Short-term effects of estrogen, tamoxifen and raloxifene on hemostasis: a randomized-controlled study and review of the literature

Arzoxifene versus raloxifene: effect on bone and safety parameters in postmenopausal women with osteoporosis

“…Arzoxifene decreased protein C to a significantly greater extent than raloxifene, and antithrombin III decreased significantly in the arzoxifene group but increased significantly in the raloxifene group. The increase in antithrombin III in the raloxifene group seen in this study was unexpected and not consistent with findings from previous studies which have consistently shown raloxifene to reduce antithrombin III levels [18][19][20][21]. Neither arzoxifene nor raloxifene affected protein S levels.…”

“…Reductions in anticoagulant proteins have been hypothesized to play a role in the increased risk of VTE associated with use of SERMs and estrogen therapies [17,18], and in this study, we measured protein C, protein S, and antithrombin III levels. Some differences were observed in the effects of arzoxifene and raloxifene on anticoagulant proteins.…”

Curiouser and curiouser: Recent advances in measurement of thrombin-activatable fibrinolysis inhibitor (TAFI) and in understanding its molecular genetics, gene regulation, and biological roles

“…Several studies have shown that plasma TAFI concentrations rise with age in women, but not in men [42,45,50]; consistent with this, plasma TAFI concentrations have been shown to be decreased by HMR 3339 (a selective estrogen receptor modulator) [51], raloxifene [52], estradiol plus trimegestone [53], transdermal estradiol [54], and oral estradiol plus gestodene [54]. On the other hand, some studies have reported an increase in, or no effect on, plasma TAFI concentrations with oral contraceptive use or no effect of raloxifene or tamoxifen use [52][53][54][55][56][57][58]. Clearly, additional studies in which the type of hormone treatment and method of TAFI measurement are carefully accounted for are required to address this issue.…”

In vitro human skin permeation of endoxifen: potential for local transdermal therapy for primary prevention and carcinoma in situ of the breast

“…2,21,22 Since risk of thromboembolism is a major concern not only with TAM use, but also with all selective estrogen-receptor modulators (SERMs) tested clinically to date, its avoidance would be a significant advantage for women considering SERM therapy for breast cancer prevention and for treatment of DCIS. Additionally, the very low plasma concentrations of following transdermal application of 4-OHT observed in the studies conducted so far 7,8,11 suggest that uterine toxicity and hot flashes would be reduced by the transdermal delivery of active TAM metabolites to the breast.…”