Systemic Bioavailability Study Of Col-118 Administered Topically as a 0.18 % Facial Gel And Brimonidine Ophthalmic Solution 0.2%

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
Galderma
ClinicalTrials.gov Identifier:
NCT00697541
First received: June 12, 2008
Last updated: August 6, 2014
Last verified: August 2014
  Purpose

Phase II systemic bioavailability crossover study to measure the exposure of Col-118 topical 0.18 % Facial Gel and Brimonidine Ophthalmic Solution 0.2%


Condition Intervention Phase
Erythematous Rosacea
Drug: 0.18% COL-118 facial gel (1.8 mg brimonidine)
Drug: 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop)
Drug: Advanced Eye Relief
Drug: COL-118 facial gel vehicle
Phase 2

Study Type: Interventional
Study Design: Allocation: Randomized
Endpoint Classification: Bio-availability Study
Intervention Model: Crossover Assignment
Masking: Double Blind (Subject, Caregiver, Investigator, Outcomes Assessor)
Primary Purpose: Treatment
Official Title: A Phase II, Single-Center, Two-Way Crossover Relative Systemic Bioavailability Study of Col-118 Administered Topically as a 0.18 % Facial Gel and Brimonidine Ophthalmic Solution 0.2% Administered to the Eye in Subjects With Moderate to Severe Erythematous Rosacea

Resource links provided by NLM:


Further study details as provided by Galderma:

Primary Outcome Measures:
  • Cmax - Maximum Systemic Concentration of Brimonidine [ Time Frame: 0 Hour (prior to dose) and at 1, 2, 3, 4, 5, 6, 7, and 8 hours post-morning dose ] [ Designated as safety issue: No ]
    Maximum observed plasma concentration

  • AUC - Area Under the Curve of Brimonidine [ Time Frame: 0 Hour (prior to dose) and at 1, 2, 3, 4, 5, 6, 7, and 8 hours post-morning dose ] [ Designated as safety issue: No ]

    Area under the plasma concentration-time curve from 0 hour to the last measurable plasma concentration, calculated by the linear trapezoidal method

    After two topical applications of 0.18% COL-118 facial gel, plasma levels of brimonidine for all subjects were below the LoQ (25 pg/mL), with the exception of one single outlier value.

    Thus, no PK analysis could be performed for 0.18% COL-118 facial gel.

    After ocular administration of 0.2% brimonidine tartrate ophthalmic solution, quantifiable plasma concentrations of brimonidine were observed in 11 of the 18 subjects who received the brimonidine tartrate ophthalmic solution. Brimonidine rapidly appeared in plasma The mean Cmax was not calculated because values were not quantifiable for 7 of 18 subjects The mean AUC0-t also was not calculated.


  • Tmax - Time to Maximum Plasma Concentration [ Time Frame: 0 Hour (prior to dose) and at 1, 2, 3, 4, 5, 6, 7, and 8 hours post-morning dose ] [ Designated as safety issue: No ]
    time to maximum plasma concentration


Enrollment: 20
Study Start Date: May 2008
Study Completion Date: June 2008
Primary Completion Date: June 2008 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: A
One 1-g application of 0.18% COL-118 facial gel (1.8 mg brimonidine) administered topically plus one drop of Advanced Eye Relief™ in each eye, once in the morning. 1 g of 0.18% COL-118 facial gel is reapplied once after four hours
Drug: 0.18% COL-118 facial gel (1.8 mg brimonidine)
One 1-g application of 0.18% COL-118 facial gel (1.8 mg brimonidine) administered topically plus one drop of Advanced Eye Relief™ in each eye, once in the morning. 1 g of 0.18% COL-118 facial gel is reapplied once after 4 hours
Other Name: brimonidine
Drug: Advanced Eye Relief
One 1-g application of 0.18% COL-118 facial gel (1.8 mg brimonidine) administered topically plus one drop of Advanced Eye Relief™ in each eye, once in the morning. 1 g of 0.18% COL-118 facial gel is reapplied once after 4 hours
Active Comparator: B
One 1-g application of COL-118 facial gel vehicle (0.0 mg brimonidine tartrate) administered topically plus one drop of 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop) in each eye. Four hours after the first application 1-g of COL-118 facial gel vehicle (0.0 mg brimonidine) is administered topically
Drug: 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop)
One 1-g application of COL-118 facial gel vehicle (0.0 mg brimonidine tartrate) topically plus one drop of 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop) in each eye. Four hours after the first application 1-g of COL-118 facial gel vehicle (0.0 mg brimonidine) is administered topically.
Other Name: brimonidine tartrate/drop
Drug: COL-118 facial gel vehicle
One 1-g application of COL-118 facial gel vehicle (0.0 mg brimonidine tartrate) administered topically plus one drop of 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop) in each eye. Four hours after the first application 1-g of COL-118 facial gel vehicle (0.0 mg brimonidine) is administered topically

