Back to results

Study to Assess Safety, Tolerability and Pharmacokinetics of XC221 in Healthy Volunteers

Primary Purpose

Influenza, Acute Respiratory Infection

Status

Completed

Phase

Phase 1

Locations

Russian Federation

Study Type

Interventional

Intervention

XC221 60 mg

XC221 200 mg

Placebo

About this trial

This is an interventional treatment trial for Influenza focused on measuring Healthy volunteers, Phase I, PHARMENTERPRISES

Eligibility Criteria

18 Years - 45 Years (Adult)MaleAccepts Healthy Volunteers

Inclusion Criteria:

Non-smoking men aged 18 to 45 years (inclusive);
Verified diagnosis "healthy" according to standard clinical, laboratory and instrumental methods of examination;
Body mass >50 kg and body mass index of 18.5 to 30 kg/m2 (inclusive);
Negative result of tests for alcohol and drugs;
Consent to use reliable methods of contraception during the study and 3 months after its completion (condoms with spermicide);
Signed patient information sheet and informed consent form for participation in the study.

Exclusion Criteria:

Chronic diseases of cardiovascular, bronchopulmonary, neuroendocrine, musculoskeletal system and also disease of digestive tract, liver, kidneys, blood;
Laboratory abnormalities at screening;
Surgical interventions on digestive tract in the anamnesis (except for an appendectomies);
Systolic pressure is less than 90 mm Hg. or more than 130 mm Hg., diastolic pressure is less than 60 mm Hg. or more than 85 mm Hg., pulse rate less than 60/min. or more than 80/min.;
Course intake of medicinal products (including herbs and biologically active additives) for preventive or curative purposes within 1 month prior to screening;
Antibodies to HIV and hepatitis C virus, the presence of the hepatitis B surface antigen, a positive syphilis test;
The presence of a sleep disorder (for example, night work, sleep disturbances, insomnia, recent return from another time zone, etc.);
Signs of alcohol or drug abuse; taking alcohol or drugs during 4 days before screening; smoking 3 months before screening;
History of allergies (including medicines and food products);
Blood donation / plasma, surgical intervention (in a hospital environment) during 12 weeks before screening;
Participation in other clinical trials or taking the study drug during 3 months before screening;
Acute infectious diseases less than 4 weeks before the start of the study;
Impossibility to understand or follow protocol instructions/

Sites / Locations

SBEI HPE The First Moscow State Medical University n.a. Sechenov of Ministry of Health of Russian Federation, University Hospital #2, Department of Development of New Medicines

Arms of the Study

Arm 1

Arm 2

Arm 3

Arm Type

Experimental

Placebo Comparator

Arm Label

XC221 60 mg

XC221 200 mg

Placebo

Arm Description

Cohort 1:16 subjects were randomized in a 3:1 ratio to be treated either with 60 mg XC221 (12 subjects) or placebo (4 subjects, see placebo arm).

Cohort 2: 16 subjects were randomized in a 3:1 ratio to be treated either with 200 mg XC221 (12 subjects) or placebo (4 subjects, see placebo arm).

Placebo comparator arm consists of 8 subjects (4 subjects from each cohort).

Outcomes

Primary Outcome Measures

Number of Adverse events per treatment arm

Adverse events have been classified according to CTCAE ver 4.03. Adverse events will be summarized descriptively by treatment arm. Verbatim terms will be mapped to preferred terms and organ systems using the current Medical Dictionary for Regulatory Activities version. For each preferred term, frequency counts and percentages will be calculated by cohort.The nature, severity, seriousness, and relationship to study medication will be summarized for all study subjects

Secondary Outcome Measures

Pharmacokinetics of XC221GI by assessing AUC0-inf

Area under the curve "concentration of the drug-time" from the time of administration of the drug till infinity

Pharmacokinetics of XC221A by assessing AUC0-inf

Area under the curve "concentration of the drug-time" from the time of administration of the drug till infinity

Pharmacokinetics of XC221GI by assessing Cmax

Maximum plasma concentration

Pharmacokinetics of XC221A by assessing Cmax

Maximum plasma concentration

Pharmacokinetics of XC221GI by assessing AUC0-t

Area under the curve "concentration of the drug-time" from the time of administration of the drug till the time (t) the last blood sampling

Pharmacokinetics of XC221A by assessing AUC0-t

Area under the curve "concentration of the drug-time" from the time of administration of the drug till the time (t) the last blood sampling

