Double-blind, Randomized, Placebo-controlled Study of the Safety, Tolerability and Pharmacokinetics of Ascending Doses of XC243 After Single and Multiple Oral Administration in Healthy Volunteers.

NCT05628116 | Completed Phase 1 DMC

• 1 other identifier: PAIN-ХС243-01
• Study Type: interventional
• Target: 38
• Locations: 1 country
• Sites: 1

Brief Summary

A double-blind, randomized, placebo-controlled, Phase I clinical study of the safety, tolerability and pharmacokinetics (PK) of ascending doses of XC243 after single and multiple oral administration in healthy volunteers. It's planned to include sequentially 2 cohorts of 7 volunteers who will receive a single dose of XC243 (50 mg and 100 mg) or placebo (cohort ratio 5:2), 1 cohort of 14 volunteers who will receive a single dose of XC243 200 mg or placebo first on an empty stomach, and after the washing period after eating (cohort ratio 12:2) and 1 cohort of 10 volunteers who will receive XC243 200 mg or placebo on an empty stomach during 14 days (cohort ratio 8:2).

Conditions

Healthy Volunteers

Keywords

Phase 1

Outcome Measures

Primary Outcomes (1)

• Number of Adverse events (AEs) per treatment arm

  Adverse events will be classified according to CTCAE. 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.

  Day 1-Day 35

Secondary Outcomes (5)

• Pharmacokinetics of XC243 by assessing AUC0-inf

  Day 1- Day 14

• Pharmacokinetics of XC243 by assessing Cmax

  Day 1- Day 14

• Pharmacokinetics of XC243 by assessing AUC0-t

  Day 1- Day 14

• Pharmacokinetics of XC243 by assessing Tmax

  Day 1- Day 14

• Pharmacokinetics of XC243 by assessing T1/2

  Day 1- Day 14

Study Arms (7)

XC243 50 mg single

EXPERIMENTAL

Cohort 1 - 7 subjects will be randomized in a 5:2 ratio to be treated either XC243 50 mg (5 subjects) or placebo (2 subjects, see placebo single arm)

Drug: XC243 50 mg single

XC243 100 mg single

EXPERIMENTAL

Cohort 2 - 7 subjects will be randomized in a 5:2 ratio to be treated either XC243 100 mg (5 subjects) or placebo (2 subjects, see placebo single arm)

Drug: XC243 100 mg single

Placebo single

PLACEBO COMPARATOR

Placebo comparator arm will consist of 4 subjects (1 subject each from Сohorts 1 and 2)

Drug: Placebo single

XC243 200 mg single-dose food effect

EXPERIMENTAL

Cohort 3 - 14 subjects will be randomized in a 12:2 ratio to be treated either XC243 200 mg (12 subjects) or placebo (2 subjects, see placebo single arm) first on an empty stomach, and after the washing period after eating

Drug: XC243 200 mg single-dose food effect

Placebo single-dose food effect

PLACEBO COMPARATOR

Placebo comparator arm will consist of 2 subjects from Cohort 3

Drug: Placebo single-dose food effect

XC243 200 mg multiple

EXPERIMENTAL

Cohort 4 - 10 subjects will be randomized in a 8:2 ratio to be treated either XC243 200 mg (8 subjects) or placebo (2 subjects, see placebo multiple arm)

Drug: XC243 200 mg multiple

Placebo multiple

PLACEBO COMPARATOR

Placebo comparator arm will consist of 2 subjects from cohort 4

Drug: Placebo multiple

Interventions

XC243 50 mg single DRUG

The volunteers will receive a single dose of the ID (1 tablet once, 50 mg)

XC243 50 mg single

XC243 100 mg single DRUG

The volunteers will receive a single dose of the ID (2 tablets once, 100 mg)

XC243 100 mg single

Placebo single DRUG

The volunteers will receive a single dose of the ID (1 or 2 tablets once)

Placebo single

XC243 200 mg single-dose food effect DRUG

The volunteers will receive single dose of the ID during first on an empty stomach, and after the washing period after eating (4 tablets, 200 mg)

XC243 200 mg single-dose food effect

Placebo single-dose food effect DRUG

The volunteers will receive single dose of the ID during first on an empty stomach, and after the washing period after eating (4 tablets)

Placebo single-dose food effect

XC243 200 mg multiple DRUG

The volunteers will receive multiple doses of the ID during 14 days (4 tablets daily, 200 mg each)

