Bioavailability Clinical Trial of Oral Minoxidil 1 mg

NCT06015516 | Completed Phase 1

• 2 other identifiers: P23112a2023-503796-14-00
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

Brief Summary

The goal of this clinical trial is to learn about the pharmacokinetic profile (behaviour of the drug in the body) of a new oral formulation of minoxidil administered in healthy volunteers. The main question that is to answer is to evaluate the bioavailability of the oral test formulation of minoxidil. The secondary onjectives is to compare it with the formulation already on the market (i.e . Regaxidil® 20 mg/mL cutaneous solution). It is planned that 14 healthy female volunteers of legal age (without any known pathology) participate in the study. The expected duration of the study is approximately 23-56 days. Each volunteer that decide to participate in this study will be sequentially administered one of the formulations planned for the study: either the test formulation (oral minoxidil tablets of 1 mg, developed by Industrial Farmacéutica Cantabria, S.A.), or the reference formulation (minoxidil skin solution, 20 mg/mL, marketed by Industrial Farmacéutica Cantabria, S.A.). After five days of administration of one of the study formulations, at least 7 days will elapse before starting an additional five days of administration of the other study formulation that had not been administered in the first sequence. Assignment to this sequence of administration of the study formulations (oral formulation or topical solution) shall be completely randomised. In each of these sequential periods of five days of administration of the study formulations, the concentration of minoxidil will be quantified in blood samples, which will be taken from each of the volunteers at certain times after the administration of the medication. These blood analyses will enable to determine the parameters that define the pharmacokinetic profile of the new oral formulation under study.

Conditions

Healthy

Keywords

Bioavailability; Clinical trial; minoxidil

Outcome Measures

Primary Outcomes (2)

• Area Under the Curve From Time Zero to the last determination (AUC0-t and AUC(0-τ)ss) for minoxidil.

  According to the recommendations of the regulatory authorities, for the analysis of the compared bioavailability of the formulations from single dose and under steady-state conditions, the primary endpoint will be the area under the curve during a dosage interval (AUC0-t and AUC(0-τ)ss) calculated using the linear trapezoidal method, maximum plasma concentration (Cmax and Cmax,ss) and concentration at the end of the dosing interval (Cτ,ss) at steady state calculated from the plasma concentrations of minoxidil.

  Day 0 (pre-dose) and at multiple time-points (up to day 5) post-dose.

• Maximum observed plasma concentration (Cmax and Cmax,ss) for minoxidil from time zero to the last determination at steady state (Cτ,ss).

  Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. According to the recommendations of the regulatory authorities, for the analysis of the compared bioavailability of the formulations from single dose and under steady-state conditions, the primary endpoint will be the area under the curve during a dosage interval (AUC0-t and AUC(0-τ)ss) calculated using the linear trapezoidal method, maximum plasma concentration (Cmax and Cmax,ss) and concentration at the end of the dosing interval (Cτ,ss) at steady state calculated from the plasma concentrations of minoxidil.

  Day 0 (pre-dose) and at multiple time-points (up to day 5) post-dose.

Secondary Outcomes (3)

• Area Under the Curve (AUC) for both minoxidil formulations.

  Day 0 (pre-dose) and at multiple time-points (up to day 5) post-dose.

• Maximum Plasma Concentration (Cmax) and Peak Cmax steady state for both minoxidil formulations.

  Day 0 (pre-dose) and at multiple time-points (up to day 5) post-dose.

• To evaluate the safety and tolerability of oral minoxidil .

  Day 0 (pre-dose) and at multiple time-points (up to day 5) post-dose.

Study Arms (2)

Treatment Test: Oral minoxidil 1 mg tablets

EXPERIMENTAL

Participants will be administered one tablet of oral minoxidil 1mg once a day, orally, after fasting for at least 10 hours, with 240 mL or 8 Oz. of water, and fasting for a further 5 hours.

Drug: Minoxidil Tablets

Treatment Reference: Regaxidil 20 mg/ml (2%) topical solution

ACTIVE COMPARATOR

Participants will be administered topically on the scalp after fasting for at least 10 hours pre-dose and 5 hours post-dose. After the administration subject should not wash her head for at least 5 hours. Each one mL dose of 2% topical minoxidil will be carefully measured to provide 20 mg of minoxidil using the syringe provided with each bottle.

Drug: Minoxidil topical solution 20 mg/ml

Interventions

Minoxidil Tablets DRUG

Since oral minoxidil is a new formulation and, according to the recommendations of the Regulatory Authorities, it is considered appropriate to carry out a multiple dose study to evaluate and to compare the bioavailability between both formulations (oral versus topical solution), measuring the plasma concentrations of minoxidil. Achievement of steady-state is assessed by comparing at least three pre-dose concentrations for each formulation, as half-life of minoxidil is around 4 hours, we will administered 5 doses in each period.