Pharmacokinetics of XC221GI by assessing Tmax

Time to maximum drug concentration in the blood plasma administration

Pharmacokinetics of XC221A by assessing Tmax

Time to maximum drug concentration in the blood plasma administration

Pharmacokinetics of XC221GI by assessing T1/2

Terminal elimination half-life

Pharmacokinetics of XC221A by assessing T1/2

Terminal elimination half-life

Full Information

NCT ID

NCT03459391

First Posted

February 26, 2018

Last Updated

March 2, 2018

Sponsor

PHARMENTERPRISES LLC

1. Study Identification

Unique Protocol Identification Number

NCT03459391

Brief Title

Study to Assess Safety, Tolerability and Pharmacokinetics of XC221 in Healthy Volunteers

Official Title

A Double-blind, Randomized, Placebo-controlled Study of the Safety,Tolerability and Pharmacokinetics of Increasing Doses of XC221 After Single and Repeated Oral Administration in Healthy Volunteers

Study Type

Interventional

2. Study Status

Record Verification Date

March 2018

Overall Recruitment Status

Completed

Study Start Date

May 22, 2017 (Actual)

Primary Completion Date

September 26, 2017 (Actual)

Study Completion Date

September 26, 2017 (Actual)

3. Sponsor/Collaborators

Responsible Party, by Official Title

Sponsor

Name of the Sponsor

PHARMENTERPRISES LLC

4. Oversight

Studies a U.S. FDA-regulated Drug Product

Studies a U.S. FDA-regulated Device Product

Data Monitoring Committee

Yes

5. Study Description

Brief Summary

A double-blind, randomized, placebo-controlled, Phase I clinical study of the safety and tolerability of increasing doses of drug XC221 after single and repeated oral administration in healthy volunteers. The volunteers received the study drug once, and then continued daily intake for 5 days after a 6-day break. The primary objective of the study was to evaluate the safety and tolerability profile for drug XC221 after single and multiple administration based on the frequency and severity of adverse events and changes in vital signs, laboratory results, electrocardiography and results of the physical examination. The secondary objective of the study was to assess pharmacokinetics of active pharmaceutical substance XC221GI and its metabolite XC221A.

Detailed Description

One Russian center was approved for participation in this study. One center was initiated. Healthy volunteers were enrolled in 1 center. The study consisted of 4 periods: screening, single administration, multiple administration and follow-up. All eligible subjects were randomized into the study in appropriate cohort groups sequentially. Cohort 1 - XC221 or Placebo 60 mg once and then daily 5 days after a 6-day break; Cohort 2 - XC221 or Placebo 200 mg once and then daily during 5 days after a 6-day break. The decision regarding increasing of the study drug dose for a subsequent cohort was made by the Data Safety Monitoring Committee on the basis of preliminary safety results assessment. A total of 24 volunteers received XC221 (60 mg or 200 mg) and a total of 8 volunteers received the placebo during the study participation. The follow-up period lasted for 4 weeks.

6. Conditions and Keywords

Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study

Influenza, Acute Respiratory Infection

Keywords

Healthy volunteers, Phase I, PHARMENTERPRISES

7. Study Design

Primary Purpose

Treatment

Study Phase

Phase 1

Interventional Study Model

Sequential Assignment

Model Description

The dose cohorts were included into the study subsequently based on preliminary safety results evaluation performed by the Data Safety Monitoring Committee. 2 doses of XC221/placebo (60 mg and 200 mg) were used in the study.The duration of exposure to the study drug was 6 days in each cohort: Day 1, once, at the step of single administration, and then in 6 days, daily, 1 time a day for 5 days at the step of multiple administration.

Masking

ParticipantInvestigator

Masking Description

Blinding was carried out by using Placebo equivalent to XC221 tablets without active substance and the corresponding labeling of the study drug.

Allocation

Randomized

Enrollment

32 (Actual)

8. Arms, Groups, and Interventions

Arm Title

XC221 60 mg

Arm Type

Experimental

Arm Description

Cohort 1:16 subjects were randomized in a 3:1 ratio to be treated either with 60 mg XC221 (12 subjects) or placebo (4 subjects, see placebo arm).

Arm Title

XC221 200 mg

Arm Type

Experimental

Arm Description

Cohort 2: 16 subjects were randomized in a 3:1 ratio to be treated either with 200 mg XC221 (12 subjects) or placebo (4 subjects, see placebo arm).

Arm Title

Placebo

Arm Type

Placebo Comparator

Arm Description

Placebo comparator arm consists of 8 subjects (4 subjects from each cohort).

Intervention Type

Drug

Intervention Name(s)

XC221 60 mg

Intervention Description

The volunteers received the study drug once, and then continued daily intake for 5 days after a 6-day break.

Intervention Type

Drug

Intervention Name(s)

XC221 200 mg

Intervention Description

The volunteers received the study drug once, and then continued daily intake for 5 days after a 6-day break.

