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Phase I Single Ascending Dose and Multiple Ascending Doses of Oral AFA-281 in Healthy Volunteers

Phase 1
Recruiting
Conditions
Pain, Neuropathic
Pain, Inflammatory
Interventions
Registration Number
NCT05547503
Lead Sponsor
Afasci Inc
Brief Summary

Phase I Part 1 (single ascending dose):

Double-blind dosing will occur in healthy volunteers in 4 cohorts of 8 subjects each. Six subjects in each cohort will be randomized to receive AFA-281 and 2 subjects will be randomized to receive the matching placebo. At the end of the Part 1 study is to evaluate the safety and tolerability of AFA-281. Following completion of each cohort, bioanalytical analyses will be conducted to evaluate the pharmacokinetic profile.

Phase I Part 2 (multiple dose for 14 days):

Pending the results from Part 1, healthy volunteers will be administered AFA-281 for 14 to 21 consecutive days in 3 cohorts. At scheduled intervals after dosing, and at the end of the cohort's study period to evaluate the safety and tolerability and the pharmacokinetic profile of AFA-281.

Detailed Description

Phase I Part 1 (single ascending dose):

Healthy volunteers will be admitted to the clinical research unit on Day -1. There will be five cohorts with 8 subjects per cohort. Six subjects per cohort will receive AFA-281 at one of 4 doses and 2 will receive placebo. Oral capsules will be administered on the morning of Day 1, following a 10-hour fast. Blood draws for assessment of Pharmacokinetic parameters will occur 0.2-1 hr pre-dose and at 0.5-, 1-, 2-, 3-, 4-, 8-, 10, 12-, 16-, 24-, 36-, 48-hr, and up to 72-hr post-dose. Vital signs will be collected at scheduled times following dosing. A 12-lead ECG will be obtained pre-dose and scheduled at 2, 4, 8, 24 hr, and 3- or 4 days post- dose. Various clinical laboratory tests will be drawn on Day -1, within 1 hr prior to dosing, and at scheduled timepoints after dosing while the volunteer is housed in the research center. Subjects of Cohorts 1 - 3 will be released following completion of blood draws and safety assessments up to 48 hours and Cohorts 4 and 5 subjects will return for 72-hour blood draws and Day 4 ECG and safety assessment.

Phase I Part 2 (multiple ascending doses - 14 days):

After assessment of the safety data from the single dose Phase I Part 1, healthy volunteers will be randomized into 3 cohorts with 8 subjects per cohort. Five subjects per cohort will receive AFA-281 and 3 will receive placebo. Oral capsules will be administered in dose titration and split daily dose in fours time daily (QID) for 14 - 21 consecutive days. Routine clinical monitoring will occur as in Part 1. Baseline physical examination, vital signs, clinical lab tests, and ECGs will be performed prior to dosing, at scheduled intervals after dosing, and at the end of the cohort's study period to evaluate the safety and tolerability, and the pharmacokinetic profile of AFA-281. Reports of potential adverse events will be elicited, and vital signs and 12-lead ECG will be measured in a similar manner to Part 1. Similarly, clinical laboratory tests will be drawn prior to and after dosing.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
58
Inclusion Criteria
  • Participants must be in good general health with no significant medical history and have no clinically significant abnormalities on physical examination at screening and/or before administration of the initial dose of study drug.

    • Participants must have a Body Mass Index (BMI) between 18.0 and 30.0 kg/m2 inclusive.
    • Participants must have clinical laboratory values within normal range as specified by the testing laboratory, unless deemed not clinically significant by the Investigator or delegate.
    • Participants must have an ECG without clinically significant pathologic abnormalities.
Exclusion Criteria
  • Participants with significant medical history or clinically significant abnormalities
  • Participants with clinically significantly pathologic abnormalities
  • Participants with ECG abnormalities

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Placebo ControlAFA-281Double blind placebo control
AFA-281AFA-281Part 1: AFA-281 administered as an oral capsule at 5 dose levels for one day. Part 2: AFA-281 administered as an oral capsule at 3 dose levels twice daily for 14 consecutive days. Doses will be determined after completion of Part 1.
Primary Outcome Measures
NameTimeMethod
Blood maximum plasma concentration (Cmax) of the study drugPre-dose and up to 72 hours after dose

Pharmacokinetics parameter Cmax will be measured to assess drug exposure levels in blood

Treatment-Related Adverse EventsPredose and Up to 72 hours after dose

Number of participants with treatment-related adverse events will be assessed using CTCAE v5.0

Heart ratePredose and Up to 72 hours after dose

Heart rate as one of vital signs will be measured

Body temperaturePredose and Up to 72 hours after dose

Body temperature (0C) as one of vital signs will be measured

Blood PressurePredose and Up to 72 hours after dose

Blood pressure as one of vital signs will be measured

Electrocardiogram (ECG)Pre-dose and up to 72 hours after dose

Triplicate 12-lead ECG will be measured to evaluate electrical activity of the heart

Blood chemistryPre-dose and up to 72 hours after dose

Blood chemistry parameters will be measured

HematologyPre-dose and up to 72 hours after dose

Hematology parameters will be measured

CoagulationPre-dose and up to 72 hours after dose

Coagulation parameters (PT/INR, PTT) will be measured

Blood study drug half-life (t1/2)Pre-dose and up to 72 hours after dose

Pharmacokinetics parameter t1/2 will be measured to evaluate drug half-life in the blood

Area under the plasma concentration versus time curve (AUC) of the study drugPre-dose and up to 72 hours after dose

Pharmacokinetics parameter AUC will be measured

UrinalysisPre-dose and up to 72 hours after dose

Urinalysis parameters will be measured using dipstick and microscopic examination.

Secondary Outcome Measures
NameTimeMethod
Plasma Concentration (Cmax) of the major metabolite in bloodUp to 72 hours after dose

Pharmacokinetics parameter Cmax of a major metabolite will be measured.

Area under the plasma concentration versus time curve (AUC) of the major metabolite in bloodUp to 72 hours after dose

Pharmacokinetics parameter AUC of a major metabolite will be measured.

The major metabolite half-life (t1/2) in bloodUp to 72 hours after dose

Pharmacokinetics parameter t1/2 of a major metabolite will be measured.

A dose and exposure relationshipPre-dose and up to 72 hours after dose

Doses of study drug and blood exposure levels will be analyzed to determine dose proportionality.

Tmax of the study drug (parent compound) in bloodUp to 72 hours after dose

Pharmacokinetics parameter Time at which Cmax of the study drug appeared will be determined.

Trial Locations

Locations (1)

CenExcel CNS

🇺🇸

Los Alamitos, California, United States

CenExcel CNS
🇺🇸Los Alamitos, California, United States
Steven Reynolds, DO
Principal Investigator
Hanna Voltattorni, BS
Contact
714-34-2252
h.voltattorni@cenexel.com
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