OBJECTIVE: @entity39707 , an orally active third-generation selective @entity172 -receptor modulator (SERM), opposes the action of @entity172 on the breast and endometrium but exerts an @entity172 -agonist effect on bone and the lipid profile. Since this is an appealing combination for hormonal therapy of @entity172 -related @entity5 , we initiated testing the potential of @entity39707 in @entity1 with @entity1204 . METHODS: Two phase I studies were conducted to evaluate the safety and pharmacokinetics of single and multiple doses of @entity39707 . In addition, two multi-institutional phase II trials have been completed on 100 @entity1 with metastatic or recurrent @entity1204 . RESULTS: No serious adverse events were observed in the single-dose phase I study, the principal side effect being hot flashes in 5/15 healthy volunteers. In the second phase I study, conducted in 32 @entity1 with metastatic @entity0 , one @entity1 had a serious, possibly drug-related adverse reaction ( @entity1151 ). The two multi-institutional trials demonstrated significant activity at 20 mg/day in @entity1 with metastatic or recurrent @entity1204 . Observed clinical response rates were 25 and 31%, with a median response duration of 19.3 and 13.9 months, respectively. Progression of the disease was stabilized in a substantial number of @entity1 . @entity137 was mild, except for two cases of @entity1151 that might have been drug related. CONCLUSIONS: Further investigation is warranted to verify these preliminary response rates and the clinical significance of the stable disease cases, to compare clinical outcomes with those in progestin-treated @entity1 , and to elucidate the mechanisms of SERM action in this disease.

@entity39707 as therapy for XXXX .

@entity172 :: ('MESH:D004967', 'Chemical') :: ['estrogen'] @entity1 :: ('9606', 'Species') :: ['women', 'patients', 'patient'] @entity1204 :: ('MESH:D016889', 'Disease') :: ['endometrial cancer', 'treatment-refractory endometrial cancer'] @entity137 :: ('MESH:D064420', 'Disease') :: ['Toxicity'] @entity0 :: ('MESH:D001943', 'Disease') :: ['breast cancer'] @entity5 :: ('MESH:D009369', 'Disease') :: ['cancers'] @entity1151 :: ('MESH:D011655', 'Disease') :: ['pulmonary embolism'] @entity39707 :: ('MESH:C115121', 'Chemical') :: ['arzoxifene', 'Arzoxifene']
@entity1204 :: (MESH:D016889,Disease) :: ['endometrial cancer']
