Fulvestrant (Faslodex™) is a pure antiestrogen that is effective in treating estrogen receptor-(ER) positive breast cancer tumors that are resistant to selective estrogen receptor modulators such as tamoxifen. Clinical trials investigating the utility of adding fulvestrant to other therapeutics have not been shown to affect cytochrome P450-mediated metabolism. Effects on phase II metabolism and...

PURPOSE Phosphatidylinositol 3-kinase (PI3K) inhibitors are being developed for the treatment of estrogen receptor α (ER)-positive breast cancer in combination with antiestrogens. Understanding the temporal response and pharmacodynamic effects of PI3K inhibition in ER(+) breast cancer will provide a rationale for treatment scheduling to maximize therapeutic index. EXPERIMENTAL DESIGN Antiestr...

I read with great interest the article by Verma et al. [1], in which they reported detailed safety analysis in hormone receptor-positive/HER2-negative advanced metastatic breast cancer receiving palbociclib in combination with fulvestrant (PALOMA-3). They found that treatment with palbociclib in combination with fulvestrant was generally safe and well tolerated in patients with hormone receptor...

Male breast cancer is rare and treatment recommendations are mainly extrapolated from the results of trials on women. Most breast cancers in men are estrogen receptor (ER)/ progesterone receptor (PgR) positive; as a consequence, tamoxifen remains the standard adjuvant treatment and is also the mainstay first-line treatment of advanced disease, with reported response rates varying from 25% to 80...

Osteosarcoma is one of the most malignant bone tumors of childhood and adolescence. Interestingly, the presence of estrogen receptors α and β has been reported in human bone cells, including osteosarcoma. Thus, inhibitors of estrogens such as fulvestrant, are considered candidates for novel endocrine therapy in treatment of osteosarcoma. Another anticancer agent that seems to be very effective ...

PURPOSE Fulvestrant, a potent estrogen receptor (ER) antagonist with a novel mechanism of action, has shown efficacy in pretreated patients with advanced breast cancer. We assessed the efficacy and tolerability of fulvestrant in Korean postmenopausal women. METHODS Of the 25 candidates identified at Asan Medical Center, Seoul, Korea, six were deemed ineligible due to inadequate baseline and f...

Fulvestrant is a selective estrogen receptor degrader that binds, blocks and degrades the estrogen receptor (ER), leading to complete inhibition of estrogen signaling through the ER. This review article further explains the mechanism of action of the drug and goes on to review the trials carried out to optimize its dosing. Multiple trials have been undertaken to compare fulvestrant with other e...

We report the first study of the biological effect of fulvestrant on ER positive clinical breast cancer using sequential biopsies through to progression. Thirty-two locally/systemically advanced breast cancers treated with first-line fulvestrant (250 mg/month) were biopsied at therapy initiation, 6 weeks, 6 months and progression and immunohistochemically-analyzed for Ki67, ER, EGFR and HER2 ex...

The EMERALD clinical trial showed significantly prolonged progression-free survival (PFS) and a manageable toxicity profile for elacestrant vs SOC endocrine therapy in patients (pts) with ER+/HER2- mBC following progression on prior CDK4/6 inhibitor therapy. Benefit was observed the overall population pts ESR1 mutations (mESR1). Here, we report subgroup analysis from comparing efficacy to fulve...

BACKGROUND Second line endocrine therapy has limited antitumour activity. Fulvestrant inhibits and downregulates the oestrogen receptor. The mitogen-activated protein kinase (MAPK) pathway is one of the major cascades involved in resistance to endocrine therapy. We assessed the efficacy and safety of fulvestrant with selumetinib, a MEK 1/2 inhibitor, in advanced stage breast cancer progressing ...