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Aromatase inhibitors

Ronald A Lubet, Vernon E Steele, M M Juliana, Ann Bode, Fariba Moeinpour, Clinton J Grubbs
Daily vs. weekly dosing with EGFR inhibitors (gefitinib and lapatinib) and an AKT inhibitor (MK2206) were compared in two rodent breast cancer models. Female Sprague-Dawley rats were administered methylnitrosourea (MNU) at 50 days of age, and gefitinib (daily/weekly dosing at 10/70 mg/kg BW) or lapatinib (daily/weekly dosing at 75/525 mg/kg BW) were administered by gavage beginning 5 days after MNU. For the prevention studies, weekly or daily dosing with gefitinib or lapatinib reduced cancer multiplicity >75%, and all treatments reduced tumor weights by >90%...
March 14, 2018: Oncology Reports
E Martínez de Dueñas, J Gavila-Gregori, S Olmos-Antón, A Santaballa-Bertrán, A Lluch-Hernández, E J Espinal-Domínguez, M Rivero-Silva, A Llombart-Cussac
Cyclin-dependent kinases (CDKs) play a key role in cell cycle regulation, which makes them a clear therapeutic target to interfere with cell division and proliferation in cancer patients. Palbociclib, a specific inhibitor of CDK4/6 with outstanding clinical efficacy data and limited toxicity, has been recently approved for the treatment of hormone receptor (HR)-positive human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer, either in combination with an aromatase inhibitor or in combination with fulvestrant in women who have received prior endocrine therapy...
March 21, 2018: Clinical & Translational Oncology
Berna Ozdemir, Georgios Sflomos, Cathrin Brisken
Estrogen receptor positive (ER+) tumors account for 70 to 80 % of all breast cancer (BC) cases and are characterized by estrogen dependency for their growth. Endocrine therapies using estrogen receptor antagonists or aromatase inhibitors represent a key component of the standard of care for these tumors. The occurrence of de novo or acquired resistance to estrogen withdrawal represents an important clinical problem, impacting on patient survival. In addition, despite an initially favourable outcome, a part of ER+ BC patients present with disease recurrence locally or at distant sites years or even decades after apparent remission...
March 21, 2018: Endocrine-related Cancer
George S Tria, Tinya Abrams, Jason Baird, Heather E Burks, Brant Firestone, L Alex Gaither, Lawrence G Hamann, Guo He, Christina A Kirby, Sunkyu Kim, Franco Lombardo, Kaitlin J Macchi, Donald P McDonnell, Yuji Mishina, John D Norris, Jill Nunez, Clayton Springer, Yingchuan Sun, Noel M Thomsen, Chunrong Wang, Jianling Wang, Bing Yu, Choi-Lai Tiong-Yip, Stefan Peukert
In breast cancer, estrogen receptor alpha (ERα) positive cancer accounts for approximately 74% of all diagnoses, and in these settings, it is a primary driver of cell proliferation. Treatment of ERα positive breast cancer has long relied on endocrine therapies such as selective estrogen receptor modulators, aromatase inhibitors, and selective estrogen receptor degraders (SERDs). The steroid-based anti-estrogen fulvestrant (5), the only approved SERD, is effective in patients who have not previously been treated with endocrine therapy as well as in patients who have progressed after receiving other endocrine therapies...
March 22, 2018: Journal of Medicinal Chemistry
Bayan Alemrayat, Abdelbary Elhissi, Husam M Younes
Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to control the release, potentially maximize the therapeutic efficiency and minimize the side effects of the drug. LTZ was incorporated into Poly (D, L-Lactide) (PDLLA) NPs by employing the emulsion-solvent evaporation technique using a range of drug concentrations...
March 21, 2018: Pharmaceutical Development and Technology
Kelly J Chan, Divya Jolly, Jennifer J Liang, Jamie D Weinand, Joshua D Safer
OBJECTIVE: Existing transgender treatment guidelines suggest that for transmasculine treatment, there is a possible need for estrogen-lowering strategies adjunct to testosterone therapy. Further, guidelines advocate consideration of prophylactic female reproductive tissue surgeries for transgender men to avoid the possibility of estrogen-related health risks. Despite the paucity of objective data, some transgender men seek conversion inhibitors. We sought to determine estradiol levels in transgender men treated with testosterone therapy and the change in those levels with treatment, if any...
March 21, 2018: Endocrine Practice
Rajiv Gandhi Govindaraj, Misagh Naderi, Manali Singha, Jeffrey Lemoine, Michal Brylinski
Rare, or orphan, diseases are conditions afflicting a small subset of people in a population. Although these disorders collectively pose significant health care problems, drug companies require government incentives to develop drugs for rare diseases due to extremely limited individual markets. Computer-aided drug repositioning, i.e., finding new indications for existing drugs, is a cheaper and faster alternative to traditional drug discovery offering a promising venue for orphan drug research. Structure-based matching of drug-binding pockets is among the most promising computational techniques to inform drug repositioning...
