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Mi Hwa Heo, Hee Kyung Kim, Hansang Lee, Ji-Yeon Kim, Jin-Seok Ahn, Young-Hyuck Im, Yeon Hee Park
Background/Aims: We conducted a retrospective analysis of the clinical activity of fulvestrant in postmenopausal women with hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer (MBC) previously treated with endocrine therapy and/or chemotherapy. Methods: We reviewed the medical records of all patients with MBC treated at Samsung Medical Center between January 2009 and August 2016. Patients received fulvestrant 250 mg intramuscularly every 28 days (from January 2009 to November 2010) or 500 mg intramuscularly every 28 days (from December 2010 to August 2016)...
March 16, 2018: Korean Journal of Internal Medicine
Jun Won Park, Su Hyung Lee, Gye-Hyung Woo, Hyo-Jung Kwon, Dae-Yong Kim
TXNIP is a potent tumor suppressor with reduced expression in various types of human cancer. The prognostic and predictive power of TXNIP has been recognized in human breast cancer. The aim of this study is to investigate the clinical relevance and functional roles of TXNIP downregulation in breast cancer. We examined TXNIP expression at the protein level in tissue microarray (TMA)-based human breast cancers and its correlation with clinical parameters and molecular markers on immunohistochemistry (IHC). Compared with normal tissues, TXNIP expression was significantly decreased in human breast cancer tissues and animal mammary tumors, along with tumor progression...
March 7, 2018: Biochemical and Biophysical Research Communications
Lunming Liu, Weifeng Shen, Zhihui Zhu, Jinxiong Lin, Qingxia Fang, Yeping Ruan, Huajun Zhao
Fulvestrant is the FDA-approved "pure anti-estrogen" agent for malignant breast cancer therapy. But endocrine resistance causes drug failure. A new approach is desired for fulvestrant-resistant breast cancer (FRBC) therapy. This study aims to find an effective approach to inhibit FRBC for patients with advanced breast cancer. MTT assay was first performed to detect the effect of inhibitors of c-ABL (imatinib) and EGFR (lapatinib) on FRBC cells. Microarray analysis was carried out to identify microRNA which is significantly changed between parental and FRBC cells...
March 6, 2018: Biochemical and Biophysical Research Communications
Kenji Tamura, Makoto Kodaira, Chikako Shimizu, Kan Yonemori, Mayu Yunokawa, Akihiko Shimomura, Takayuki Kobayashi, Kenji Nakano, Junichi Tomomatsu, Yoshinori Ito, Jun Tanaka, Hiroshi Kuriki, Zhaodi Gu, Shunji Takahashi
Taselisib is a potent and selective phosphatidylinositide 3-kinase (PI3K) inhibitor. This paper reports the first study of taselisib administration in Japanese patients. The aim of this two-stage, phase I, multicenter, open-label, dose-escalation study was to evaluate the safety, pharmacokinetics, and preliminary efficacy of taselisib as monotherapy in Japanese patients with advanced solid tumors (Stage 1), and as part of combination therapy in Japanese patients with hormone receptor (HR)-positive locally advanced or recurrent breast cancer (Stage 2)...
March 3, 2018: Cancer Science
Gong Deuk Bae, Eun-Young Park, Dong Jae Baek, Hee-Sook Jun, Oh Yoon Sin
Liquiritigenin (LQ) is a major active component of licorice root, which is a flavone used for treating many diseases, including diabetes. LQ has been shown to exhibit a glucose-lowering effect in diabetic mice. Therefore, we investigated the potential of LQ to protect against lipotoxicity-induced beta-cell apoptosis and the underlying molecular mechanisms. Exposure of INS-1 rat insulinoma cells to LQ significantly increased cell viability and blocked palmitate (PA)-induced apoptosis, as evidenced by the reduction of Annexin-V-stained cells, cleaved caspase-3 levels, and poly (ADP-ribose) polymerase (PARP) activity, as well as upregulation of Bcl-2 expression...
