The combination of 2% 4-hydroxyanisole (Mequinol) and 0.01% tretinoin is effective in improving the appearance of solar lentigines and related hyperpigmented lesions in two double-blind multicenter clinical studies.

Abstract

BACKGROUND:

Solar lentigines are a chronic condition of the aging population resulting from years of cumulative sun exposure. A topical treatment that is both safe and effective would be welcome and useful. Combinations of therapeutic agents are often used and allow synergy of mechanisms with tolerability. A tyrosinase inhibitor in use in Europe, 4-hydroxyanisole (Mequinol), and the retinoid tretinoin have been used singly as depigmenting agents.

OBJECTIVE:

The efficacy and safety of the combination product of 2% 4-hydroxyanisole (4HA [mequinol]) /0.01% tretinoin solution (tradename Solagé) were evaluated in two phase III, randomized, controlled, double-blind trials.

METHODS:

Subjects were randomized to treatment with 4HA/tretinoin solution, one of the active components (4HA or tretinoin), or vehicle. Subjects applied the test solution with a wand applicator twice daily to all solar lentigines and related hyperpigmented lesions on the face, forearms, and backs of hands for up to 24 weeks. Trial 1 had a 24-week no-treatment regression phase and trial 2 had a 4-week no-treatment regression phase. Information collected included clinical assessments of Target Lesion Pigmentation, Physician's Global Assessment of Improvement/Worsening, an Assessment of Overall Cosmetic Effect, and a Subject's Self-Assessment Questionnaire.

RESULTS:

The 4HA/tretinoin combination was clinically superior to each of its active components and to the vehicle in the treatment of solar lentigines. At the end of treatment, in trial 1 and trial 2, 4HA/tretinoin was statistically superior to each of its active components and vehicle on the forearms and face (P </=.03), except versus tretinoin on the face in trial 2 (P =.2). In trial 2, a trend toward greater efficacy of 4HA/tretinoin over tretinoin on the face was demonstrated at the end of treatment (P =.2), which was also increasingly evident at the end of the 4-week follow-up (P =.06). Most skin-related adverse events were mild and were similar for both the 4HA/tretinoin and tretinoin treatment groups.

CONCLUSION:

For the treatment of solar lentigines and related hyperpigmented lesions, the topical combination product containing 2% 4HA/0.01% tretinoin solution is well tolerated and superior to either active component.

• Authors: A B Fleischer Jr, E H Schwartzel, S I Colby, D J Altman
• Journal: Journal of the American Academy of Dermatology (J Am Acad Dermatol) Vol. 42 Issue 3 Pg. 459-67 (Mar 2000) ISSN: 0190-9622 [Print] United States
• PMID: 10688717 (Publication Type: Clinical Trial, Clinical Trial, Phase III, Journal Article, Multicenter Study, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)

Chemical References

• Anisoles
• Antioxidants
• Keratolytic Agents
• Tretinoin
• mequinol

Topics

• Administration, Cutaneous
• Adult
• Aged
• Aged, 80 and over
• Anisoles (administration & dosage, adverse effects)
• Antioxidants (administration & dosage, adverse effects)
• Arm
• Double-Blind Method
• Drug Therapy, Combination
• Facial Dermatoses (drug therapy)
• Female
• Hand Dermatoses (drug therapy)
• Humans
• Hyperpigmentation (drug therapy)
• Keratolytic Agents (administration & dosage, adverse effects)
• Lentigo (drug therapy)
• Male
• Middle Aged
• Severity of Illness Index
• Treatment Outcome
• Tretinoin (administration & dosage, adverse effects)