Compositions and methods for topical tamoxifen citrate therapy

摘要

The present invention provides topical compositions and methods for administering tamoxifen citrate while minimizing the incidence and or severity of adverse drug experiences associated with tamoxifen therapy. In one aspect, these compositions and methods provide a lower plasma concentration of tamoxifen metabolites, such as 4-hydroxytamoxifen and N-desmethyltamoxifen, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient tamoxifen as the sole active agent to benefit a subject with tamoxifen therapy.

主权项

1. A method for reducing plasma concentration of tamoxifen metabolites associated with tamoxifen therapy, the method comprising:
topically administering a pharmaceutical composition to a subject comprising tamoxifen citrate to a subject to provide a plasma area under the curve (AUC) ratio of a tamoxifen metabolite to tamoxifen of from about 0 to about 0.04 on day 1 and about 0.07 to about 0.14 on day 28.