February 27, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Ben O'Leary, Sarah Hrebien, James P Morden, Matthew Beaney, Charlotte Fribbens, Xin Huang, Yuan Liu, Cynthia Huang Bartlett, Maria Koehler, Massimo Cristofanilli, Isaac Garcia-Murillas, Judith M Bliss, Nicholas C Turner
CDK4/6 inhibition substantially improves progression-free survival (PFS) for women with advanced estrogen receptor-positive breast cancer, although there are no predictive biomarkers. Early changes in circulating tumor DNA (ctDNA) level may provide early response prediction, but the impact of tumor heterogeneity is unknown. Here we use plasma samples from patients in the randomized phase III PALOMA-3 study of CDK4/6 inhibitor palbociclib and fulvestrant for women with advanced breast cancer and show that relative change in PIK3CA ctDNA level after 15 days treatment strongly predicts PFS on palbociclib and fulvestrant (hazard ratio 3...
March 1, 2018: Nature Communications
Yumiko Koi, Chinami Koga, Sayuri Akiyoshi, Takanobu Masuda, Hideki Ijichi, Yoshiaki Nakamura, Mayumi Ishida, Shinji Ohno, Eriko Tokunaga
BACKGROUND: Previous studies have suggested that the presence of visceral metastasis is a parameter useful in predicting the treatment efficacy of fulvestrant in patients with advanced breast cancer. PATIENTS AND METHODS: We retrospectively examined the association between treatment efficacy and presence of visceral metastasis in 75 patients with hormone receptor-positive recurrent breast cancer who were treated with fulvestrant or no more than five lines of other endocrine monotherapy after recurrence...
March 2018: Anticancer Research
Shuai Liu, Bingxin Gu, Jianping Zhang, Yongping Zhang, Xiaoping Xu, Huiyu Yuan, Yingjian Zhang, Zhongyi Yang
OBJECTIVE: Our study aimed to investigate the feasibility of PET/CT for monitoring the influence of fulvestrant on sensitizing docetaxel by downregulating ERα in ERα+ breast cancer. METHODS: Docetaxel-insensitive ERα+ breast cancer cells (DIS-ZR751) were established, identified and cultured. ERα expression, toxicity and viability of DIS-ZR751 were analyzed before and after treatment in vitro. DIS-ZR751-bearing nude mice were randomly divided into four groups according to different treatments: blank (DIS-ZR751), docetaxel (DIS-ZR751+DOC), fulvestrant (DIS-ZR751+FUL), and combination treatment (DIS-ZR751+DOC+FUL)...
February 24, 2018: Annals of Nuclear Medicine
Shanchun Guo, Changde Zhang, Melyssa Bratton, Madhusoodanan Mottamal, Jiawang Liu, Peng Ma, Shilong Zheng, Qiu Zhong, Lin Yang, Thomas E Wiese, Yong Wu, Matthew J Ellis, Margarite Matossian, Matthew E Burow, Lucio Miele, René Houtman, Guangdi Wang
Advances in oral SERDs development so far have been confined to nonsteroidal molecules such as those containing a cinnamic acid moiety, which are in earlystage clinical evaluation. ZB716 was previously reported as an orally bioavailable SERD structurally analogous to fulvestrant. In this study, we examined the binding details of ZB716 to the estrogen receptor alpha (ERα) by computer modeling to reveal its interactions with the ligand binding domain as a steroidal molecule. We also found that ZB716 modulates ERα-coregulator interactions in nearly identical manner to fulvestrant...
January 23, 2018: Oncotarget
Eid Alabed Alibrahim, Ramaroson Andriansitohaina, Kévin Hardonnière, Raffaella Soleti, Sébastien Faure, Gilles Simard
AIM: Chlordecone is able to induce pro-angiogenic effect through an estrogen receptor (ERα) pathway involving NO release and VEGF. The present study aimed to determine the molecular mechanisms by which chlordecone promotes angiogenesis in human endothelial cells. RESULTS: High but not low concentration of chlordecone increased mitochondrial respiratory capacity and mitochondrial DNA content in endothelial cells. The ROS scavenger MnTMPyP was able to prevent the increase of both VEGF expression and capillary length induced by chlordecone...