2018: NPJ Systems Biology and Applications
Dillon F Da Fonte, Chris J Martyniuk, Lei Xing, Vance L Trudeau
Radial glial cells (RGCs) are the main macroglia in the teleost brain and have established roles in neurogenesis and neurosteroidogenesis. They are the only brain cell type expressing aromatase B ( cyp19a1b ), the enzyme that synthesizes estrogens from androgen precursors. There are few studies on the regulation of RGC functions, but our previous investigations demonstrated that dopamine stimulates cyp19a1b expression in goldfish RGCs, while secretoneurin A (SNa) inhibits the expression of this enzyme. Here, we determine the range of proteins and cellular processes responsive to SNa treatments in these steroidogenic cells...
2018: Frontiers in Endocrinology
Yukio Nakamura, Mikio Kamimura, Akio Morikawa, Akira Taguchi, Takako Suzuki, Hiroyuki Kato
Background: The aim of this study was to evaluate the effects of denosumab in patients with osteoporosis (OP) and non-metastatic breast cancer following treatment of 1) surgery, 2) surgery and aromatase inhibitors, and 3) surgery, aromatase inhibitors, and anti-cancer agents, compared with those in primary OP patients. Patients and methods: In this retrospective 24-month study, patients were divided into the primary OP group (34 cases) or OP receiving breast cancer treatment group (breast cancer group; 17 cases)...
2018: Therapeutics and Clinical Risk Management
Sara Clemenza, Flavia Sorbi, Ivo Noci, Tommaso Capezzuoli, Irene Turrini, Carlo Carriero, Nicolò Buffi, Massimiliano Fambrini, Felice Petraglia
Endometriosis is a chronic disease, and a lifelong management plan should be developed by using pharmacological treatment and surgical procedures. The pathogenesis of endometriosis is complicated and has not been definitively established. The mechanisms involved are numerous, and their understanding is constantly evolving. Currently, the first-line drugs act by blocking ovarian function, creating an hypoestrogenic environment. The blockade of estrogen secretion and receptor activity and the activation of progesteron receptors are the main target of several current drugs, as well as those under development...
February 15, 2018: Best Practice & Research. Clinical Obstetrics & Gynaecology
Kathrin Strasser-Weippl, Michaela J Higgins, Judith-Anne W Chapman, James N Ingle, George W Sledge, George T Budd, Matthew J Ellis, Kathleen I Pritchard, Mark J Clemons, Tanja Badovinac-Crnjevic, Lei Han, Karen A Gelmon, Manuela Rabaglio, Catherine Elliott, Lois E Shepherd, Paul E Goss
Background: Celecoxib and low-dose aspirin might decrease risk of breast cancer recurrence. Methods: In the Canadian Cancer Trials Group MA.27, postmenopausal hormone receptor-positive breast cancer patients were randomly assigned (2 × 2) to adjuvant exemestane or anastrozole, and celecoxib or placebo. Low-dose aspirin of 81 mg or less was a stratification factor. Due to concerns about cardiac toxicity, celecoxib use was stopped in December 2004, while stratification by aspirin use was removed through protocol amendment...
March 15, 2018: Journal of the National Cancer Institute
Michaël R Laurent
An overview of selected papers related to bone published in 2017 is provided. PURPOSE: This paper accompanies a lecture at the 2018 Belgian Bone Club annual Clinical Update Symposium held in Brussels on January 20th, discussing the best papers (in the opinion of the author) published in the previous year. METHODS: A PubMed search using the keyword "bone" and articles published in 2017. RESULTS: Hot topics include screening for osteoporosis, novel anabolic drugs such as romosozumab and abaloparatide for osteoporosis and rare metabolic bone diseases, as well as long-term efficacy of denosumab and possible risk of multiple vertebral fractures following its discontinuation...
March 15, 2018: Archives of Osteoporosis
Sribalasubashini Muralimanoharan, Youn-Tae Kwak, Carole R Mendelson
Dysregulation of human trophoblast invasion and differentiation with placental hypoxia can result in preeclampsia, a hypertensive disorder of pregnancy. Herein, we characterized the role and regulation of miR-1246, which is markedly induced during human syncytiotrophoblast differentiation. miR-1246 is known to target GSK3β and AXIN2, inhibitors of WNT/β-catenin signaling, which is crucial for placental development, and is predicted to target JARID2, which promotes silencing of developmentally regulated genes...
