Mirvaso

CLINICAL PHARMACOLOGY

Mechanism of Action

Brimonidine is a relatively selective alpha-2 adrenergic agonist. Topical application of MIRVASO topical gel may reduce erythema through direct vasoconstriction.

Pharmacokinetics

Absorption

The absorption of brimonidine from MIRVASO topical gel was evaluated in a clinical trial in 24 adult subjects with facial erythema associated with rosacea. All enrolled subjects received once daily topical application of MIRVASO topical gel 1 gram to the entire face for 29 days. Pharmacokinetic assessments were performed on Day 1, Day 15, and Day 29. The mean plasma maximum concentration (Cmax) and area under the concentration-time curve (AUC) were highest on Day 15, with Cmax and AUC values (± standard deviation) of 46 ± 62 pg/mL and 417 ± 264 pg.hr/mL respectively. The systemic drug exposure was slightly lower on Day 29 indicating no further drug accumulation.

Metabolism

Brimonidine is extensively metabolized by the liver.

Excretion

Urinary excretion is the major route of elimination of brimonidine and its metabolites.

Clinical Studies

MIRVASO topical gel was evaluated for the treatment of moderate to severe, persistent (nontransient) facial erythema of rosacea in two randomized, double-blind, vehicle-controlled clinical trials, which were identical in design. The trials were conducted in 553 subjects aged 18 years and older who were treated once daily for 4 weeks with either MIRVASO topical gel or vehicle. Overall, 99% of subjects were Caucasian and 76% were female. Baseline disease severity was graded using a 5point Clinical Erythema Assessment (CEA) scale and a 5-point Patient Self Assessment (PSA) scale, on which subjects scored either “moderate” or “severe” on both scales.

The primary efficacy endpoint in both pivotal trials was 2-grade Composite Success, defined as the proportion of subjects with a 2-grade improvement on both CEA and PSA measured at hours 3, 6, 9, and 12 on Day 29. Table 2 presents the efficacy results. In addition to Day 29, efficacy was evaluated on Day 15 and Day 1, and the results are presented in Figures 1 and 2 for Studies 1 and 2, respectively.

Table 2: Summary of 2-grade Composite Success on Day 29

Success Study 1 Study 2
MIRVASO Topical Gel
(N=129)
Vehicle Gel
(N=131)
MIRVASO Topical Gel
(N=148)
Vehicle Gel
(N=145)
Hour 3 31% 11% 25% 9%
Hour 6 30% 10% 25% 9%
Hour 9 26% 10% 18% 11%
Hour 12 23% 9% 22% 10%
2-grade Composite Success: 2-grade improvement on CEA and 2-grade improvement on PSA.

Figure 1: 2-grade Composite Success by Hour and Day for Study 1

2-grade Composite Success by Hour and Day for Study 1 - Illustration

Figure 2: 2-grade Composite Success by Hour and Day for Study 2

2-grade Composite Success by Hour and Day for Study 2 - Illustration

Last reviewed on RxList: 9/6/2013
This monograph has been modified to include the generic and brand name in many instances.

A A A

Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


Women's Health

Find out what women really need.

Health Resources
advertisement
advertisement
Use Pill Finder Find it Now See Interactions

Pill Identifier on RxList

  • quick, easy,
    pill identification

Find a Local Pharmacy

  • including 24 hour, pharmacies

Interaction Checker

  • Check potential drug interactions
Search the Medical Dictionary for Health Definitions & Medical Abbreviations