February 13, 2018: International Journal of Biochemistry & Cell Biology
Zilei Liu, Jie Li, Suhua Li, Gencheng Li, K Barry Sharpless, Peng Wu
Sulfur(VI) Fluoride Exchange (SuFEx) is a new family of click chemistry transformations which relies on readily available materials to produce compounds bearing the S VI -F motif. The potential of SuFEx in drug discovery has just started to be explored. We report the first method of SuFEx chemistry for the conversion of phenolic compounds to their respective arylfluorosulfate derivatives in situ in 96-well plates. This method is compatible with automated synthesis and screening to quickly assess the biological activities of the in situ generated, crude products...
February 16, 2018: Journal of the American Chemical Society
Shinzaburo Noguchi, Matthew J Ellis, John F R Robertson, Jackie Thirlwell, Mehdi Fazal, Zhimin Shao
BACKGROUND: The international, phase III FALCON study (NCT01602380) in postmenopausal patients with hormone receptor-positive, locally advanced/metastatic breast cancer (LA/MBC) who had not received prior endocrine therapy, demonstrated statistically significant improvement in progression-free survival (PFS) for patients who received fulvestrant 500 mg vs anastrozole 1 mg. This subgroup analysis evaluated PFS in Asian (randomized in China, Japan, or Taiwan) and non-Asian patients from the FALCON study...
February 15, 2018: Breast Cancer: the Journal of the Japanese Breast Cancer Society
Ugne Sabale, Mattias Ekman, Daniel Thunström, Claire Telford, Christopher Livings
OBJECTIVES: In Sweden, breast cancer (BC) represents 30% of newly diagnosed cancers and is the most common cancer in women. For hormone-dependent BC, endocrine therapies varying in efficacy and price are available. The aim of this study is to assess the cost effectiveness of fulvestrant 500 mg as a second-line hormonal therapy for postmenopausal women with estrogen receptor-positive metastatic or locally advanced BC versus letrozole, anastrozole, and exemestane in Sweden. METHODS: A three-state (pre-progression, post-progression, and death) partitioned-survival model was used to estimate progression-free (PFS) and overall survival (OS) by extrapolating trial results beyond the trial period to capture costs and benefits over a lifetime perspective...
December 2017: PharmacoEconomics Open
Pedro Alvarez, Paul G Green, Jon D Levine
Neonatal handling (NH) of male rat pups strongly attenuates stress response and stress-induced persistent muscle hyperalgesia in adults. Since female sex is a well-established risk factor for stress-induced chronic muscle pain, we explored whether NH provides resilience to stress-induced hyperalgesia in adult female rats. Rat pups underwent NH, or standard (control) care. Muscle mechanical nociceptive threshold was assessed before and after water avoidance (WA) stress, when they were adults. In contrast to males, NH produced only a modest protection against WA stress-induced muscle hyperalgesia in females...
February 9, 2018: Journal of Pain: Official Journal of the American Pain Society
Xiaoqing Jia, Jingyi Cheng, Zhenzhou Shen, Zhimin Shao, Guangyu Liu
Previous studies have reported that hypoxia-inducible factor (HIF)-1α confers endocrine resistance and that zoledronic acid (ZOL) decreases HIF‑1α expression in estrogen receptor‑positive breast cancer. The present study investigated the effect of the combination treatment with ZOL and fulvestrant and its possible mechanism for HIF‑1α inhibition in vitro and in vivo. First, cell proliferation, clonogenic ability and HIF‑1α expression by western blotting were determined in MCF‑7 breast cancer cells stably expressing HIF‑1α in vitro...