XC243 200 mg multiple

Placebo multiple DRUG

The volunteers will receive multiple doses of the ID during 14 days (4 tablets daily)

Placebo multiple

Eligibility Criteria

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

You may qualify if:

• The volunteer read, understood and signed the Information Leaflet and the Informed Consent Form to participate in the study;
• Non-smoking men (nonsmokers at least within the last year before the screening) at the ages from 18 through 45;
• Verified diagnosis "healthy" according to standard clinical, laboratory and instrumental methods of examination;
• Blood Pressure (BP): Systolic blood pressure (SBP) 100 to 130 mm Hg, diastolic blood pressure (DBP) from 70 to 89 mm Hg (inclusive);
• Heart rate (HR) from 60 to 90 units/min (inclusive);
• Respiratory rate (RR) from 12 to 20 min-1 (inclusive);
• Body temperature from 36 to 36.9 ° C (inclusive);
• Body mass index from 18.5 to 30.0 kg/m2 with body weight of more than 45 kg and no more than 110 kg;
• Negative result of breath alcohol test, urine test for narcotic substances;
• Consent to use adequate contraceptive methods throughout the study, including the post-observation period (7 days in Cohorts 1-3 and 14 days in Cohort 4), as well as 90 days at its end;
• Agreement to observe the daily and nutritional regimen provided for by the study protocol.

You may not qualify if:

• The history of chronic diseases of the cardiovascular, bronchopulmonary, nervous, endocrine, musculoskeletal system, as well as the gastrointestinal tract (GI), liver, kidneys, blood, mental illness, epilepsy or seizure;
• Deviations of standard laboratory and instrumental values, as well as physical examination results from normal values at screening;
• History of GI surgery (excluding appendectomy);
• Administration of drugs less than 2 weeks before screening (including preparations of plant origin, vitamins and dietary supplements), with the exception of episodic administration of paracetamol at a dose of up to 1.5 g/day;
• Taking drugs that affect liver function (for example, inhibitors and/or inducers of cytochrome P450) less than 30 days before screening;
• Presence of antibodies to HIV and hepatitis C virus at screening, presence of hepatitis B virus surface antigen, presence of antibodies to T. Pallidum \*;
• Presence of a positive test for SARS-CoV-2 at screening;
• Presence of unstable sleep structure (for example, night shift work, sleep disturbances, insomnia, recent return from another time zone, etc.), extreme physical activity (for example, lifting weights);
• A special diet (for example, vegetarian, vegan, hypocaloric (less than 1000 kcal/day));
• Taking alcohol within 4 days of screening or testing positive for exhaled alcohol at screening or on Day -1;
• Taking narcotic drugs within 4 days before screening or a positive urine drug test at screening or on Day -1;
• History of alcohol and/or drug dependence or intake of more than 5 units of alcohol per week (one unit of alcohol is 40 ml of strong alcoholic beverages, 330 ml of beer or 150 ml of wine) since the beginning of the screening stage;
• Smoking or using nicotine-containing products at present and for 6 months prior to screening;
• History of allergic and/or hypersensitivity reactions to drugs;
• Hypersensitivity to study drug components;

Sponsors & Collaborators

• PHARMENTERPRISES LLC: lead

Study Sites (1)

LLS X7 Clinical Research

Saint Petersburg, 194156, Russia

Location

MeSH Terms

Interventions

Single Person

Intervention Hierarchy (Ancestors)

Marital Status; Family Characteristics; Demography; Population Characteristics; Socioeconomic Factors

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Masking Details: Blinding was carried out by using placebo equivalent to XC243 tablets without active pharmaceutical ingredients (API) and the corresponding labeling of the ID.
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: The dose cohorts will be included into the study subsequently based on preliminary safety results evaluation performed by the DSMC. 2 doses of XC243/placebo (50 mg, 100 mg) were used in the single-dose ascending study. 1 dose of XC243/placebo (200 mg) were used in the single-dose food effect study. 1 dose of XC243/placebo (200 mg) were used in the repeated dose study.The duration of exposure to the ID is planned 1 day in single dosing cohorts and 14 days in multiple dosing cohort.

Study Record Dates

• First Submitted: November 16, 2022
• First Posted: November 28, 2022
• Study Start: September 28, 2022
• Primary Completion: September 21, 2023
• Study Completion: September 21, 2023
• Last Updated: November 18, 2023

Record last verified: 2023-11

Locations

RU (1)