A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women
- Robert ManselAffiliated withDepartment of Surgery, Wales College of Medicine, Cardiff University Email author
- , Amit GoyalAffiliated withDepartment of Surgery, Wales College of Medicine, Cardiff University
- , Elisabeth Le NestourAffiliated withBesins International
- , Valérie Masini-EtévéAffiliated withBesins International
- , Katharine O’ConnellAffiliated withColumbia University Medical Center
- , Afimoxifene (4-OHT) Breast Pain Research Group
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Many women experience symptoms of cyclical mastalgia, such as breast pain, tenderness, and nodularity. Tamoxifen and other drugs have been used to alleviate cyclical mastalgia symptoms; however, their use is associated with potentially serious side effects. The current study compared the safety and efficacy of two doses of a topical gel containing 4-hydroxytamoxifen (Afimoxifene, formerly known as 4-OHT) with placebo gel for the treatment of moderate to severe cyclical mastalgia.
Premenopausal women aged at least 18 years experiencing moderate to severe symptoms were randomized to receive placebo, 2 mg, or 4 mg of Afimoxifene daily delivered as a transdermal hydroalcoholic gel for 4 menstrual cycles. The primary efficacy parameter was change in mean pain intensity as measured by the Visual Analog Scale (VAS) for the seven worst pain score days within a cycle from baseline to the fourth cycle.
After 4 cycles of treatment, statistically significant improvements relative to placebo were measured in mean VAS score in the 4-mg Afimoxifene group (−12.71 mm [95% confidence interval, −0.96 to −24.47; P = 0.034]). Patient global assessment of pain, physician’s assessment of pain, tenderness on palpation, and nodularity following 4 cycles of treatment were significantly more likely to show improvements in the 4-mg group, compared with placebo (P = 0.010 [pain]; P = 0.012 [tenderness]; P = 0.017 [nodularity]). Overall, Afimoxifene was well tolerated with few adverse events and no drug-related SAE occurred in any group.
There were no changes in menstrual pattern or plasma hormone levels and no breakthrough vaginal bleeding in patients treated with Afimoxifene.
After 4 months of treatment, daily topical breast application of Afimoxifene resulted in statistically significant improvements in signs and symptoms of cyclical mastalgia across patient- and physician-rated scales with excellent tolerability and safety.
Keywords4-Hydroxytamoxifen Afimoxifene Mastalgia Cyclical mastalgia Breast tenderness Breast pain
- A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women
Breast Cancer Research and Treatment
Volume 106, Issue 3 , pp 389-397
- Cover Date
- Print ISSN
- Online ISSN
- Springer US
- Additional Links
- Cyclical mastalgia
- Breast tenderness
- Breast pain
- Industry Sectors
- Author Affiliations
- 1. Department of Surgery, Wales College of Medicine, Cardiff University, Cardiff, CF14 4XN, UK
- 2. Besins International, Paris, France
- 3. Columbia University Medical Center, New York, USA