An Open Label Pharmacokinetic Study of ASP-001 Formulations in Healthy Volunteers

NCT07445464 | Not Yet Recruiting Phase 1

• 1 other identifier: ASP-001-01
• Study Type: interventional
• Target: 12
• Locations: 0 countries
• Sites: N/A

Brief Summary

This study will assess the pharmacokinetics (PKs), safety and tolerability of ASP-001 in healthy volunteers. ASP-001 is an orally disintegrating tablet (ODT) formulation of flunarizine. This study will assess two formulations, Formulation A and Formulation B, at dose levels of 2 and 5 mg compared to the reference product, the Sibelium brand of flunarizine 5 mg tablet. Whilst this is not a first-in-human (FIH) study of flunarizine, which is available in countries outside of Australia and has been studied extensively, it is a FIH study of ASP-001. In this open-label study, 12 participants will be assigned to one of five dosing sequences, in which they will receive a single dose of ASP-001 or Sibelium 5 mg in five separate dosing periods. The study drugs will be:

• Treatment A: ASP-001 Formulation A, 5 mg
• Treatment B: ASP-001 Formulation A, 2 mg
• Treatment C: ASP-001 Formulation B, 5 mg
• Treatment D: ASP-001 Formulation B, 2 mg
• Treatment E: Sibelium, 5 mg Each dosing period will be separated by at least a 7-day washout period after the day of dosing. Approximately 14 days after the fifth and final dosing day, participants will return to the site to complete their end of study assessments. Aboriginal and Torres Strait Islander participants will not be targeted directly; however, they will be permitted to be on-study if they meet all of the eligibility criteria. Participants under the age of 18 will not be permitted on study.

Conditions

Pharmacokinetic Analysis

Outcome Measures

Primary Outcomes (9)

• Frel

  relative bioavailability calculated on the ratio of intervention to control

  Through Study Day 5 for each intervention and control

• AUC(0-inf)

  area under the concentration-time curve from time zero to infinity (extrapolated)

  Through Study Day 5 for each intervention and control

• AUC(0-t)

  area under the concentration-time curve from time zero until the last observed concentration

  Through Study Day 5 for each intervention and control

• Cmax

  maximal observed concentration

  Through Study Day 5 for each intervention and control

• Tmax

  time when the maximal concentration is observed

  Through Study Day 5 for each intervention and control

• T½ el

  terminal elimination half-life

  Through Study Day 5 for each intervention and control

• Kel

  terminal elimination rate constant

  Through Study Day 5 for each intervention and control

• Cl/F

  Apparent clearance

  Through Study Day 5 for each intervention and control

• Vz/F

  apparent volume of distribution

  Through Study Day 5 for each intervention and control

Secondary Outcomes (3)

• Evaluate the safety and tolerability

  Throughout the study period

• Metabolic Profile

  Through Study Day 5 for each intervention and control

• Dose Proportionality

  Through Study Day 5 for each intervention and control

Study Arms (5)

Treatment A: ASP-001 Formulation A, 5 mg

EXPERIMENTAL

Drug: Flunarizine

Treatment B: ASP-001 Formulation A, 2 mg

EXPERIMENTAL

Drug: Flunarizine

Treatment C: ASP-001 Formulation B, 5 mg

EXPERIMENTAL

Drug: Flunarizine

Treatment D: ASP-001 Formulation B, 2 mg

EXPERIMENTAL

Drug: Flunarizine

Treatment E: Sibelium, 5 mg

ACTIVE COMPARATOR

identical active ingredient

Drug: Flunarizine

Interventions

Flunarizine DRUG

ODT formulation for buccal administration

Treatment A: ASP-001 Formulation A, 5 mg; Treatment B: ASP-001 Formulation A, 2 mg; Treatment C: ASP-001 Formulation B, 5 mg; Treatment D: ASP-001 Formulation B, 2 mg

Eligibility Criteria

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

You may qualify if:

• Male or female, ≥18 and ≤65 years of age at screening, with body mass index (BMI) ≥18.5 and ≤32.0 kg/m2 and body weight ≥50.0 kg for males and ≥45.0 kg for females.
• Healthy as defined by:
• the absence of clinically significant illness and surgery (including abdominal or gastrointestinal surgery that may alter drug absorption) within 4 weeks prior to dosing.
• the absence of clinically significant history of neurological (including Parkinson's disease or other extrapyramidal disorders), endocrine, cardiovascular, respiratory, hematological, immunological, psychiatric (including depression), gastrointestinal, renal, hepatic, and metabolic disease.
• Non smoker, defined as no use of tobacco or nicotine containing products (including cigarettes, e cigarettes, cigars, pipes, or smokeless tobacco) for at least 6 months prior to screening.
• Female participants of non-childbearing potential must be:
• post-menopausal (spontaneous amenorrhea for at least 12 months prior to dosing) with confirmation by documented follicle stimulating hormone (FSH) levels ≥40 mIU/mL; or
• surgically sterile (bilateral oophorectomy, bilateral salpingectomy, or hysterectomy) or having had a tubal ligation performed at least 3 months prior to dosing.
• Sexually active female participants of childbearing potential and non-sterile male participants must be willing to use an acceptable contraceptive method throughout the study as detailed in section 7.1.
• Willing to take off dentures or mouth piercing at the time of dosing.
• Able to understand the study procedures and provide signed informed consent to participate in the study.

You may not qualify if:

• Any clinically significant abnormal finding at physical examination at screening.
• PHQ-9 score \> 10 at screening or baseline (Day -1).
• Clinically significant abnormal laboratory test results or positive serology test results for HBsAg, HCV antibody, or HIV antigen and antibody at screening. Any abnormalities or deviations outside the normal ranges for any clinical laboratory testing can be repeated once at the discretion of the investigator and/or designee.
• Any of the following laboratory parameters above 1.5× upper limit of normal (ULN) at screening or baseline (Day -1): AST, ALT, direct bilirubin, indirect bilirubin, and total bilirubin. Values over 1.5× ULN may be repeated once for confirmation if the investigator considers it reasonable (e.g., potential elevation due to recent strenuous physical activity).
• Value of creatinine clearance (CrCl) \<60 mL/min, as estimated by the Cockcroft-Gault equation.
• Positive pregnancy test or lactating female participant.
• Positive urine drug screen, urine cotinine test, or alcohol breath test.
• Known allergic reactions to flunarizine or other related drugs, or to any excipient in the formulation.
• Clinically significant ECG abnormalities or vital signs abnormalities (systolic blood pressure lower than 90 or over 140 mmHg, diastolic blood pressure lower than 40 or over 90 mmHg, or heart rate less than 40 or over 100 bpm) at screening. Any abnormalities or deviations outside the normal range for vital signs and ECG can be repeated at the discretion of the investigator and/or designee.
• History of drug abuse within 1 year prior to screening or recreational use of marijuana within 1 month, or use of cocaine, phencyclidine \[PCP\], crack, opioid derivatives (including heroin) or amphetamine derivatives within 3 months prior to screening.
• History of alcohol abuse within 1 year prior to screening or regular use of alcohol within 6 months prior to screening that exceeds 14 standard drinks for females or 21 standard drinks for males of alcohol per week (1 standard drink = 375 mL of mid-strength beer 3.5% alcohol/volume, 100 mL of wine 13.5% alcohol/volume, or 30 mL of distilled alcohol 40% alcohol/volume).
• Use of medications within the the following timeframes prior to dosing:
• Depot injections or drug implants: within 3 months.
• Strong CYP2D6 inhibitors or strong CYP inducers such as fluoxetine, paroxetine, bupropion, quinidine, cinacalcet, terbinafine, mirabegron, darifenacin, rifampin, carbamazepine, phenytoin, phenobarbital, and St. John's wort: within 30 days.
• Prescription medications: within 14 days.

Sponsors & Collaborators

• Aspartes Pharmaceuticals, Inc.: lead

MeSH Terms

Interventions

Flunarizine

Intervention Hierarchy (Ancestors)

Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Peter Schrader, MBBS, FRACP

  Linear Clinical Research

  PRINCIPAL INVESTIGATOR

Central Study Contacts

Paul Glidden, PhD

CONTACT

1 9055129873; admin@aspartes.com

Denny Medjedovic

CONTACT

1 9055129873; admin@aspartes.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: 5-way, randomized, open-label, sequential single administration under fasting conditions

Study Record Dates

• First Submitted: February 21, 2026
• First Posted: March 3, 2026
• Study Start: April 9, 2026
• Primary Completion: June 2, 2026
• Study Completion: July 1, 2026
• Last Updated: March 3, 2026

Record last verified: 2026-02

Data Sharing

• IPD Sharing: Will not share