Search results for "AMIDES"

showing 10 items of 552 documents

Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF -mutant melanoma (COLUMBUS): a multicentre, open-label, randomis…

2017

Summary Background Combined BRAF-MEK inhibitor therapy is the standard of care for BRAF V600 -mutant advanced melanoma. We investigated encorafenib, a BRAF inhibitor with unique target-binding properties, alone or in combination with the MEK inhibitor binimetinib, versus vemurafenib in patients with advanced BRAF V600 -mutant melanoma. Methods COLUMBUS was conducted as a two-part, randomised, open-label phase 3 study at 162 hospitals in 28 countries. Eligible patients were aged 18 years or older and had histologically confirmed locally advanced (American Joint Committee on Cancer [AJCC] stage IIIB, IIIC, or IV), unresectable or metastatic cutaneous melanoma, or unknown primary melanoma; a B…

AdultMaleProto-Oncogene Proteins B-raf0301 basic medicineOncologymedicine.medical_specialtySkin NeoplasmsTime FactorsPhases of clinical researchYoung Adult03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsBiomarkers TumormedicineHumansMolecular Targeted TherapyProgression-free survivalVemurafenibMelanomaProtein Kinase InhibitorsAgedAged 80 and overSulfonamidesPerformance statusbusiness.industryMelanomaMEK inhibitorBinimetinibMiddle Agedmedicine.diseaseProgression-Free Survival030104 developmental biologyVemurafenibOncologyTolerabilitychemistry030220 oncology & carcinogenesisMutationBenzimidazolesFemaleCarbamatesbusinessmedicine.drugThe Lancet Oncology
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Erythema nodosum-like lesions during BRAF inhibitor therapy: Report on 16 new cases and review of the literature.

2015

Importance BRAF inhibitors have been licensed for the therapy of BRAF-mutated melanoma. Recently, inflammatory skin lesions clinically resembling erythema nodosum have been reported as therapy side-effects that may lead to treatment discontinuation. Objective To identify and characterize cases with BRAF inhibitor-associated erythema nodosum-like inflammatory skin lesions and development of an algorithm for their management. Design and Setting Retrospective chart review of melanoma patients treated with BRAF inhibitors in 14 departments of Dermatology in Germany and Austria and PubMed search for cases in the literature. Results Sixteen patients were identified who developed erythema nodosum-…

AdultMaleProto-Oncogene Proteins B-rafmedicine.medical_specialtyIndolesErythemaBiopsyMedizinDermatology030207 dermatology & venereal diseases03 medical and health sciencesYoung Adult0302 clinical medicineErythema NodosumOximesmedicineHumansskin and connective tissue diseasesVemurafenibneoplasmsAgedRetrospective StudiesSkinTrametinibErythema nodosumSulfonamidesintegumentary systembusiness.industryMelanomaImidazolesDabrafenibMiddle Agedmedicine.diseaseDermatology3. Good healthInfectious DiseasesVemurafenib030220 oncology & carcinogenesisFemalemedicine.symptombusinessPanniculitisVasculitismedicine.drugJournal of the European Academy of Dermatology and Venereology : JEADV
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Human dopamine receptor D2/D3 availability predicts amygdala reactivity to unpleasant stimuli

2009

r r Abstract: Dopamine (DA) modulates the response of the amygdala. However, the relation between dopa- minergic neurotransmission in striatal and extrastriatal brain regions and amygdala reactivity to affective stimuli has not yet been established. To address this issue, we measured DA D2/D3 receptor (DRD2/3) availability in twenty-eight healthy men (nicotine-dependent smokers and never-smokers) using positron emission tomography with ( 18 F)fallypride. In the same group of participants, amygdala response to unpleasant visual stimuli was determined using blood oxygen level-dependent (BOLD) functional mag- netic resonance imaging. The effects of DRD2/3 availability in emotion-related brain …