Detailed Description:

A double-blind, randomized, 2-way crossover, safety, pharmacokinetic/-dynamic (PK/PD) study of 0.18% COL-118 facial gel and 0.2% brimonidine ophthalmic solution administered in male and female patients with moderate to severe erythematous rosacea.

Twenty male and female subjects with moderate to severe erythematous rosacea will be randomized into 2 groups of 10 subjects.

Each group will be randomized to receive 2 treatments (Treatments A and B, in Sequence 1: A/B or Sequence 2: B/A), as follows:

Treatment A: One 1-g application of 0.18% COL-118 facial gel (1.8 mg brimonidine) administered topically plus one drop of Advanced Eye Relief™ in each eye, once in the morning. 1 g of 0.18% COL-118 facial gel is reapplied once after four hours;

Treatment B: One 1-g application of COL-118 facial gel vehicle (0.0 mg brimonidine tartrate) administered topically plus one drop of 0.2% brimonidine ophthalmic solution (0.1 mg brimonidine tartrate/drop) in each eye. Four hours after the first application 1-g of COL-118 facial gel vehicle (0.0 mg brimonidine) is administered topically.

There will be at least a 1-day washout between dose administrations (Period 1 and Period 2).

Blood samples for PK analysis of brimonidine levels will be collected at the following time points during Period 1 and Period 2: 0 Hour (prior to dose) and at 1, 2, 3, 4 (prior to 2nd dose), 5, 6, 7, and 8 hours post-dose.

  Eligibility

Ages Eligible for Study:   18 Years and older
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   No
Criteria

Inclusion Criteria:

  • Male or female ≥18 years of age
  • Clinical diagnosis of rosacea
  • A score of ≥ 3 on the CEAS
  • A score of ≥ 3 on the PSA
  • IOP ≥ 10 mm Hg
  • Non-pregnant and non-lactating females

Exclusion Criteria:

  • History of hypersensitivity or allergies to any ingredient of the study drugs, unless approved by the Investigator
  • Use of brimonidine prescription medications within 14 days prior to Check-in
  • Use of any over-the-counter (OTC), non-prescription preparations (including vitamins, minerals, and phytotherapeutic/herbal/plant-derived preparations) within 7 days prior to Check-in, unless deemed acceptable by the Investigator
  • Use of systemic or topical steroids applied to the face 14 days prior to Check in
  • The use of any Rx or OTC products for the treatment of acne or rosacea within 14 days prior to check in
  • The use of isotretinoin within 180 days prior to check in
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT00697541

Locations
United States, Pennsylvania
KGL, Inc.
Broomall, Pennsylvania, United States, 19008
Sponsors and Collaborators
Galderma
Investigators
Principal Investigator: James Leyden, M.D. KGL, Inc.
  More Information

No publications provided

Responsible Party: Galderma
ClinicalTrials.gov Identifier: NCT00697541     History of Changes
Other Study ID Numbers: COL-118-ROSE-202, RD.06.SPR.18126
Study First Received: June 12, 2008
Results First Received: September 19, 2013
Last Updated: August 6, 2014
Health Authority: United States: Food and Drug Administration

Keywords provided by Galderma:
erythematous rosacea
facial gel
brimonidine
ophthalmic solution

Additional relevant MeSH terms:
Rosacea
Skin Diseases
Pharmaceutical Solutions
Brimonidine
Ophthalmic Solutions
Therapeutic Uses
Pharmacologic Actions
Antihypertensive Agents
Cardiovascular Agents
Adrenergic alpha-2 Receptor Agonists
Adrenergic alpha-Agonists
Adrenergic Agonists
Adrenergic Agents
Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Physiological Effects of Drugs

ClinicalTrials.gov processed this record on September 30, 2014