نتایج جستجو برای: fulvestrant
تعداد نتایج: 782 فیلتر نتایج به سال:
BACKGROUND While premature suture fusion, or craniosynostosis, is a relatively common condition, the cause is often unknown. Estrogens are associated with growth plate fusion of endochondral bones. In the following study, we explore the previously unknown significance of estrogen/estrogen receptor signaling in cranial suture biology. METHODOLOGY/PRINCIPAL FINDINGS Firstly, estrogen receptor (...
Approximately 60% of ovarian cancers are positive for the estrogen receptor (ER); however, ER-targeted treatment is disappointing due to drug resistance as compared with breast cancer. In estrogen-sensitive cancers, estrogen activates Src to phosphorylate p27 promoting its degradation and increasing cell cycle progression. Since Src is frequently activated in ovarian cancers, we investigated wh...
Abstract Purpose: Resistance to treatment with endocrine therapy in patients HR+, HER2? advanced breast cancer (ABC) is common and dual inhibition of CDK4/6 PI3K pathways may delay the development resistance. This phase Ib trial evaluates safety tolerability triple double regimens containing inhibitor ribociclib. Patients Methods: In this open-label, multicenter, study, 70 postmenopausal women ...
BACKGROUND Fulvestrant ('Faslodex') is a new type of oestrogen receptor (ER) antagonist that down-regulates the ER and has no known agonist effects. PATIENTS AND METHODS In this open-label, Phase II trial, 30 postmenopausal Japanese women with hormone-sensitive advanced breast cancer, who had progressed on tamoxifen/toremifene following an initial response, received fulvestrant (250 mg; once-...
The underlying mechanisms leading to antiestrogen resistance in estrogen-receptor α (ER)-positive breast cancer is still poorly understood. The aim of this study was therefore to identify biomarkers and novel treatments for antiestrogen resistant breast cancer. We performed a kinase inhibitor screen on antiestrogen responsive T47D breast cancer cells and T47D-derived tamoxifen and fulvestrant r...
BACKGROUND Hormone therapy, oral contraceptives, and tamoxifen increase the risk of thrombotic disease. These compounds also reduce plasma content of tissue factor pathway inhibitor-1 (TFPI), which is the physiological inhibitor of the tissue factor pathway of coagulation. The current aim was to study if estrogens and estrogen receptor (ER) modulators may inhibit TFPI production in cultured end...
Estradiol (E(2)) drives growth hormone (GH) secretion via estrogen receptors (ER) located in the hypothalamus and pituitary gland. ERalpha is expressed in GH releasing hormone (GHRH) neurons and GH-secreting cells (somatotropes). Moreover, estrogen regulates receptors for somatostatin, GHR peptide (GHRP, ghrelin), and GH itself, while potentiating signaling by IGF-I. Given this complex network,...
ZB716 is a selective estrogen receptor downregulator (SERD) with excellent oral bioavailability and superior efficacy. In this study, we investigate the in vitro and in vivo metabolism and the pharmacokinetics of ZB716 by incubation with liver microsomes, liver cytosol, and by orally dosing rodents. Metabolic products were identified and quantified by a combination of liquid chromatography and ...
PURPOSE This trial was conducted to determine the maximum tolerated dose (MTD) and preliminary efficacy of buparlisib, an oral pan-class I PI3K inhibitor, plus fulvestrant in postmenopausal women with metastatic estrogen receptor positive (ER(+)) breast cancer. EXPERIMENTAL DESIGN Phase IA employed a 3+3 design to determine the MTD of buparlisib daily plus fulvestrant. Subsequent cohorts (pha...
BACKGROUND Metastatic uterine cancer is notoriously difficult to treat, presenting a poor prognosis and a median survival time of less than 1 year. We present the successful use of the antiestrogen fulvestrant in an endocrine therapy-naive patient with advanced uterine cancer. CASE REPORT A 64-year-old female presented with advanced uterine cancer 7.0 x 6.0 x 5.5 cm in size, with infiltration...
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