New antiestrogens in XXXX : a review.

@entity172 @entity28002 @entity137 @entity23392 @entity440 @entity0 @entity5 @entity1299
A comprehensive review of the literature from 1975 to 1995 was conducted. Reports were identified using the Cancerline and Medline databases. The chemical structure, @entity172 agonist and antagonist activity, and in vitro studies were reviewed and compared with those of tamoxifes. Also, the antitumor activity in cell lines and animal models was highlighted. The mechanisms of action, metabolism, route of administration, dose scheduling, antitumor activity, and side effects of each agent were reviewed and compared with those for @entity440 , where available. Several new antiestrogens are at various stages of development. They are divided into nonsteroidal and steroidal antiestrogens. Among the nonsteroidal antiestrogens are agents like @entity23392 and @entity28002 . Both produce response rates, and both have @entity137 profiles that are comparable to @entity440 . In addition, @entity23392 can chemosensitize @entity172 receptor-negative @entity5 , reverse multidrug resistance, and affect @entity440 -resistant @entity5 . The short half-life of @entity28002 results in minimal serum accumulation, and therefore it may be sequentially used with other systemic therapies to maximize cell kill. @entity1299 , a steroidal antiestrogen, is well tolerated, active in @entity440 -resistant @entity5 , and has a potential role in the preoperative management of advanced @entity0 . Other potential benefits of these and other agents are discussed. Pure antiestrogens have documented antibreast cancer activity that is in some instances more potent than @entity440 . Some have activity in @entity172 receptor-negative or @entity440 -resistant @entity5 . Others may help to reverse chemotherapy resistance. In addition, the potential role of these antiestrogens in radioimaging and their effect on lipid metabolism is also being recognized.
