug: Prezista®
* Drug: GP30101
* Drug: Prezista®


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Signed informed consent form. Male aged 18 to 45 years. Verified diagnosis is healthy according to data Standard clinical, laboratory and Instrumental methods of examination. Body mass index between 18,5 and 30 kg/m2, with body weight 60-100 kg Consent to comply with an adequate method of effective contraception throughout the study. The consent of volunteers to all restrictions imposed during the study. Russian Federation Citizens Exclusion Criteria: History of allergic problems/events. Hypersensitivity to heparin, darunavir or any of the excipients of the drugs studied. Any acute and chronic diseases, including but not limited to cardiovascular system diseases, bronchopulmonary diseases, neuroendocrine systems diseases, as well as diseases of the gastrointestinal tract, liver, kidneys, blood. Positive testing for hepatitis C (antibodies) or hepatitis B (surface antigen), HIV (antibodies to HIV-1/2), syphilis (antibodies to Treponema pallidum). The WHO norms deviations of the heart rate (60-89), Sistolic BP (100-130 mm Hg), Diatolic BP (60-89 mm Hg), respiratory rate (12-20), body temperature (35.7 - 37.6 °C). Abnormal ECG during screening. Inaccessible veins of the upper extremities, vein thrombosis, thrombophlebitis in the anamnesis or in the family history of the next of kin, compromised veins due to frequent previous venipuncture. Psychiatric disorders, history of epilepsy and seizures. Surgical interventions on the gastrointestinal tract (except appendectomy). Acute infectious diseases in less than 4 weeks before the start of the study. Regular medication use (intake) less than 2 weeks before the start of the study. Significant loss of blood within 3 months prior to screening, including but not limited to blood donation or extended surgery or trauma resulting in the blood loss. History of alcohol or drugs abuse or any indication of the regular use of more than 10 units of alcohol per week (1 Unit = 200 mL of wine or 500 mL of beer or 50 mL of alcohol 40%). Positive test results for alcohol or drug use. Nicotine addiction, regular use of tobacco, including all types of electronic cigarettes, less than 6 months prior to screening. Participation in a clinical trial of any drugs (including experimental) or experimental medical devices for 3 months or 5 half-lives, whichever is longer, before the study. Dehydration due to diarrhea, vomiting, or other causes within the last 24 hours before the start of the study. Any diet (for example, vegetarian, fasting, etc.) or lifestyle (including night work and extreme physical activity) that may interfere with the study. Taking medications that have a pronounced effect on hemodynamics, liver function, etc. (barbiturates, omeprazole, cimetidine, etc.) less than 30 days before the start of the study. Volunteers who are obvious or likely, according to the investigator, are unable to understand and evaluate the information on this study as part of the process of signing informed consent, in particular regarding the expected risks and possible discomfort.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 45 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Basic Science
Allocation: Randomized
Intervention Model: Crossover Assignment
Interventional Model Description: Crossover Assignment two-way crossover
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: TR Sequence<br>In first Intervention period subjects was administered test medecine (GP30101) and in seconde Intervention period subjects was administered reference medecine (Prezista) | Drug: GP30101<br>* Single oral dose 800 mg, administered in a fed condition, co-administered with low dose ritonavir as a pharmacokinetic enhancer<br>* Other names: First aIntervention Period;Drug: Prezista®<br>* Single oral dose 800 mg, administered in a fed condition, co-administered with low dose ritonavir as a pharmacokinetic enhancer<br>* Other names: Second Intervention Period;|
| Experimental: RT Sequence<br>In first Intervention period subjects was administered reference medecine (Prezista) and in seconde Intervention period subjects was administered test medecine (GP30101) | Drug: Prezista®<br>* Single oral dose 800 mg, administered in a fed condition, co-administered with low dose ritonavir as a pharmacokinetic enhancer<br>* Other names: First aIntervention Period;Drug: GP30101<br>* Single oral dose 800 mg, administered in a fed condition, co-administered with low dose ritonavir as a pharmacokinetic enhancer<br>* Other names: Second Intervention Period;|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| C(max) | Pharmacokinetics by Assessment of Observed Maximum Plasma Concentration (Cmax) | -35 min prior dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24, 48, 72 hour post-dose | 
| AUC(0-t) | Pharmacokinetics by Assessment of Area Under the Curve From Time Zero Extrapolated to t (AUC(0-t) | -35 min prior dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24, 48, 72 hour post-dose | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| T(max) | Pharmacokinetics by Assessment of Time of Maximum concentration observed (T(max) | -35 min prior dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24, 48, 72 hour post-dose | 
| T(1/2) | Pharmacokinetics by Assessment of elimination half-life T(1/2) | -35 min prior dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24, 48, 72 hour post-dose | 
| K(e) | Pharmacokinetics by Assessment of elimination rate constant | -35 min prior dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 24, 48, 72 hour post-dose |