AdultMalePyrrolidinesEmotionsNeurotransmissionAmygdalaDopamine receptor D3DopamineDopamine receptor D2medicineHumansRadiology Nuclear Medicine and imagingPrefrontal cortexResearch ArticlesBrain MappingRadiological and Ultrasound TechnologyReceptors Dopamine D2SmokingReceptors Dopamine D3Tobacco Use DisorderAmygdalaMagnetic Resonance ImagingOxygenmedicine.anatomical_structureNeurologyFallyprideCerebrovascular CirculationPositron-Emission TomographyBenzamidesVisual PerceptionAnxietyNeurology (clinical)Anatomymedicine.symptomPsychologyNeurosciencePhotic Stimulationmedicine.drug
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The applicability of SRTM in [18F]fallypride PET investigations: Impact of scan durations

2011

The high-affinity radioligand [18F]fallypride (FP) is frequently used for quantification of striatal/extrastriatal D2/3 receptors and the receptor occupancies of antipsychotics (APs). Its 110 minutes half-life allows long scan durations. However, the optimum scan duration is a matter of debate. This investigation focuses on scan-duration-related effects on simplified reference tissue model (SRTM) results and the time point of transient equilibrium in a large sample of dynamic FP positron emission tomography (PET) scans. Fifty drug-free and 50 AP-treated subjects underwent FP-PET scans (180 minutes scan duration). The binding potential ( BPND) of the putamen, thalamus, and temporal cortex w…

AdultMalePyrrolidinesTime FactorsMaterials scienceAdolescentShuttle Radar Topography MissionRadioligand AssayYoung AdultRadioligandmedicineHumansTemporal cortexTransient equilibriummedicine.diagnostic_testReceptors Dopamine D2business.industryMental DisordersPutamenReceptors Dopamine D3Binding potentialMiddle AgedCorpus StriatumNeurologyFallypridePositron emission tomographyPositron-Emission TomographyBenzamidesFemaleOriginal ArticleNeurology (clinical)Cardiology and Cardiovascular MedicineNuclear medicinebusinessAntipsychotic AgentsJournal of Cerebral Blood Flow & Metabolism
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Dopamine D2/D3 receptor availability and venturesomeness.

2011

The construct of impulsivity is considered as a major trait of personality. There is growing evidence that the mesolimbic dopamine system plays an important role in the modulation of impulsivity and venturesomeness, the two key components within the impulsivity-construct. The aim of the present study was to explore an association between trait impulsivity measured with self-assessment and the dopaminergic neurotransmission as measured by positron emission tomography (PET) in a cohort of healthy male subjects. In vivo D2/D3 receptor availability was determined with [(18)F]fallypride PET in 18 non-smoking healthy subjects. The character trait impulsivity was measured using the Impulsiveness-V…

AdultMaleSelf-AssessmentPyrrolidinesStatistics as TopicNeuroscience (miscellaneous)Neuropsychological TestsImpulsivityStatistical parametric mappingPersonality AssessmentBrain mappingDevelopmental psychologyCohort StudiesYoung AdultRisk-TakingDopamine receptor D3Dopamine receptor D2Surveys and QuestionnairesmedicineHumansRadiology Nuclear Medicine and imagingTemporal cortexBrain MappingReceptors Dopamine D2BrainPsychiatry and Mental healthFallypridePositron-Emission TomographyBenzamidesImpulsive Behaviormedicine.symptomPersonality Assessment InventoryPsychologyNeurosciencePsychiatry research
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Ezetimibe/Simvastatin 10/20 mg versus Rosuvastatin 10 mg in high-risk hypercholesterolemic patients stratified by prior statin treatment potency

2010

Abstract Objective This post-hoc analysis compared the lipid-altering efficacy of Ezetimibe/Simvastatin 10/20 mg (EZ/Simva) versus Rosuvastatin 10 mg (Rosuva) in patients stratified by statin potency/dose prior to randomization. Methods Patients with elevated low-density lipoprotein cholesterol (LDL-C) despite prior statin treatment (n = 618) were randomized 1:1 to EZ/Simva 10/20 mg or Rosuva 10 mg for 6 weeks. Percent change from baseline in lipids and attainment of lipid targets were assessed within each subgroup (low potency n = 369, high potency n = 249). Consistency of the treatment effect across subgroups was evaluated by testing for treatment-by-subgroup interaction. No multiplicity …

