Search results for "Aromatase Inhibitor"

showing 10 items of 30 documents

Early Denosumab for the prevention of osteoporotic fractures in breast cancer women undergoing aromatase inhibitors: A case-control retrospective stu…

2021

BACKGROUND: Aromatase inhibitors (AIs) might have a detrimental impact on bone health in breast cancer (BC) women. Denosumab has been shown to reduce the risk of fractures, but the appropriate time for starting is yet to be clearly defined. OBJECTIVE: To evaluate the effects of early treatment with Denosumab (⩽ 12 months after starting AIs) compared to a delayed treatment in BC women. METHODS: In this retrospective case-control study, we included medical records of BC post-menopausal women, treated with AIs therapy; they were divided as: study group (starting Denosumab ⩽ 12 months after AIs) and control group (> 12 months). At the baseline (T0) and at 18 months (T1), we evaluated the lum…

Osteoporosisrisk of fracture0302 clinical medicineRetrospective StudieBone DensityOrthopedics and Sports Medicine030212 general & internal medicineAromataseOsteoporosis PostmenopausalbiologyBone Density Conservation AgentsAromatase InhibitorsSettore MED/34 - Medicina Fisica E RiabilitativaMedical recordRehabilitationMiddle Agedmedicine.anatomical_structureDenosumab030220 oncology & carcinogenesisOsteoporosis risk of fractures breast cancer denosumab bone healthFemaleDenosumabCase-Control StudieBreast NeoplasmHumanmedicine.drugmedicine.medical_specialtyBone Density Conservation AgentPhysical Therapy Sports Therapy and RehabilitationBreast NeoplasmsBone health03 medical and health sciencesbreast cancerBreast cancerInternal medicinemedicineAromatase InhibitorHumansbone healthFemoral neckAgedRetrospective Studiesrisk of fracturesbusiness.industryOsteoporosiRetrospective cohort studymedicine.diseaseCase-Control Studiesbiology.proteinbusinessOsteoporotic Fractures
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Single-digit nanomolar inhibitors lock the aromatase active site via a dualsteric targeting strategy

2022

The most frequently diagnosed breast cancer (BC) type in women expresses estrogen receptor (ER) , depends on estrogens for its growth, being classified as ER positive (ER+). The gold standard therapy for the treatment of this tumor relies on the inhibition of the aromatase enzyme, which catalyzes estrogen biosynthesis. Despite the clinical success of current aromatase inhibitors (AIs), after prolonged therapeutic regimens, BC ER + patients experience acquired resistance and disease relapse. This points up the urgent need for a newer generation of AIs able to overcome resistance issues, while mitigating toxicity and side effects of current therapies. Here we performed the synthesis, biologic…

PharmacologyOrganic ChemistryBreast NeoplasmsGeneral MedicineMolecular dynamicsQM/MMAromataseAllosteric inhibitionAromatase inhibitorsBreast cancerReceptors EstrogenSettore CHIM/03 - Chimica Generale E InorganicaCatalytic DomainDrug DiscoveryBreast cancer; Aromatase inhibitors; Allosteric inhibition; Molecular dynamics; QM; MMHumansFemaleEuropean Journal of Medicinal Chemistry
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Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor

2020

The intensive use of pesticides has led to their increasing presence in water, soil, and agricultural products. Mounting evidence indicates that some pesticides may be endocrine disrupting chemicals (EDCs), being therefore harmful for the human health and the environment. In this study, three pesticides, glyphosate, thiacloprid, and imidacloprid, were tested for their ability to interfere with estrogen biosynthesis and/or signaling, to evaluate their potential action as EDCs. Among the tested compounds, only glyphosate inhibited aromatase activity (up to 30%) via a non-competitive inhibition or a mixed inhibition mechanism depending on the concentration applied. Then, the ability of the thr…

aromatasemedicine.drug_classHealth Toxicology and Mutagenesislcsh:MedicineEstrogen receptorMixed inhibitionEndocrine Disruptors010501 environmental sciencesPharmacology01 natural sciencesArticle03 medical and health scienceschemistry.chemical_compoundImidaclopridReceptorsmedicineHumansAromataseestrogenic activity030304 developmental biology0105 earth and related environmental sciences0303 health sciencesAromatase inhibitorendocrine disrupting chemicalbiologyAromatase Inhibitorslcsh:RPublic Health Environmental and Occupational HealthEstrogenspesticidesPesticideThiaclopridEstrogenmolecular dynamicsReceptors EstrogenchemistryEstrogenMELN allosteric inhibitionbiology.proteingene reporter assayAromatase; Endocrine disrupting chemical; Estrogen receptor; Estrogenic activity; Gene reporter assay; MELN allosteric inhibition; Molecular dynamics; Neonicotinoids; Pesticides; Aromatase; Aromatase Inhibitors; Estrogens; Humans; Receptors Estrogen; Endocrine Disruptors; Pesticidesneonicotinoidsestrogen receptorInternational Journal of Environmental Research and Public Health
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Effect of Combining Impact-Aerobic and Strength Exercise, and Dietary Habits on Body Composition in Breast Cancer Survivors Treated with Aromatase In…

