Search results for "ZOL"

showing 10 items of 4792 documents

PD123319, angiotensin II type II receptor antagonist, inhibits oxidative stress and inflammation in 2, 4-dinitrobenzene sulfonic acid-induced colitis…

2019

Angiotensin II, the main effector of renin angiotensin system, plays an important role in the inflammatory process and most of its effects are mediated through the AT1 receptor activation. However, the knowledge about the AT2 receptor involvement in this process is still evolving. We previously found that in an experimental model of colitis, AT2 receptor activation can contribute to the impairment of the muscle contractility in vitro in the course of inflammation. Here, we investigated the potential alleviating effects of the in vivo treatment of PD123319 (1-[[4-(Dimethylamino)-3-methylphenyl]methyl]-5-(diphenylacetyl)-4,5,6,7- tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid ditriflu…

Male0301 basic medicineColonPyridinesmedicine.drug_classImmunologyAngiotensin II Type 2 Receptor BlockersPharmacologyAT2 receptorReceptor Angiotensin Type 2Inflammatory bowel diseaseInflammatory bowel diseaseProinflammatory cytokineContractility03 medical and health sciencesAngiotensin0302 clinical medicinemedicineAnimalsPharmacology (medical)Rats WistarColitisReceptorPharmacologyInflammationAngiotensin II receptor type 1ChemistryAngiotensin IIImidazolesColitismedicine.diseaseReceptor antagonistAngiotensin IIRatsDinitrobenzenesOxidative Stress030104 developmental biology030217 neurology & neurosurgery
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Overall survival in patients with BRAF-mutant melanoma receiving encorafenib plus binimetinib versus vemurafenib or encorafenib (COLUMBUS): a multice…

2018

Summary Background Encorafenib plus binimetinib and encorafenib alone improved progression-free survival compared with vemurafenib in patients with BRAF V600 -mutant melanoma in the COLUMBUS trial. Here, we report the results of the secondary endpoint of overall survival. Methods COLUMBUS was a two-part, randomised, open-label, phase 3 study done at 162 hospitals in 28 countries. Eligible patients were aged at least 18 years with histologically confirmed, locally advanced, unresectable, or metastatic cutaneous melanoma, or unknown primary melanoma, BRAF V600E or BRAF V600K mutation, an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1, and were treatment naive or had pr…

Male0301 basic medicineOncologySkin NeoplasmsTime FactorsMedizinPhases of clinical researchGene mutationchemistry.chemical_compound0302 clinical medicineAntineoplastic Combined Chemotherapy ProtocolsVemurafenibMelanomaAged 80 and overTrametinibSulfonamides10177 Dermatology ClinicBinimetinibMiddle AgedProgression-Free SurvivalPhenotypeOncologyTolerability030220 oncology & carcinogenesisDisease ProgressionFemale2730 Oncologymedicine.drugAdultProto-Oncogene Proteins B-rafmedicine.medical_specialty610 Medicine & healthYoung Adult03 medical and health sciencesInternal medicineBiomarkers TumormedicineHumansGenetic Predisposition to DiseaseProgression-free survivalProtein Kinase InhibitorsAgedPerformance statusbusiness.industry030104 developmental biologyVemurafenibchemistryMutationBenzimidazolesCarbamatesbusinessThe Lancet Oncology
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The comparison of outcomes from tyrosine kinase inhibitor monotherapy in second- or third-line for advanced non-small-cell lung cancer patients with …

2016

// Giuseppe Bronte 1, * , Tindara Franchina 2, * , Massimiliano Alu 3, * , Giovanni Sortino 1 , Claudia Celesia 1 , Francesco Passiglia 1 , Giuseppina Savio 3 , Agata Laudani 3 , Alessandro Russo 2 , Antonio Picone 2 , Sergio Rizzo 1 , Michele De Tursi 4 , Elisabetta Gambale 4 , Viviana Bazan 1 , Clara Natoli 4 , Livio Blasi 3 , Vincenzo Adamo 2 , Antonio Russo 1 1 Department of Surgical, Oncological and Oral Sciences, University of Palermo, Palermo, Italy 2 Medical Oncology Unit-AOOR Papardo-Piemonte, Messina and Department of Human Pathology, University of Messina, Messina, Italy 3 Medical Oncology Unit, A.R.N.A.S. Civico, Palermo, Italy 4 Department of Medical, Oral and Biotechnological …

