Phase 1 Pharmacokinetic Study of Minoxidil SL Tablets

A Phase 1 Randomized, Double Blind, Crossover Pharmacokinetic Study of Minoxidil Sublingual Tablets in Adult Male and Female Healthy Volunteers.

This is a phase 1 randomized, double blind, crossover study examining the pharmacokinetic profile of two different doses of minoxidil sublingual tablets in healthy adult volunteers.

The main objective is to determine the pharmacokinetics of minoxidil following sublingual administration of a single dose in adult male and female healthy volunteers. The secondary objective is to evaluate the safety of minoxidil following sublingual administration of a single dose in adult male and female healthy volunteers.

A total of 12 participants (6 male and 6 female) will be recruited for study participation.

The duration of study participation is up to 43 days including screening and safety follow up. A single dose of study medication (strength A or strength B) will be administered on Day 1 to all study participants and PK samples will be taken periodically over a 12-hr period. After at least 7-day washout period the other dose of study medication (strength B or strength A, respectively) will be administered to all participants and PK samples will be taken periodically over a 12-hr period.

Study Overview

• Status: Completed
• Conditions: Pharmacokinetic
• Intervention / Treatment: Drug: Strength A Sublingual Minoxidil; Drug: Strength B Sublingual Minoxidil

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• Australia
  • Victoria
    • East Melbourne, Victoria, Australia, 3002
      • Dr Rodney Sinclair Pty Ltd

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Male and female subjects between 18 and 65 years of age (inclusive) at screening.
• In good general health in the opinion of the Investigator based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitoring (ECG). A subject with a clinical abnormality or laboratory parameters outside the reference range for the population being studied may be included only if, in the opinion of the Investigator, the finding is (a) unlikely to introduce additional risk to the subject, (b) will not interfere with study procedures or confound study results, and (c) is not listed in the Exclusion Criteria.
• Body mass index (BMI) is between 18.5 - 30.0 kg/m2 with a body weight of at least 50 kg.
• Have systolic blood pressure within normal limits (90-140 mm Hg).
• Have adequate venous access on their left or right arm to allow collection of multiple blood samples.
• Women of Childbearing Potential (WOCBP) must agree to use a highly effective method of contraception from enrolment to the safety follow-up visit.
• Women of non-childbearing potential must be post-menopausal or permanently sterilised at least 6 months prior to screening.
• All WOCBP must have a negative serum pregnancy test at screening and a negative urine pregnancy test before dosing on each dosing day.
• Willing and able to attend all study visits and comply with treatment plan and required study procedures.
• Able to comprehend and willing to sign and date a written informed consent form.

Exclusion Criteria:

• History of hypersensitivity or allergies to any ingredients contained in the study medication.
• A positive urine drugs of abuse screen at Screening or alcohol breath test on dosing days, unless for a legitimate medical reason as determined by the Investigator.
• A positive Hepatitis B surface antigen, Hepatitis C antibody result, or human immunodeficiency virus (HIV) result at screening.
• Current participation in any other investigational drug or medical device trial, which includes administration of an investigational study medication or medical device, or within 3 months or 5 half-lives of the investigational product, whichever is longer, prior to receiving first dose.
• Unwilling to comply with all study procedures and assessments.
• Participants with specific underlying conditions (e.g. cardiovascular disease, cardiac arrhythmia, hepatic comorbidity, renal comorbidity, phaeochromocytoma), clinically significant findings from medical history, clinical laboratory tests, ECG, or vital signs that, in the opinion of the Investigator, could interfere with the objectives of the study or put the participant at risk.
• Use of anti-hypertensive medication or any other medications that, in the opinion of the Investigator, could interfere with the objectives of the study or put the participant at risk, within 14 days or 5 half-lives (whichever is longer) before the start of the study treatment.
• A history of alcoholism, substance or drug abuse-related disorders in the past year as deemed significant by the Investigator.
• Pregnant, planning a pregnancy, or nursing a child.
• Major surgery within 4 weeks prior to the screening evaluation, or planned surgery prior to completion of all study procedures.
• Donation of blood or blood products of 470 mL or greater within 12 weeks prior to dosing in Period 1.
• Dietary requirements that prevent consumption of the standardised study meals.
• Poor complier or unlikely to attend specified study days.
• Study site or Sponsor employee, or immediate family member of a study site or Sponsor employee.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Triple

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Strength A Sublingual Minoxidil	Drug: Strength A Sublingual Minoxidil; One single dose of Strength A sublingual minoxidil
Experimental: Strength B Sublingual Minoxidil	Drug: Strength B Sublingual Minoxidil; One single dose of Strength B sublingual minoxidil

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area under the concentration-time profile (AUClast, AUCinf) of sublingual minoxidil	The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). AUClast measures the total minoxidil exposure in the body up to the last measurable time point, while AUCinf estimates total minoxidil exposure from the time it's taken until it completely leaves the body.	At Day 1 and Day 8
Maximum observed concentration (Cmax) of sublingual minoxidil	The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). Cmax is the highest concentration of minoxidil in the blood after it's taken.	At Day 1 and Day 8
Time of maximum observed concentration (Tmax) of sublingual minoxidil	The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). Tmax measures the time it takes for minoxidil to reach its highest concentration in the blood after it's taken.	At Day 1 and Day 8
Terminal rate constant (λz) of sublingual minoxidil	The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). The terminal rate constant measures the speed at which the concentration of minoxidil decreases in the blood during the last stage of elimination.	At Day 1 and Day 8
Terminal half-life (T½) of sublingual minoxidil	The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). The terminal half-life measures the time it takes for the concentration of minoxidil in the blood to decrease by half during the last stage of elimination.	At Day 1 and Day 8

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Type of adverse events	The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.	At Day 1, Day 8, and Day 15
Incidence of Adverse Events	The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.	At Day 1, Day 8, and Day 15
Relationship of adverse events to study drug	The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.	At Day 1, Day 8, and Day 15
Severity of adverse events	The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.	At Day 1, Day 8, and Day 15
Change from baseline in clinical safety monitoring parameters	The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.	At Day 1, Day 8, and Day 15

Collaborators and Investigators

• Sponsor: Samson Clinical Operations Pty Ltd

Study record dates

Study Major Dates

• Study Start (Actual): November 6, 2024
• Primary Completion (Actual): December 23, 2024
• Study Completion (Actual): December 23, 2024

Study Registration Dates

• First Submitted: October 21, 2024
• First Submitted That Met QC Criteria: November 6, 2024
• First Posted (Actual): November 7, 2024

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: February 13, 2025
• Last Verified: February 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Vasodilator Agents; Antihypertensive Agents; Minoxidil
• Other Study ID Numbers: SAM-001

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No