Intervention Type

Drug

Intervention Name(s)

Placebo

Intervention Description

The volunteers received the study drug once, and then continued daily intake for 5 days after a 6-day break.

Primary Outcome Measure Information:

Title

Number of Adverse events per treatment arm

Description

Time Frame

Change from pre-dose to Day 28

Secondary Outcome Measure Information:

Title

Pharmacokinetics of XC221GI by assessing AUC0-inf

Description

Area under the curve "concentration of the drug-time" from the time of administration of the drug till infinity

Time Frame

Day 1 and 11 (Pre dose, 15 min, 30 min, 1,1.5, 2, 2.5, 3, 4, 5, 6, 8,12 and 16 h post dose), Day 2 and Day 12 (24 h ±10 min post dose), Day 3 and Day 13 (48 h ±10 min post dose), Day 4 and Day 14 (72 h ±10 min post dose), Day 7 to 10 (Pre dose)

Title

Pharmacokinetics of XC221A by assessing AUC0-inf

Description

Area under the curve "concentration of the drug-time" from the time of administration of the drug till infinity

Time Frame

Title

Pharmacokinetics of XC221GI by assessing Cmax

Description

Maximum plasma concentration

Time Frame

Title

Pharmacokinetics of XC221A by assessing Cmax

Description

Maximum plasma concentration

Time Frame

Title

Pharmacokinetics of XC221GI by assessing AUC0-t

Description

Area under the curve "concentration of the drug-time" from the time of administration of the drug till the time (t) the last blood sampling

Time Frame

Title

Pharmacokinetics of XC221A by assessing AUC0-t

Description

Area under the curve "concentration of the drug-time" from the time of administration of the drug till the time (t) the last blood sampling

Time Frame

Title

Pharmacokinetics of XC221GI by assessing Tmax

Description

Time to maximum drug concentration in the blood plasma administration

Time Frame

Title

Pharmacokinetics of XC221A by assessing Tmax

Description

Time to maximum drug concentration in the blood plasma administration

Time Frame

Title

Pharmacokinetics of XC221GI by assessing T1/2

Description

Terminal elimination half-life

Time Frame

Title

Pharmacokinetics of XC221A by assessing T1/2

Description

Terminal elimination half-life

Time Frame

10. Eligibility

Sex

Male

Minimum Age & Unit of Time

18 Years

Maximum Age & Unit of Time

45 Years

Accepts Healthy Volunteers

Eligibility Criteria

Inclusion Criteria: Non-smoking men aged 18 to 45 years (inclusive); Verified diagnosis "healthy" according to standard clinical, laboratory and instrumental methods of examination; Body mass >50 kg and body mass index of 18.5 to 30 kg/m2 (inclusive); Negative result of tests for alcohol and drugs; Consent to use reliable methods of contraception during the study and 3 months after its completion (condoms with spermicide); Signed patient information sheet and informed consent form for participation in the study. Exclusion Criteria: Chronic diseases of cardiovascular, bronchopulmonary, neuroendocrine, musculoskeletal system and also disease of digestive tract, liver, kidneys, blood; Laboratory abnormalities at screening; Surgical interventions on digestive tract in the anamnesis (except for an appendectomies); Systolic pressure is less than 90 mm Hg. or more than 130 mm Hg., diastolic pressure is less than 60 mm Hg. or more than 85 mm Hg., pulse rate less than 60/min. or more than 80/min.; Course intake of medicinal products (including herbs and biologically active additives) for preventive or curative purposes within 1 month prior to screening; Antibodies to HIV and hepatitis C virus, the presence of the hepatitis B surface antigen, a positive syphilis test; The presence of a sleep disorder (for example, night work, sleep disturbances, insomnia, recent return from another time zone, etc.); Signs of alcohol or drug abuse; taking alcohol or drugs during 4 days before screening; smoking 3 months before screening; History of allergies (including medicines and food products); Blood donation / plasma, surgical intervention (in a hospital environment) during 12 weeks before screening; Participation in other clinical trials or taking the study drug during 3 months before screening; Acute infectious diseases less than 4 weeks before the start of the study; Impossibility to understand or follow protocol instructions/

Facility Information:

Facility Name

SBEI HPE The First Moscow State Medical University n.a. Sechenov of Ministry of Health of Russian Federation, University Hospital #2, Department of Development of New Medicines

City

Moscow

ZIP/Postal Code

119435

Country

Russian Federation

12. IPD Sharing Statement

Plan to Share IPD

Learn more about this trial

Study to Assess Safety, Tolerability and Pharmacokinetics of XC221 in Healthy Volunteers

We'll reach out to this number within 24 hrs