Bioavailability and Tolerability of Fexofenadine Hydrochloride Topical Lotion 1% (ATOFEX-1)

An Open Label, Single-Dose, Single-Treatment, Single-Period Safety and Bioavailability Study of Fexofenadine Hydrochloride Topical Lotion 1% in Healthy, Adult, Male Human Subjects

The investigational lotion is envisaged as an short- and long term "Ease & Prevent" monotherapy for adults and children with mild to moderate eczema. With itch representing the most burdensome symptom in eczema, the main objectives with the lotion is fast and efficient itch relief, high tolerability, and high short- and long term safety. This phase 1 study aims to monitor skin tolerability, and how much of the active compound that is absorbed to the bloodstream.

Study Overview

• Status: Completed
• Conditions: Psoriasis; Eczema; Pruritus; Atopic Dermatitis; Psoriasis Vulgaris; Urticaria; Skin Rash; Urticaria Chronic; Skin Inflammation; Atopic Dermatitis Eczema; Rash; Atopic Rash
• Intervention / Treatment: Drug: Fexofenadine Hydrochloride Topical Lotion 1% (OP2101)

Detailed Description

Fexofenadine Hydrochloride Topical Lotion 1% (OP2101) is a novel formulation developed for the treatment of skin disorders characterized by pruritus. Research show that oral Fexofenadine Hydrochloride (FX) may lead to a small improvement of pruritus in patients with Atopic Dermatitis (AD). In clinical practice, oral antihistamines are widely used off-label for pruritus relief in AD, indicating a discrepancy in trial outcomes and real-life experience. The pre-study thesis postulates that the antipruritic effect of FX can be leveraged in a dose-response relationship facilitated by high topical concentration of FX in direct contact with the pathological process of the skin. The sponsor also suggest that the Cytosolic phospholipase A2 (cPLA2) blocking property of FX is an untapped resource that is likely to be dose-response dependent and manifested by means of high topical concentration in proximity to the inflammatory process. The repositioning of FX to a topical treatment has the potential for high safety, efficacy, fast relief, and ease of use. OP2101 is also aimed at inflammation control, suppression of bacterial imbalance, moisture retention, upregulation of antimicrobial peptides, and skin barrier restoration. As such, it targets six of the pathological pillars of AD. Assessment of topical tolerability and skin adsorption (systemic exposure) are the main objectives in this phase 1 study.

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

Contacts and Locations

Study Locations

• Bangladesh
  • Ramna
    • Dhaka, Ramna, Bangladesh, 1217
      • BCT Ltd.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

1. Healthy male human subjects between 18 to 45 years of age (both inclusive).
2. Having a Body Mass Index (BMI) between 18.5 and 30.0 kg/m2 (both inclusive).
3. Have no abnormal findings during screening done 21 days prior to administration of study drug, medical history and examination, laboratory evaluations, 12-lead ECG recordings.
4. Has an optimum physical condition which enables subjects to be fit for a Pharmacokinetic sampling according to principal investigator's evaluation.
5. Able to comply with the study procedures in the opinion of the PI/CI.
6. Able to give written consent for participation in the study.
7. Subjects who have taken at least two doses of COVID 19 vaccine and possess certificate for the same.
8. Intact skin without major scarring or tattoos.
9. An unusual diet (e.g., low salt), for any medical reason or non-medical reason for three weeks prior to receiving the study drug and throughout the subjects' participation in the study. In any such case subject selection will be at the discretion of the PI/CI.

Exclusion Criteria:

1. Known hypersensitivity or idiosyncratic reaction to Fexofenadine Hydrochloride or any of the excipients in the formulation.
2. Diagnosed with, or a family history of, long QT syndrome (LQTS).
3. Skin disorders or current skin discomforts.
4. Any disease or condition which might compromise the haemopoietic, renal, hepatic, endocrine, pulmonary, central nervous, cardiovascular, immunological, dermatological, gastrointestinal, genital or any other body system.
5. Ingestion of any medicine at any time within 14 days before Check In. In any such case subject selection will be at the discretion of the PI/CI and medicine taken will be recorded.
6. Any history or presence of asthma (including aspirin induced asthma) or NSAID induced urticaria.
7. History of substance abuse and or addiction to drugs and alcohol.
8. Smokers, who smoke 9 or more cigarettes / day or inability to abstain during the study.
9. Habituated to drinking tea or coffee (more than 5 cups/day) or inability to abstain during the study
10. Habituated to tobacco/tobacco containing products (more than 10 gm/day) or inability to abstain during the study.
11. A positive result for Serological tests [including hepatitis B & C, HIV antibody and syphilis {VDRL (RPR) /TPHA}] tests.
12. Donation of blood (1 unit: 350 mL) within 90 days prior to receiving the first dose of study drug.
13. The receipt of an investigational product or participation in a drug research study within a period of 90 days prior to the first dose of study drug.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm

Intervention / Treatment

Experimental: OP2101; Treatment with Fexofenadine Hydrochloride Topical Lotion 1% (OP2101)