AdultMaleSimvastatinmedicine.medical_specialtySettore MED/09 - Medicina InternaStatinRandomizationAdolescentmedicine.drug_classEndocrinology Diabetes and MetabolismHypercholesterolemiaClinical BiochemistryUrologyPharmacologyYoung AdultEndocrinologyEzetimibemedicineHumansPotencyRosuvastatinRosuvastatin Calciumlcsh:RC620-627AgedBiochemistry medicalAged 80 and overSulfonamidesSimvastatin; Ezetimibe;hypercholesterolemic;ChemistryhypercholesterolemicResearchAnticholesteremic AgentsBiochemistry (medical)nutritional and metabolic diseasesMiddle AgedEzetimibeFluorobenzeneslcsh:Nutritional diseases. Deficiency diseasesRosuvastatin CalciumPyrimidinesTreatment OutcomeSimvastatinAzetidinesFemalelipids (amino acids peptides and proteins)Ezetimibe/simvastatinHydroxymethylglutaryl-CoA Reductase Inhibitorsmedicine.drugLipids in Health and Disease
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Lipid-altering efficacy of ezetimibe/simvastatin 10/20 mg compared with rosuvastatin 10 mg in high-risk hypercholesterolaemic patients inadequately c…

2009

SUMMARY Aims: To evaluate the efficacy of switching from a previous statin monotherapy to ezetimibe ⁄simvastatin (EZE ⁄SIMVA) 10 ⁄20 mg vs. rosuvastatin (ROSUVA) 10 mg. Methods: In this randomised, double-blind study, 618 patients with documented hypercholesterolaemia [low-density lipoprotein cholesterol (LDL-C) ‡ 2.59 and £ 4.92 mmol ⁄l] and with high cardiovascular risk who were taking a stable daily dose of one of several statin medications for ‡ 6 weeks prior to the study randomisation visit entered a 6-week open-label stabilisation ⁄screening period during which they continued to receive their prestudy statin dose. Following stratification by study site and statin dose ⁄potency, patien…

AdultMaleSimvastatinmedicine.medical_specialtyimvastatinStatinmedicine.drug_classHypercholesterolemiaCoronary Artery DiseaseGastroenterologyhypercholesterolaemicchemistry.chemical_compoundDouble-Blind MethodEzetimibeRisk FactorsInternal medicinemedicineHumansRosuvastatinRosuvastatin CalciumAgedAged 80 and overSulfonamidesbiologybusiness.industryCholesterolCholesterol LDLGeneral MedicineMiddle AgedFluorobenzenesRosuvastatin CalciumPyrimidinesTreatment OutcomeEndocrinologychemistrySimvastatinHMG-CoA reductasebiology.proteinAzetidinesDrug Therapy CombinationFemalelipids (amino acids peptides and proteins)Ezetimibe/simvastatinHydroxymethylglutaryl-CoA Reductase Inhibitorsbusinessezetimibemedicine.drugInternational Journal of Clinical Practice
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Loss of the preconditioning effect of rosuvastatin during sustained therapy: a human in vivo study

2011

Studies have demonstrated that the acute administration of 3-hydroxy-3 methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors has protective effects in the setting of ischemia-reperfusion (IR). Previously, we demonstrated that a single dose of rosuvastatin prevented IR-induced endothelial dysfunction in humans through a cyclooxygenase-2-dependent mechanism. Whether the chronic administration of HMG-CoA reductase inhibitors provides similar protection remains controversial and is unknown in humans. Eighteen male volunteers were randomized to receive a single dose of rosuvastatin (20 mg) or placebo. Twenty-four hours later, endothelium-dependent, radial artery flow-mediated dilation (FMD) w…

