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”

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

Study Type: Interventional

Study Design: Treatment, Randomized, Double Blind (Subject, Caregiver, Investigator, Outcomes Assessor), Active Control, Crossover Assignment, Bio-availability Study

Study Primary Completion Date: June 2008

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.

Intervention(s) in this Clinical Trial

• 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
• 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.

Arms, Groups and Cohorts in this Clinical Trial

• 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
• 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

Primary Measures

• To assess the relative bioavailability of 0.18% COL-118 facial gel and 0.2% brimonidine ophthalmic solution under conditions of maximum use in patients with moderate to severe erythematous rosacea.
  • Time Frame: 0 Hour (prior to dose) and at 1, 2, 3, 4 (just prior to the 2nd dose), 5, 6, 7, and 8 hours post-morning dose
    Safety Issue?: No

Secondary Measures

• To evaluate the safety of COL-118 administered topically as a facial gel in male and female subjects with moderate to severe erythematous rosacea
  • Time Frame: at Screening and at specified times during the study, and/or at Study Completion
    Safety Issue?: No

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

Gender Eligibility for this Clinical Trial: Both

Minimum Age for this Clinical Trial: 18 Years

Maximum Age for this Clinical Trial: N/A

Are Healthy Volunteers Accepted for this Clinical Trial?: No

Lead Sponsor: Galderma

Information obtained from ClinicalTrials.gov on July 02, 2009

Link to the current ClinicalTrials.gov record. http://clinicaltrials.gov/show/NCT00697541

Study ID Number: COL-118-ROSE-202

ClinicalTrials.gov Identifier: NCT00697541

Health Authority: United States: Food and Drug Administration