Male0301 basic medicineOncologymedicine.medical_specialtyLung Neoplasmsmedicine.drug_classEGFRTyrosine kinase inhibitorKaplan-Meier EstimateTyrosine-kinase inhibitorErlotinib Hydrochloride03 medical and health sciences0302 clinical medicineGefitinibCarcinoma Non-Small-Cell LungInternal medicinemedicineHumansChemotherapyErlotinib HydrochlorideLung cancerProtein Kinase InhibitorsChemotherapy EGFR Non-small-cell lung cancer Tyrosine kinase inhibitor OncologyAgedRetrospective StudiesAged 80 and overPerformance statusbusiness.industryChemotherapy; EGFR; Non-small-cell lung cancer; Tyrosine kinase inhibitor; OncologyGefitinibRetrospective cohort studyMiddle Agedmedicine.diseaserespiratory tract diseasesSurgeryErbB ReceptorsClinical trialTreatment Outcome030104 developmental biologyOncology030220 oncology & carcinogenesisMutationQuinazolinesFemaleErlotinibbusinessNon-small-cell lung cancerResearch Papermedicine.drug
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Ibrutinib versus temsirolimus in patients with relapsed or refractory mantle-cell lymphoma : an international, randomised, open-label, phase 3 study

2016

Mantle-cell lymphoma is an aggressive B-cell lymphoma with a poor prognosis. Both ibrutinib and temsirolimus have shown single-agent activity in patients with relapsed or refractory mantle-cell lymphoma. We undertook a phase 3 study to assess the efficacy and safety of ibrutinib versus temsirolimus in relapsed or refractory mantle-cell lymphoma.This randomised, open-label, multicentre, phase 3 clinical trial enrolled patients with relapsed or refractory mantle-cell lymphoma confirmed by central pathology in 21 countries who had received one or more rituximab-containing treatments. Patients were stratified by previous therapy and simplified mantle-cell lymphoma international prognostic index…

Male0301 basic medicineOncologymedicine.medical_specialtyPhases of clinical researchAntineoplastic AgentsKaplan-Meier EstimateLymphoma Mantle-Cell03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternational Prognostic IndexPiperidinesRecurrenceInternal medicinemedicineHumansAgedNeoplasm StagingAged 80 and overSirolimusbusiness.industryBortezomibAdenineGeneral MedicineMiddle AgedTemsirolimusSurgeryClinical trialPyrimidinesTreatment Outcome030104 developmental biologyTolerabilitychemistry030220 oncology & carcinogenesisIbrutinibRefractory Mantle Cell LymphomaPyrazolesFemalebusinessmedicine.drug
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Pulmonary infiltrate with characteristic “reversed halo” and “air crescent” signs

2016

Male0301 basic medicinePathologymedicine.medical_specialtyAntifungal AgentsPancytopenia030106 microbiologyAstrocytoma030218 nuclear medicine & medical imagingImmunocompromised Host03 medical and health sciences0302 clinical medicineBronchoscopyInternal MedicineHumansMedicineInvasive Pulmonary Aspergillosisbusiness.industryMiddle AgedCombined Modality TherapyAspergillusPulmonary infiltratesVoriconazoleHaloTomography X-Ray Computedbusiness
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Neuronal nitric oxide synthase is involved in CB/TRPV1 signalling: Focus on control of hippocampal hyperexcitability

2017

Cannabinoids (CB), transient receptors potential vanilloid type 1 (TRPV1) and nitric oxide (NO) were found to be interlinked in regulating some neuronal functions such as membrane excitability and synaptic transmission. TRPV1 play a fundamental role since it represents a synaptic target for CB that triggers several downstream cellular pathways. In this regard, recent evidence report that TRPV1 could influence NO production by modulating neuronal NO synthase (nNOS) activity. In the present research, we pointed to manipulate nNOS function to assess its role on TRPV1 signalling in hyperexcitability conditions elicited in the dentate gyrus of hippocampal formation. The activation of TRPV1 recep…