AdultMaleTime FactorsAdolescentEndotheliumPhysiologyCoenzyme AHyperemiaPharmacologyReductaseDrug Administration ScheduleYoung Adultchemistry.chemical_compoundDouble-Blind MethodIschemiaIn vivoPhysiology (medical)medicineHumansRosuvastatinRosuvastatin CalciumOntarioAnalysis of VarianceSulfonamidesCyclooxygenase 2 Inhibitorsbiologybusiness.industryFluorobenzenesVasodilationRosuvastatin CalciumPyrimidinesmedicine.anatomical_structurechemistryCelecoxibRegional Blood FlowReperfusion InjuryRadial ArteryHMG-CoA reductasebiology.proteinCelecoxibPyrazolesHydroxymethylglutaryl-CoA Reductase InhibitorsCardiology and Cardiovascular MedicinebusinessBlood Flow Velocitymedicine.drugAmerican Journal of Physiology-Heart and Circulatory Physiology
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Agomelatine and Hepatotoxicity: Implications of Cumulated Data Derived from Spontaneous Reports of Adverse Drug Reactions

2013

Considering the antidepressant agomelatine (AGM) there is a discrepancy between the widespread knowledge of the potential of AGM to cause hepatotoxic adverse drug reactions (ADR) and the availability of corresponding published data. This impedes an adequate assessment of the hepatotoxicity profile of AGM. We conducted a query of the database of a German Medical Regulatory Body (BfArM) and analyzed spontaneous reports of hepatotoxic ADR. We identified n=58 cases of AGM-related hepatotoxic ADR. Most frequent ADR was asymptomatic increase of liver enzymes (79%); n=6 patients (10%) with AGM-related toxic hepatitis were reported. Characteristics of patients: female sex (69%), age > 50 years (mea…

AdultMaleToxic hepatitismedicine.medical_specialtyDatabases FactualPharmacologyAsymptomaticLiver diseaseRisk FactorsGermanyInternal medicineAcetamidesPharmacovigilancemedicineHumansAgomelatinePharmacology (medical)ContraindicationAgedAged 80 and overPolypharmacybusiness.industryGeneral MedicineMiddle Agedmedicine.diseaseAntidepressive AgentsDiscontinuationPsychiatry and Mental healthFemaleChemical and Drug Induced Liver Injurymedicine.symptombusinessmedicine.drugPharmacopsychiatry
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Rationale and design of dal-VESSEL: a study to assess the safety and efficacy of dalcetrapib on endothelial function using brachial artery flow-media…

2011

Dalcetrapib increases high-density lipoprotein cholesterol (HDL-C) levels through effects on cholesteryl ester transfer protein (CETP). As part of the dalcetrapib dal-HEART clinical trial programme, the efficacy and safety of dalcetrapib is assessed in coronary heart disease (CHD) patients in the dal-VESSEL study (ClinicalTrials.gov identifier: NCT00655538), the design and methods of which are presented here. RESEARCH DESIGN AND STUDY METHOD: Men and women with CHD or CHD risk equivalent, with HDL-C levels50  mg/dL were recruited for a 36-week, double-blinded, placebo-controlled trial. After a pre-randomisation phase of up to 8 weeks, patients received dalcetrapib 600  mg/day or placebo in …

AdultMalemedicine.medical_specialtyAdolescentBrachial ArteryDalcetrapibCoronary DiseaseAtherosclerosis CETP inhibition Endothelial function Flow-mediated dilatation ester transfer protein density-lipoprotein cholesterol off-target toxicity cardiovascular-disease dependent vasodilation coronary risk nitric-oxide torcetrapib atherosclerosis cetpModels BiologicalPlaceboschemistry.chemical_compoundYoung AdultDouble-Blind Methodmedicine.arteryInternal medicineCholesterylester transfer proteinmedicineHumansSulfhydryl CompoundsBrachial arteryLipoprotein cholesterolFlow mediated vasodilatationAgedRationalizationbiologybusiness.industryAnticholesteremic AgentsEstersGeneral MedicineCetp inhibitionMiddle AgedAmidesCoronary heart diseaseClinical trialVasodilationTreatment OutcomechemistryRegional Blood FlowResearch DesignCardiologybiology.proteinlipids (amino acids peptides and proteins)FemaleEndothelium VascularbusinessAlgorithms
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