March 13, 2018: Endocrinology
Irene E G van Hellemond, Ingeborg J H Vriens, Petronella G M Peer, Astrid C P Swinkels, Carolien H Smorenburg, Caroline M Seynaeve, Maurice J C van der Sangen, Judith R Kroep, Hiltje de Graaf, Aafke H Honkoop, Frans L G Erdkamp, Franchette W P J van den Berkmortel, Jos J E M Kitzen, Maaike de Boer, Wïlfred K de Roos, Sabine C Linn, Alexander L T Imholz, Vivianne C G Tjan-Heijnen
Background: Aromatase inhibitors (AIs) are given as adjuvant therapy for hormone receptor-positive breast cancer in postmenopausal women, also to those with chemotherapy-induced ovarian function failure. The current analysis reports on endocrine data of patients with chemotherapy-induced ovarian function failure who were included in the phase III DATA study assessing different durations of adjuvant anastrozole after tamoxifen. Methods: We identified all patients with chemotherapy-induced ovarian function failure...
December 1, 2017: Journal of the National Cancer Institute
M Cunha-Silva, V N Brito, D B Macedo, D S Bessa, C O Ramos, L G Lima, P S Barroso, I J P Arnhold, D L Segaloff, B B Mendonca, A C Latronico
Testotoxicosis is a rare cause of peripheral precocious puberty in boys caused by constitutively activating mutations of the LHCG receptor. Affected males usually have normal gonadotropin profiles and fertility in their adult life. Here, we described the long-term follow-up of a 24-year-old young man with severe testotoxicosis due to a de novo activating mutation in the third transmembrane helix of the LHCGR (p.Leu457Arg). This patient was treated with different medications, including medroxyprogesterone acetate, ketoconazole, cyproterone acetate and aromatase inhibitor from age 2...
March 12, 2018: Human Reproduction
Yakup Bozkaya, Gökmen Umut Erdem, Nebi Serkan Demirci
Arthralgia, myalgia, paresthesia, reduced bone mineral density, vasomotor side effects including hot flashes and night sweats, genitourinary symptoms including decreased libido, vaginal dryness and dyspareunia are common side effects of aromatase inhibitors. Unlike the common side effects, the information on neurological side effects like hallucination of aromatase inhibitor was limited in literature cases. Herein, we reported a case of hallucination related to anastrozole in a patient with metastatic breast cancer...
January 1, 2018: Journal of Oncology Pharmacy Practice
Tiago Augusto, Georgina Correia-da-Silva, Cecília M P Rodrigues, Natércia Teixeira, Cristina Amaral
Aromatase inhibitors (AIs) are one of the principal therapeutic approaches for estrogen-receptor positive (ER+) breast cancer in postmenopausal women. They block estrogen biosynthesis through aromatase inhibition, thus preventing tumour progression. Besides the therapeutic success of the third-generation AIs, acquired-resistance may develop, leading to tumour relapse. This resistance is thought to be the result of a change in the behavior of ER in these breast cancer cells, presumably by PI3K/Akt pathway enhancement along with alterations in other signalling pathways...
March 12, 2018: Endocrine-related Cancer
G Legendre, L Delbos, E Hudon, N Chabbert-Buffet, S Geoffron, M Sauvan, H Fernandez, P-E Bouet, P Descamps
OBJECTIVE: The objective of this work is to evaluate the place of new treatments in the management of endometriosis outside the context of infertility. METHODS: A review of the literature was conducted by consulting Medline data until July 2017. RESULTS: Dienogest is effective compared to placebo in short term (NP2) and long term (NP4) for the treatment of painful endometriosis. In comparison with GnRH agonists, dienogest is also effective in terms of decreased pain and improved quality of life in non-operated patients (NP2) as well as for recurrence of lesions and symptomatology postoperatively (NP2)...
March 9, 2018: Gynecologie, Obstetrique, Fertilite & Senologie
Elena Ongaro, Lorenzo Gerratana, Marika Cinausero, Giacomo Pelizzari, Elena Poletto, Manuela Giangreco, Claudia Andreetta, Stefano Pizzolitto, Carla Di Loreto, Alessandro Marco Minisini, Mauro Mansutti, Stefania Russo, Gianpiero Fasola, Fabio Puglisi
AIM: Discordance between primary tumor and paired metastases biology has been widely detected in metastatic breast cancer. The aim of this study was to evaluate the prognostic impact of Ki67, estrogen receptor (ER), progesterone receptor (PR) and HER2 discordance. METHODS: We retrospectively analyzed a cohort of 544 patients affected by metastatic breast cancer. Variation in ER, PR, Ki67 and HER2 expression between primary site and recurrence was tested through the McNemar test...
March 12, 2018: Future Oncology
Elie El Rassy, Ziad Bakouny, Tarek Assi, Joseph Kattan
AIM: To determine which of the CDK4/6 inhibitors is the optimal treatment in metastatic luminal breast cancer. MATERIALS & METHODS: A network meta-analysis using the frequentist approach and generalized pairwise modeling was computed. RESULTS: The associations of aromatase inhibitor with ribociclib, palbociclib and abemaciclib were similar in efficacy. Palbociclib-based regimen was associated with significantly lower treatment discontinuation rates compared with the other approved drugs in this indication...
March 12, 2018: Future Oncology
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