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

NCT05547503 | Completed Phase 1 DMC FDA Drug

• 1 other identifier: AFA-281-001
• Study Type: interventional
• Target: 64
• Locations: 1 country
• Sites: 1

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.

Conditions

Pain, Neuropathic; Pain, Inflammatory

Outcome Measures

Primary Outcomes (12)

• Treatment-Related Adverse Events

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

  Predose and Up to 72 hours after dose

• Heart rate

  Heart rate as one of vital signs will be measured

  Predose and Up to 72 hours after dose

• Body temperature

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

  Predose and Up to 72 hours after dose

• Blood Pressure

  Blood pressure as one of vital signs will be measured

  Predose and Up to 72 hours after dose

• Electrocardiogram (ECG)

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

  Pre-dose and up to 72 hours after dose

• Blood chemistry

  Blood chemistry parameters will be measured

  Pre-dose and up to 72 hours after dose

• Hematology

  Hematology parameters will be measured

  Pre-dose and up to 72 hours after dose

• Coagulation

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

  Pre-dose and up to 72 hours after dose

• Urinalysis

  Urinalysis parameters will be measured using dipstick and microscopic examination.

  Pre-dose and up to 72 hours after dose

• Blood maximum plasma concentration (Cmax) of the study drug

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

  Pre-dose and up to 72 hours after dose

• Blood study drug half-life (t1/2)

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

  Pre-dose and up to 72 hours after dose

• Area under the plasma concentration versus time curve (AUC) of the study drug

  Pharmacokinetics parameter AUC will be measured

  Pre-dose and up to 72 hours after dose

Secondary Outcomes (5)

• A dose and exposure relationship

  Pre-dose and up to 72 hours after dose

• Tmax of the study drug (parent compound) in blood

  Up to 72 hours after dose

• Plasma Concentration (Cmax) of the major metabolite in blood

  Up to 72 hours after dose

• Area under the plasma concentration versus time curve (AUC) of the major metabolite in blood

  Up to 72 hours after dose

• The major metabolite half-life (t1/2) in blood

  Up to 72 hours after dose

Study Arms (2)

Placebo Control

PLACEBO COMPARATOR

Double blind placebo control

Drug: AFA-281

AFA-281

EXPERIMENTAL

Part 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.

Drug: AFA-281

Interventions

AFA-281 DRUG

Part 1: AFA-281 will be administered as a single dose at 4 dose levels (TBD) Part 2: AFA-281 will be administered twice daily for 14 - 21 days at 3 dose levels (TBD)

AFA-281; Placebo Control

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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.

You may not qualify if:

• Participants with significant medical history or clinically significant abnormalities
• Participants with clinically significantly pathologic abnormalities
• Participants with ECG abnormalities

Sponsors & Collaborators

• Afasci Inc: lead
• Cognitive Research Corporation: collaborator

Study Sites (1)

CenExcel CNS

Los Alamitos, California, 90720, United States

Location

MeSH Terms

Conditions

Neuralgia; Pain

Condition Hierarchy (Ancestors)

Peripheral Nervous System Diseases; Neuromuscular Diseases; Nervous System Diseases; Neurologic Manifestations; Signs and Symptoms; Pathological Conditions, Signs and Symptoms

Study Officials

• Xinmin Xie, MD, PhD

  Afasci Inc

  STUDY CHAIR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Masking Details: Part 1 and Part 2 studies are double-blind placebo controlled
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Part 1: Single escalation dose Part 2: Multiple escalation doses for 14 days

Study Record Dates

• First Submitted: September 14, 2022
• First Posted: September 21, 2022
• Study Start: April 11, 2023
• Primary Completion: December 4, 2024
• Study Completion: May 14, 2025
• Last Updated: October 21, 2025

Record last verified: 2025-10

Data Sharing

• IPD Sharing: Will share
• Shared Documents: SAP, ICF
• Time Frame: One year after completion of the study and 6 months after publication
• Access Criteria: To be added

Locations

US (1)