January 29, 2018: Molecular Medicine Reports
Mohammed A El-Lakany, Mohamed A Fouda, Hanan M El-Gowelli, Sahar M El-Gowilly, Mahmoud M El-Mas
The male gender is more vulnerable to immunological complications of sepsis. Here, we tested the hypotheses that female rats are protected against endotoxemia-evoked hypotension and cardiac autonomic dysfunction, and that gonadal hormone receptors account for such protection. Changes in blood pressure, heart rate, and cardiac sympathovagal balance caused by i.v. lipopolysaccharide (LPS) were determined. In male rats, LPS elevated serum TNFα together with falls in blood pressure and rises in heart rate. The spectral index of cardiac sympathovagal balance (low-frequency/high-frequency ratio, LF/HF) was reduced by LPS, suggesting an enhanced parasympathetic dominance...
January 27, 2018: European Journal of Pharmacology
Tomasz Sarosiek
Cyclin-dependent kinases (CDKs) are a family of enzyme proteins present in cell nuclei that regulate the various stages of the cell cycle. They act as proto-oncogens, and increased expression of some of these proteins (CDK4 and CDK6) is observed in breast cancer cells and associated with decreased sensitivity to anti-estrogen therapy. CDK inhibitors are chemicals that inhibit the enzymatic activity of specific CDKs. Currently three drugs in this group are available on the market and are registered for the treatment of advanced HR-positive, HER2-negative breast cancer...
January 23, 2018: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
Kenichi Sakurai, Shigeru Fujisaki, Hitomi Kubota, Yukiko Hara, Shuhei Suzuki, Keita Adachi, Ryouichi Tomita, Katsuhisa Enomoto, Tomohiro Hirano
We report an elderly patient with locally advanced breast cancer who received long-term fulvestrant therapy.The patient was a 75-year-old woman who presented with a right breast lump.She noticed the tumor 4 years and 6 months ago, but she had not visited any hospital.However, her daughter brought her to our hospital.The tumor was 73mm in diameter.A core needle biopsy for breast tumor led to a diagnosis of an invasive ductal carcinoma, positive for estrogen receptor(ER)and progesterone receptor(PgR), and negative for HER2/neu...
January 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
Yinghui Zhang, Lynn Wester, Jichao He, Tamar Geiger, Marja Moerkens, Ram Siddappa, Jean A Helmijr, Mieke M Timmermans, Maxime P Look, Caroline H M van Deurzen, John W M Martens, Chantal Pont, Marjo de Graauw, Erik H J Danen, Els M J J Berns, John H N Meerman, Maurice P H M Jansen, Bob van de Water
Antiestrogen resistance in estrogen receptor positive (ER+) breast cancer is associated with increased expression and activity of insulin-like growth factor 1 receptor (IGF1R). Here, a kinome siRNA screen has identified 10 regulators of IGF1R-mediated antiestrogen with clinical significance. These include the tamoxifen resistance suppressors BMPR1B, CDK10, CDK5, EIF2AK1, and MAP2K5, and the tamoxifen resistance inducers CHEK1, PAK2, RPS6KC1, TTK, and TXK. The p21-activated kinase 2, PAK2, is the strongest resistance inducer...
January 22, 2018: Oncogene
Lisa E Flaum, William J Gradishar
A majority of breast cancers are hormone receptor (HR) positive and are responsive to various types of hormone manipulation. Endocrine therapy is the preferred first-line therapy for patients with advanced estrogen receptor (ER) positive, HER2-negative breast cancer who do not have symptomatic visceral disease. Endocrine therapy is often continued in the second- and third-line setting, with chemotherapy deferred until tumor becomes endocrine therapy refractory and/or a visceral crisis in imminent. Therapeutic options vary based on clinical presentation and include single-agent therapies such as tamoxifen, aromatase inhibitors and fulvestrant, and combination therapies options...
2018: Cancer Treatment and Research
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