2023

This study examines both the effect of a twice-weekly combined exercise—1 h session of strength and 1 h session of impact-aerobic—on body composition and dietary habits after one year of treatment with aromatase inhibitors (AI) in breast cancer survivors. Overall, forty-three postmenopausal women with a BMI ≤ 35 kg/m2, breast cancer survivors treated with AI, were randomized into two groups: a control group (CG) (n = 22) and a training group (IG) (n = 21). Body composition, i.e., abdominal, visceral, and subcutaneous adipose tissue) was measured by magnetic resonance. In addition, some questionnaires were used to gather dietary data and to measure adherence to the Mediterranean diet. After …

body compositionnaisetrintasyöpäbreast cancer survivorscombined exerciseHealth Toxicology and Mutagenesisstrength exercisePublic Health Environmental and Occupational Healthruokavaliotaromatase inhibitorscombined exercise; impact-aerobic exercise; strength exercise; dietary habits; body composition; aromatase inhibitors; breast cancer survivorsravintoterveysvaikutuksetimpact-aerobic exercisevoimaharjoitteludietary habitskehonkoostumusInternational Journal of Environmental Research and Public Health; Volume 20; Issue 6; Pages: 4872
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Switching from Aromatase Inhibitors to Dual Targeting Flavonoid-Based Compounds for Breast Cancer Treatment

2023

Despite the significant outcomes attained by scientific research, breast cancer (BC) still represents the second leading cause of death in women. Estrogen receptor-positive (ER+) BC accounts for the majority of diagnosed BCs, highlighting the disruption of estrogenic signalling as target for first-line treatment. This goal is presently pursued by inhibiting aromatase (AR) enzyme or by modulating Estrogen Receptor (ER) α. An appealing strategy for fighting BC and reducing side effects and resistance issues may lie in the design of multifunctional compounds able to simultaneously target AR and ER. In this paper, previously reported flavonoid-related potent AR inhibitors were suitably modified…

homoisoflavones; aromatase inhibitors; ERα ligands; multitarget; molecular dynamicsOrganic ChemistryPharmaceutical ScienceERα ligandshomoisoflavonesmolecular dynamicsaromatase inhibitorsAnalytical ChemistrySettore CHIM/03 - Chimica Generale E InorganicaChemistry (miscellaneous)Drug DiscoveryMolecular MedicinemultitargetPhysical and Theoretical ChemistryMolecules
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Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors

2020

[Image: see text] Breast cancer (BC) is the most diffused cancer type in women and the second leading cause of death among the female population. Effective strategies to fight estrogen responsive (ER+) BC, which represents 70% of all BC cases, rely on estrogen deprivation, via the inhibition of the aromatase enzyme, or the modulation of its cognate estrogen receptor. Current clinical therapies significantly increased patient survival time. Nevertheless, the onset of resistance in metastatic BC patients undergoing prolonged treatments is becoming a current clinical challenge, urgently demanding to devise innovative strategies. In this context, here we designed, synthesized, and performed in …

medicine.drug_classAllosteric regulation01 natural sciencesBiochemistryBreast cancerbreast cancerDrug Discoverymedicinecytochromes P450AromataseCause of deathFemale populationchemistry.chemical_classificationbiology010405 organic chemistrybusiness.industrymolecular dynamicOrganic ChemistryDual modeAromatase inhibitormedicine.diseasemolecular dynamics0104 chemical sciences010404 medicinal & biomolecular chemistryAromatase inhibitorschemistryEstrogenSettore CHIM/03 - Chimica Generale E Inorganicaxanthonebiology.proteinCancer researchAzolebusiness
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The Patient's Anastrozole Compliance to Therapy (PACT) Program: a randomized, in-practice study on the impact of a standardized information program o…

2013

BACKGROUND Compliance and persistence are often overlooked in adjuvant breast cancer treatment. PATIENTS AND METHODS PACT was a prospective, multicenter, randomized, open, parallel-group study assessing whether educational materials (EMs) enhanced compliance with aromatase inhibitor (AI) therapy in postmenopausal women with early, hormone-receptor-positive (HR+) breast cancer. The primary end points were compliance (proportion taking ≥ 80% anastrozole) at 12 months and persistence (proportion reporting anastrozole intake during the study period). RESULTS Four thousand eight hundred and forty-four patients were randomly assigned 1:1 to receive standard therapy or standard therapy with EMs. T…