Treatment Test: Oral minoxidil 1 mg tablets

Minoxidil topical solution 20 mg/ml DRUG

Since oral minoxidil is a new formulation and, according to the recommendations of the Regulatory Authorities, it is considered appropriate to carry out a multiple dose study to evaluate and to compare the bioavailability between both formulations (oral versus topical solution), measuring the plasma concentrations of minoxidil. Achievement of steady-state is assessed by comparing at least three pre-dose concentrations for each formulation, as half-life of minoxidil is around 4 hours, we will administered 5 doses in each period.

Treatment Reference: Regaxidil 20 mg/ml (2%) topical solution

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: female
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Women, who after receiving information about the study design, the objectives, the possible risks that could be derived from it and the fact that they can refuse to collaborate at any time, give their written informed consent to participate in the study.
• Aged from 18 to 55 years old.
• No clinically significant organic or psychic conditions.
• No clinically significant abnormalities in medical records and physical examination.
• No clinically significant abnormalities in haematology, coagulation, biochemistry, serology (Ag HBs, HC antibodies, HIV antibodies) and urinalysis.
• No clinically significant abnormalities in vital signs and electrocardiogram.
• Women of child-bearing potential age women participating in the study will compromise to use a high effective contraceptive method or will be abstinent during their participation in the study.

You may not qualify if:

• Subjects affected by an organic or psychic condition. Before a volunteer is included, all the safety parameters defined in points 7.3 will be considered. Those who present clinically significant analytical alterations and in whom biochemical kidney and/or liver damage markers are outside the normal range applied by the laboratory will be excluded \[GOT, GPT and/or GGT \>2.5\*ULN and total bilirrubin \>1.5\*ULN (total bilirrubin \>1.5\*ULN is acceptable if the direct bilirrubin is \<35%)\].
• Subjects who have received prescribed pharmacological treatment in the last 15 days or abstinent of medication in the 48 hours prior to receiving the study medication, but women are allowed taking contraceptives. Contraceptive methods must be used at least 4 weeks prior to entry visit and not to be changed for the duration of the study.
• Subjects with body mass index (weight (kg)/height2 (m2)) outside the 18.5-30.0 range.
• History of sensitivity to any drug.
• Positive drug screening for cannabis, opiates, cocaine and amphetamines.
• Smoker.
• Daily consumers of alcohol and/or acute alcohol poisoning over the last week.
• Having donated blood in the last month before start of the study.
• Pregnant or breastfeeding women.
• Participation in another study with administration of investigational drugs in the previous 3 months (if the study was conducted with drug substances marketed in Spain, a period of at least 1 month or 5 half lives, what is longer, will be considered).
• Inability to follow the instructions or collaborate during the study.
• History of difficulty in swallowing
• Alterations on the scalp such as erythema, dryness or any other condition that at investigator criteria could affect the absortion of the topical solution.

Sponsors & Collaborators

• Industrial Farmacéutica Cantabria, S.A.: lead

Study Sites (1)

Hospital Universitario de la Princesa

Madrid, 28006, Spain

Location

Related Publications (3)

• Messenger AG, Rundegren J. Minoxidil: mechanisms of action on hair growth. Br J Dermatol. 2004 Feb;150(2):186-94. doi: 10.1111/j.1365-2133.2004.05785.x.

  PMID: 14996087 BACKGROUND

• Shamsaldeen OS, Al Mubki T, Shapiro J. Topical agents for hair growth promotion: what is out there? Skin Therapy Lett. 2013 Jun;18(4):5-7.

  PMID: 24310642 BACKGROUND

• Vano-Galvan S, Pirmez R, Hermosa-Gelbard A, Moreno-Arrones OM, Saceda-Corralo D, Rodrigues-Barata R, Jimenez-Cauhe J, Koh WL, Poa JE, Jerjen R, Trindade de Carvalho L, John JM, Salas-Callo CI, Vincenzi C, Yin L, Lo-Sicco K, Waskiel-Burnat A, Starace M, Zamorano JL, Jaen-Olasolo P, Piraccini BM, Rudnicka L, Shapiro J, Tosti A, Sinclair R, Bhoyrul B. Safety of low-dose oral minoxidil for hair loss: A multicenter study of 1404 patients. J Am Acad Dermatol. 2021 Jun;84(6):1644-1651. doi: 10.1016/j.jaad.2021.02.054. Epub 2021 Feb 24.

  PMID: 33639244 BACKGROUND

Related Links

• Summary of Product Characteristics (SmPC): Minoxidil 20 mg/ml solución cutánea
• Summary of Product Characteristics (SmPC): Minoxidil 10 mg tablets.

MeSH Terms

Interventions

Minoxidil

Intervention Hierarchy (Ancestors)

Piperidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Pyrimidines

Study Officials

• Dolores Ochoa Mazarro

  Clinical Trial Unit, Clinical Pharmacology Department Hospital Universitario de La Princesa (Madrid, Spain)

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: SINGLE
• Who Masked: OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 31, 2023
• First Posted: August 29, 2023
• Study Start: February 9, 2024
• Primary Completion: March 8, 2024
• Study Completion: March 8, 2024
• Last Updated: August 21, 2024

Record last verified: 2024-03

Data Sharing

• IPD Sharing: Will not share

Locations

ES (1)