NPC-12G Gel 0.2% Sirolimus PK Bridging Study

Open-label, Fixed-sequence, Two-period Comparative Bioavailability Study of Sirolimus From Topical Application of NPC-12G Gel to Oral Rapamune® Following Single Administration in Healthy Subjects Under Fasting Conditions

This study is designed to describe the relative systemic bioavailability of topical and oral sirolimus formulations.

Study Overview

• Status: Completed
• Conditions: Bioavailability Study
• Intervention / Treatment: Drug: NPC-12G Gel 0.2%; Drug: Rapamune® 2 mg tablet

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

Contacts and Locations

Study Locations

• United States
  • Florida
    • Miami, Florida, United States, 33136
      • inVentiv Health Clinical Research Services LLC

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 14 years to 61 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria

• Male or female, non-smoker (no use within 3 months prior to screening), ≥ 18 and ≤ 65 years of age, with BMI > 18.5 and < 30.0 kg/m2 and body weight ≥ 50.0 kg for males and ≥ 45.0 kg for females
• Females of childbearing potential who are sexually active with a male partner must be willing to use one of acceptable contraceptive method throughout the study and for 12 weeks after the last study drug administration

Exclusion Criteria

• Any sign of eczema/dermatitis, skin lesion, wound, or infection at the application site, or any other conditions that would prevent a safe application of the gel formulation.
• Laser or surgery at the gel application site within 2 weeks before the gel application.
• Positive alcohol breath test, urine drug screen or urine cotinine test at screeningation
• History of allergic reactions or hypersensitivity to sirolimus, sirolimus derivatives, or excipient of NPC-12G Gel
• Use of any drugs known to induce or inhibit CYP3A4 metabolism within 30 days prior to the first study drug administration
• Positive pregnancy test at screening
• Breast-feeding subject
• History of active tuberculosis or exposure to endemic areas within 8 weeks prior to QuantiFERON®-TB testing performed at screening
• Positive QuantiFERON®-TB test with positive chest X-ray, indicating possible tuberculosis infection
• Immunization with a live attenuated vaccine within 1 month prior to dosing or planned vaccination during the study and up to 3 weeks after the last study drug administration

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: Non-Randomized
• Interventional Model: Sequential Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: NPC-12G Gel 0.2% (Period 1); A single 800 mg quantity weight (1.6 mg sirolimus) dose will be applied to the central face on Day 1.	Drug: NPC-12G Gel 0.2%; Period 1; Other Names: 2 mg of sirolimus in 1 g of gel
Active Comparator: Rapamune Tablet (Period 2); Rapamune® (sirolimus) 2 mg tablet for oral dosing.	Drug: Rapamune® 2 mg tablet; Period 2; Other Names: Sirolimus

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
AUC0-48	Sampling: Pre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, and 48 hours post-dose
Cmax	Sampling: Pre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, and 48 hours post-dose
Tmax	Sampling: Pre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, and 48 hours post-dose

Collaborators and Investigators

• Sponsor: Nobelpharma

Study record dates

Study Major Dates

• Study Start (Actual): May 31, 2019
• Primary Completion (Actual): June 17, 2019
• Study Completion (Actual): June 17, 2019

Study Registration Dates

• First Submitted: May 24, 2019
• First Submitted That Met QC Criteria: May 31, 2019
• First Posted (Actual): June 3, 2019

Study Record Updates

• Last Update Posted (Actual): March 6, 2020
• Last Update Submitted That Met QC Criteria: March 4, 2020
• Last Verified: May 1, 2019

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Anti-Infective Agents; Antineoplastic Agents; Immunosuppressive Agents; Immunologic Factors; Anti-Bacterial Agents; Antibiotics, Antineoplastic; Antifungal Agents; Sirolimus
• Other Study ID Numbers: NPC-12G-4/US

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: Yes
• Studies a U.S. FDA-regulated device product: No