medicine.medical_specialtyAntineoplastic Agents Hormonalmedicine.drug_classmedicine.medical_treatmentAnastrozoleBreast NeoplasmsAnastrozolePactPersistence (computer science)Medication AdherenceEosinophilia–myalgia syndromeBreast cancerInternal medicineNitrilesmedicineHumansProspective StudiesEarly Detection of CancerAgedGynecologyAromatase inhibitorbusiness.industrySurrogate endpointHematologyMiddle AgedTriazolesmedicine.diseasePostmenopauseOncologyPatient ComplianceFemalebusinessAdjuvantmedicine.drugFollow-Up StudiesAnnals of oncology : official journal of the European Society for Medical Oncology
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Assessment of Quality of Life in Postmenopausal Women with Early Breast Cancer Participating in the PACT Trial: The Impact of Additional Patient Info…

2019

<b><i>Background:</i></b> Breast cancer patients’ self-understanding of their disease can impact their quality of life (QoL); the relationship between compliance and QoL is poorly understood. <b><i>Patients and Methods:</i></b> The Patient’s Anastrozole Compliance to Therapy (PACT) program, a prospective, randomized study, investigated the effect of additional patient information material (IM) packages on compliance with adjuvant aromatase inhibitor (AI) therapy in postmenopausal women with hormone receptor-positive early breast cancer. The QoL subanalysis presented here examined the impact of IM packages on QoL and the association between QoL…

medicine.medical_specialtymedicine.drug_classAnastrozoleDiseasePactlaw.invention03 medical and health sciences0302 clinical medicineBreast cancerQuality of lifeRandomized controlled triallawmedicine030212 general & internal medicineAromatase inhibitorbusiness.industryCancermedicine.diseasehumanitiesOncology030220 oncology & carcinogenesisPhysical therapySurgerybusinessResearch Articlemedicine.drugBreast Care
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Women, thrombosis, and cancer: A gender-specific analysis.

2017

Venous thromboembolism (VTE) is a major common complication in cancer patients. Risk-adapted thromboprophylaxis and antithrombotic therapy for patients diagnosed with VTE can reduce the recurrence of VTE events. Thrombotic risk varies according to cancer type, stage, and comorbidities. The current review analyzes most recent data and provides clinical guidance for the management of women with cancer-associated thrombosis.

medicine.medical_specialtymedicine.drug_classmedicine.medical_treatmentPregnancy Complications CardiovascularLow molecular weight heparin030204 cardiovascular system & hematologyPregnancy Complications Cardiovascular/drug therapy/epidemiology03 medical and health sciences0302 clinical medicinePregnancyRisk FactorsInternal medicineNeoplasmsAntithromboticMedicineHumanscardiovascular diseasesddc:616Venous Thromboembolism/drug therapy/epidemiologybusiness.industryAromatase InhibitorsAnticoagulantCancerAnticoagulantsThrombosisHematologyVenous Thromboembolismmedicine.diseaseequipment and suppliesThrombosisNeoplasms/complications/epidemiologySurgeryPostmenopauseVenous thrombosisAnticoagulants/therapeutic use030220 oncology & carcinogenesisFemaleHormone therapybusinessComplicationPregnancy Complications NeoplasticPregnancy Complications Neoplastic/epidemiologyThrombosis/drug therapy/epidemiologyAromatase Inhibitors/therapeutic useThrombosis research
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Abemaciclib: safety and effectiveness of a unique cyclin-dependent kinase inhibitor

2020

Introduction: The discovery and the clinical availability of novel cyclin-dependent kinases 4 and 6 inhibitors have profoundly changed the therapeutic scenario of metastatic hormone receptor-positive breast carcinoma. Among these inhibitors, abemaciclib can induce potent and sustained cell cycle arrest and immune system stimulation. Areas covered: This review summarizes the safety profile and clinical efficacy data on abemaciclib alone or in combination with aromatase inhibitors or fulvestrant in metastatic hormone receptor-positive breast carcinoma. The management of patients treated with abemaciclib is the object of this paper. Expert opinion: As shown in phase 2 and 3 clinical trials on …

safetyAminopyridinesBreast Neoplasms030204 cardiovascular system & hematology03 medical and health scienceschemistry.chemical_compoundabemaciclib breast cancer metastases hormonal receptors safetybreast cancer0302 clinical medicineBreast cancerCyclin-dependent kinaseAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansPharmacology (medical)metastasesskin and connective tissue diseasesFulvestrantProtein Kinase InhibitorsAbemaciclibbiologyAromatase Inhibitorsbusiness.industryKinasehormonal receptorsCyclin-Dependent Kinase 4Cell Cycle CheckpointsCyclin-Dependent Kinase 6General Medicinemedicine.diseaseAbemaciclibchemistry030220 oncology & carcinogenesisQuality of LifeCancer researchbiology.proteinBenzimidazolesFemalesense organsbusinessHormone
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