Male0301 basic medicineTime FactorsAction PotentialsHippocampusStimulationNitric Oxide Synthase Type IHippocampal formationHippocampusSettore BIO/09 - Fisiologia0302 clinical medicineRosaniline DyesEnzyme InhibitorsChemistryElectrophysiologyNeurologyExcitatory postsynaptic potentialAnticonvulsantsSignal TransductionAgonistIndazolesmedicine.drug_classMorpholinesTRPV1TRPV Cation ChannelsMaximal Dentate ActivationNaphthalenesNeurotransmissionArginineTransient receptors potential vanilloid type 103 medical and health sciencesHippocampumedicineAnimalsRats WistarCannabinoidAnalysis of VarianceCannabinoidsDentate gyrusNitric oxideElectric StimulationBenzoxazinesRats030104 developmental biologynervous systemSensory System AgentsCannabinoids; Electrophysiology; Hippocampus; Maximal Dentate Activation; Nitric oxide; Transient receptors potential vanilloid type 1; Neurology; Neurology (clinical)Neurology (clinical)CapsaicinNeuroscience030217 neurology & neurosurgeryEpilepsy Research
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Effect of High‐Caloric Nutrition on Survival in Amyotrophic Lateral Sclerosis

2019

International audience; Objective: Weight loss has been identified as a negative prognostic factor in amyotrophic lateral sclerosis, but there is no evidence regarding whether a high-caloric diet increases survival. Therefore, we sought to evaluate the efficacy of a high-caloric fatty diet (HCFD) for increasing survival.Methods: A 1:1 randomized, placebo-controlled, parallel-group, double-blinded trial (LIPCAL-ALS study) was conducted between February 2015 and September 2018. Patients were followed up at 3, 6, 9, 12, 15, and 18 months after randomization. The study was performed at 12 sites of the clinical and scientific network of German motor neuron disease centers (ALS/MND-NET). Eligible…

Male0301 basic medicinemortality [Amyotrophic Lateral Sclerosis]MESH: Combined Modality Therapy[SDV]Life Sciences [q-bio]law.invention0302 clinical medicineMESH: RiluzoleRandomized controlled triallawdiet therapy [Amyotrophic Lateral Sclerosis]Clinical endpointMedicineMESH: Double-Blind Methodtherapeutic use [Riluzole]MESH: Amyotrophic Lateral Sclerosismethods [Combined Modality Therapy]education.field_of_studyRiluzoleMESH: Middle AgedHazard ratioMESH: Neuroprotective AgentsMiddle Agedtherapeutic use [Neuroprotective Agents]Combined Modality Therapy3. Good healthRiluzole[SDV] Life Sciences [q-bio]Neuroprotective AgentsNeurologyMESH: Survival AnalysisFemalemedicine.drugmortality [Diet High-Fat]medicine.medical_specialtyPopulationDiet High-FatPlacebo03 medical and health sciencesDouble-Blind MethodInternal medicineHumansddc:610educationSurvival analysisMESH: Humansdrug therapy [Amyotrophic Lateral Sclerosis]business.industryAmyotrophic Lateral SclerosisSurvival AnalysisConfidence intervalMESH: MaleMESH: Diet High-Fat030104 developmental biologyNeurology (clinical)businessMESH: Female030217 neurology & neurosurgery
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Aromatase Inhibitors Plus Weight Loss Improves the Hormonal Profile of Obese Hypogonadal Men Without Causing Major Side Effects

2020

Objective: In obese men, the increased expression of the aromatase enzyme in adipose tissue leads to high conversion of androgens to estrogens contributing to hypogonadotropic hypogonadism (HHG). Our objective is to evaluate efficacy and safety of weight loss (WL) plus aromatase inhibitor (AI) therapy in severely obese men with HHG. We hypothesize that AI+WL will be more effective as compared to WL alone in improving the hormonal profile, thus muscle strength and symptoms of HHG (primary outcomes), with no significant adverse effects on lean mass, metabolic profile, and bone mineral density (secondary outcomes).Design: Randomized double-blind placebo-controlled pilot trial.Methods: Twenty-t…

