We report a case of long-term (9 years) response to 4th-line endocrine treatment with fulvestrant given for advanced breast cancer after no or poor response to prior endocrine therapies. Complete remission was achieved with full dose and maintained even after dose reduction due to unanticipated intensity of mucosal toxicity. Complete remission was temporarily lost after fulvestrant was tentativ...

Fulvestrant is a selective estrogen receptor antagonist. Based on the measured growth inhibition of 60 human cancer cell lines (NCI60) in the presence of fulvestrant, as well as the baseline gene expression of the 60 cell lines, a gene expression score that predicts response to fulvestrant was developed. The score is based on 414 genes, 103 of which show increased expression in sensitive cell l...

BACKGROUND At the time of the initial analysis of overall survival (OS) for the Comparison of Faslodex in Recurrent or Metastatic Breast Cancer (CONFIRM) randomized, double-blind, phase III trial, approximately 50% of patients had died. A final analysis of OS was subsequently planned for when 75% of patients had died. METHODS Patients were randomly assigned 1:1 to fulvestrant 500 mg administe...

PURPOSE Estrogen receptor (ER) targeting is key in management of receptor-positive breast cancer. Currently, there are no methods to optimize anti-ER therapy dosing. This study assesses the use of 16α-(18)F-fluoroestradiol ((18)F-FES) PET for fulvestrant dose optimization in a preclinical ER(+) breast cancer model. EXPERIMENTAL DESIGN In vitro, (18)F-FES retention was compared with ERα protei...

Fulvestrant is a representative pure antiestrogen and a Selective Estrogen Receptor Down-regulator (SERD). In contrast to the Selective Estrogen Receptor Modulators (SERMs) such as 4-hydroxytamoxifen that bind to estrogen receptor a (ERa) as antagonists or partial agonists, fulvestrant causes proteasomal degradation of ERa protein, shutting down the estrogen signaling to induce proliferation ar...

Owing to its favourable tolerability profile versus cytotoxic chemotherapy, endocrine therapy is the treatment of choice for postmenopausal women with hormone receptor-positive advanced breast cancer (ABC). However, tolerability concerns associated with some endocrine treatments and the potential for cross-resistance has helped to drive the need for new, effective and better-tolerated agents. F...

PURPOSE ESR1 mutations are selected by prior aromatase inhibitor (AI) therapy in advanced breast cancer. We assessed the impact of ESR1 mutations on sensitivity to standard therapies in two phase III randomized trials that represent the development of the current standard therapy for estrogen receptor-positive advanced breast cancer. MATERIALS AND METHODS In a prospective-retrospective analys...

To characterize determinants of treatment outcome in a real world population of 161 post-menopausal hormone receptor-positive metastatic breast cancer patients treated with fulvestrant. Descriptive statistics for demographics, anthropometrics, clinical and molecular characteristic were compared across subgroups of sensitivity/resistance to prior endocrine therapy and tested in uni/multivariate ...

BACKGROUND Human epidermal growth factor receptor 2 (HER2) overexpression increases the aggressiveness of breast cancer cells resulting in poorer prognosis. Patients with HER2-positive disease are less responsive to endocrine therapies. Trastuzumab monotherapy results in objective responses in only approximately 15% of patients. Fulvestrant retains activity in cells overexpressing HER2 that are...

This paper describes two rapid, sensitive and specific methods for the determination of fulvestrant in pharmaceutical preparations by high performance liquid chromatography (HPLC) and linear sweep voltammetry (LSV). HPLC method was used to study the degradation behaviour. Fulvestrant was subjected to degradation under the conditions of hydrolysis (acid and alkali), oxidation (30% H2O2). The lin...