Drug: Fexofenadine Hydrochloride Topical Lotion 1% (OP2101); Intervention: The amount of study lotion (OP2101) used is 11 grams per subject, equivalent to 22 fingertip units (FTU). The lotion is applied to the subject on back and front of the trunk, both hands (palm and back) and both arms. An SOP for handling and application of the lotion ensures the 11 grams covers 54% of the body surface area (BSA) evenly without residue. Comment: The treatment is single-dose and single-treatment. The FTU is used to standardize the amount of cream being applied in clinical research. It is also used in clinical practice and hence connects the objectiveness of the trial to the clinical situation.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse Events	Incidence and severity of local and systemic Adverse Events (AEs).	0-72 hours
Cmax	Peak plasma concentration (Cmax)	0.00 (pre-dose) and at 1.00, 4.00, 8.00, 12.00, 16.00, 24.00, 36.00, 48.00, 60.00- & 72.00-hours post-dosing.
Tmax	Peak plasma time (Tmax)	0.00 (pre-dose) and at 1.00, 4.00, 8.00, 12.00, 16.00, 24.00, 36.00, 48.00, 60.00- & 72.00-hours post-dosing.
T½	Half-life (T½)	0.00 (pre-dose) and at 1.00, 4.00, 8.00, 12.00, 16.00, 24.00, 36.00, 48.00, 60.00- & 72.00-hours post-dosing.
AUC0-72h	Area under the curve (AUC0-72h)	0.00 (pre-dose) and at 1.00, 4.00, 8.00, 12.00, 16.00, 24.00, 36.00, 48.00, 60.00- & 72.00-hours post-dosing.

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Dermal tolerability and treatment perception	Skin- and Lotion Assessment Questionnaire (SLAQ) is a proprietary 3-part questionnaire: Part 1 is a 6-modalities, 4-grade self-assessment of skin perceptions.; Part 2 is the Local Tolerability Scale (LTS).; Part 3 is a 7-modalities, 5-grade assessment of cream properties.	-60 minutes, 30 minutes, 72 hours

Other Outcome Measures

Outcome Measure	Measure Description	Time Frame
Radial pulse	Radial pulse (beats per minute)	At the time of check-in, prior to dosing and at 03.00, 06.00, 12.00, 24.00, 36.00, 48.00, & 60.00 hours (± 60 minutes) post dose and prior to check-out.
Systolic blood pressure	Systolic blood pressure (mmHg)	At the time of check-in, prior to dosing and at 03.00, 06.00, 12.00, 24.00, 36.00, 48.00, & 60.00 hours (± 60 minutes) post dose and prior to check-out.
Diastolic blood pressure	Diastolic blood pressure (mmHg)	At the time of check-in, prior to dosing and at 03.00, 06.00, 12.00, 24.00, 36.00, 48.00, & 60.00 hours (± 60 minutes) post dose and prior to check-out.
Respiratory rate	Respiratory rate (breaths per minute)	0.00 (pre-dose) and at 1.00, 4.00, 8.00, 12.00, 16.00, 24.00, 36.00, 48.00, 60.00- & 72.00-hours post-dosing.
Body temperature	Body temperature (Celsius degrees)	0.00 (pre-dose) and at 1.00, 4.00, 8.00, 12.00, 16.00, 24.00, 36.00, 48.00, 60.00- & 72.00-hours post-dosing.

Collaborators and Investigators

• Sponsor: OrchestratePharma GmbH
• Collaborators: VidiLife Clinical Research Associate

Study record dates

Study Major Dates

• Study Start (Actual): April 1, 2022
• Primary Completion (Actual): October 16, 2022
• Study Completion (Actual): October 16, 2022

Study Registration Dates

• First Submitted: July 2, 2022
• First Submitted That Met QC Criteria: July 13, 2022
• First Posted (Actual): July 18, 2022

Study Record Updates

• Last Update Posted (Actual): March 29, 2023
• Last Update Submitted That Met QC Criteria: March 27, 2023
• Last Verified: March 1, 2023

More Information

Terms related to this study

• Keywords: Psoriasis; Urticaria; Atopic Dermatitis; Pruritus; Eczema; Rash; Inflammatory Skin Disease
• Additional Relevant MeSH Terms: Pathologic Processes; Skin Diseases; Immune System Diseases; Hypersensitivity, Immediate; Genetic Diseases, Inborn; Skin Diseases, Genetic; Skin Diseases, Vascular; Skin Diseases, Papulosquamous; Hypersensitivity; Skin Manifestations; Skin Diseases, Eczematous; Inflammation; Psoriasis; Exanthema; Dermatitis; Eczema; Pruritus; Dermatitis, Atopic; Urticaria; Chronic Urticaria; Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Anti-Allergic Agents; Histamine H1 Antagonists; Histamine Antagonists; Histamine Agents; Histamine H1 Antagonists, Non-Sedating; Fexofenadine
• Other Study ID Numbers: iVRS-CD-22-021

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