Male0301 basic medicineobesityBone densityEndocrinology Diabetes and MetabolismPilot Projectslcsh:Diseases of the endocrine glands. Clinical endocrinologyaromatase inhibitorsEndocrinology0302 clinical medicineBone DensityWeight lossMedicineTestosteroneTestosteroneBone mineralEstradiolMiddle AgedPrognosisClinical TrialAndrogensMetabolomemedicine.symptombone microarchitecturemedicine.drugAdultmedicine.medical_specialtyHormone Replacement Therapymedicine.drug_classAnastrozole030209 endocrinology & metabolismsex hormonesBone and Bones03 medical and health sciencesDouble-Blind MethodHypogonadotropic hypogonadismInternal medicineWeight LossHumanshypogonadismMuscle StrengthAgedbody compositionlcsh:RC648-665Aromatase inhibitorbusiness.industrymedicine.disease030104 developmental biologyEndocrinologyLean body massbusinessBiomarkersFollow-Up StudiesFrontiers in Endocrinology
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Real-life use of elbasvir/grazoprevir in adults and elderly patients: a prospective evaluation of comedications used in the PITER cohort.

2021

Background In patients treated for HCV infection, potential drug–drug interactions (DDIs) can occur among direct-acting antiviral drugs (DAAs) and comedications used. The real-life effectiveness and safety of elbasvir/grazoprevir (ELB/GZR) among co-medicated HCV patients was evaluated. Methods We prospectively evaluated consecutive patients from 15 clinical centres participating in PITER who were treated with ELB/GZR and had been followed for at least 12 weeks after treatment. Data were prospectively collected on the use of comedications (including discontinuation, dose modification and addition of drugs) and potential DDIs with DAAs. Results Of the 356 patients with at least 12-week post-t…

Male030312 virologycombination therapytreatment experienced patientsDrug Combinationchronic hepatitis C drug drug interactions virus genotype 1 treatment experienced patients pump inhibitor use combination therapy treatment naive liver fibrosisgrazoprevir elbasvir80 and overAge FactorPharmacology (medical)Drug InteractionsProspective StudiesChronicProspective cohort studyliver fibrosisAged 80 and over0303 health sciencesAge FactorsImidazolesMiddle AgedHepatitis CDrug CombinationsInfectious DiseasesTreatment OutcomeDrug InteractionGrazoprevirCohortdrug drug interactionsFemalepump inhibitor useHumanmedicine.drugmedicine.medical_specialtyElbasvirQuinoxalinetreatment naiveelbasvirAntiviral AgentsNO03 medical and health sciencesInternal medicineQuinoxalinesmedicinechronic hepatitis CElbasvir GrazoprevirHumansImidazoleAgedBenzofuransAntiviral AgentPharmacology...business.industrygrazoprevirCarbamazepineHepatitis C Chronicmedicine.diseaseComorbidityDiscontinuationBenzofuranAge Factors; Aged; Aged 80 and over; Antiviral Agents; Benzofurans; Drug Combinations; Drug Interactions; Female; Hepatitis C Chronic; Humans; Imidazoles; Male; Middle Aged; Prospective Studies; Quinoxalines; Treatment Outcomebusinessvirus genotype 1Antiviral therapy
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Synthesis and pharmacological evaluation of 1-methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acid derivatives

1998

Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl] -1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3 alpha-HSD, but no correlation was observed with …

Male3-Hydroxysteroid DehydrogenasesStereochemistryAnti-Inflammatory AgentsPharmaceutical SciencePyrazoleChemical synthesisMicechemistry.chemical_compoundAcetic acidIn vivoDrug DiscoveryPhenylbutazonemedicineAnimalsEnzyme InhibitorsAnalgesicsbiology3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)Acute toxicityRatschemistryEnzyme inhibitorToxicitybiology.proteinPyrazolesmedicine.drugIl Farmaco
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