Search results for "Angiogenesis Inhibitors"

showing 10 items of 100 documents

Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Epheephrin system

2015

The Eph receptor-ephrin system is an emerging target for the development of novel anti-angiogenic therapies. Research programs aimed at developing small-molecule antagonists of the Eph receptors are still in their initial stage as available compounds suffer from pharmacological drawbacks, limiting their application in vitro and in vivo. In the present work, we report the design, synthesis and evaluation of structure-activity relationships of a class of Δ(5)-cholenoyl-amino acid conjugates as Eph-ephrin antagonists. As a major achievement of our exploration, we identified N-(3β-hydroxy-Δ(5)-cholen-24-oyl)-L-tryptophan (UniPR1331) as the first small molecule antagonist of the Eph-ephrin syste…

MaleModels MolecularAnti-angiogenic agentsAngiogenesis InhibitorsEpheephrin antagonistsPharmacologyEphA2MiceStructure-Activity RelationshipIn vivoCell Line TumorOral bioavailabilityProteineprotein interaction inhibitorsDrug DiscoveryAnimalsHumansStructure–activity relationshipEphrinAmino AcidsReceptorReceptors Eph Familychemistry.chemical_classificationPharmacologyDose-Response Relationship DrugMolecular StructureAnti-angiogenic agents; Bile acids; EphA2; Epheephrin antagonists; Oral bioavailability; Proteineprotein interaction inhibitors; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryErythropoietin-producing hepatocellular (Eph) receptorEndothelial CellsBiological activityGeneral MedicineEPH receptor A2biological factorsBile acidsAmino acidchemistryBiochemistryEphrins
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Osteonecrosis of the Jaw in Patients With Metastatic Renal Cell Cancer Treated With Bisphosphonates and Targeted Agents: Results of an Italian Multic…

2015

Osteonecrosis of the jaw (ONJ) associated with the use of bisphosphonates has been rarely reported in metastatic renal cell cancer (RCC) patients. Since the introduction of combined therapies consisting of nitrogen-containing bisphosphonates (NBPs) and targeted agents, an increasing number of RCC patients were reported to develop ONJ, suggesting that therapeutic angiogenesis suppression might increase the risk of ONJ in NBPs users. We performed a multicenter retrospective study and reviewed literature data to assess the occurrence and to investigate the nature of ONJ in RCC patients taking NBPs and targeted agents. Nine Italian Centers contributed to the data collection. Patients with expos…

MaleOncologyIndolesAngiogenesis InhibitorsPyrroleBevacizumab; m-TOR inhibitor; Sorafenib; Sunitinib; Zoledronic acidRetrospective StudieAntineoplastic Combined Chemotherapy ProtocolsSunitinibAged 80 and overDiphosphonatesSunitinibImidazolesOsteonecrosisKidney NeoplasmMiddle AgedSorafenibKidney NeoplasmsBevacizumabDiphosphonateItalyOncologyOsteonecrosiFemaleAngiogenesis InhibitorHumanmedicine.drugSorafenibmedicine.medical_specialtyBevacizumab; m-TOR inhibitor; Sorafenib; Sunitinib; Zoledronic acid; Aged; Aged 80 and over; Angiogenesis Inhibitors; Antineoplastic Combined Chemotherapy Protocols; Carcinoma Renal Cell; Diphosphonates; Female; Humans; Imidazoles; Indoles; Italy; Jaw; Kidney Neoplasms; Male; Middle Aged; Osteonecrosis; Pyrroles; Retrospective Studies; Oncology; UrologyBevacizumabUrologyInternal medicinemedicineHumansPyrrolesIn patientMetastatic renal cell cancerImidazoleCarcinoma Renal CellZoledronic acidAgedRetrospective StudiesAntineoplastic Combined Chemotherapy Protocolbusiness.industryRetrospective cohort studymedicine.diseasem-TOR inhibitorSurgeryZoledronic acidJawIndolebusinessOsteonecrosis of the jaw
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Phase II trial of ptk787/zk 222584 (vatalanib) administered orally once-daily or in two divided daily doses as second-line monotherapy in relapsed or…

2011

ABSTRACT Background The objective of this multicenter, prospective uncontrolled phase II trial was to determine efficacy, safety and tolerability of vatalanib, an oral angiogenesis inhibitor targeting all known vascular endothelial growth factor receptors, in the second-line treatment of non-small-cell lung cancer (NSCLC). Patients and methods Patients with stage IIIB/IV NSCLC-proven tumor progression during or after one platinum-based chemotherapy regimen received a fixed dose of 1250 mg vatalanib either once-daily dosing (QD) or two divided daily dosing (TDD: 500 mg a.m. + 750 mg p.m.) until disease progression or unacceptable toxicity. Primary end point was the disease control rate (DCR)…

MaleOncologyVatalanibmedicine.medical_specialtyLung NeoplasmsPyridinesMedizinPhases of clinical researchnon-small cell lung cancer (NSCLC)Angiogenesis InhibitorsAntineoplastic AgentsKaplan-Meier EstimateDisease-Free SurvivalRecurrenceCarcinoma Non-Small-Cell LungInternal medicinemedicineHumansProgression-free survivalDosingLung cancerNeoplasm StagingSalvage TherapyDose-Response Relationship Drugbusiness.industryHematologymedicine.diseaseChemotherapy regimenSurgeryOncologyTolerabilityPhthalazinesFemalebusiness
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Dicer and drosha expression and response to bevacizumab-based therapy in advanced colorectal cancer patients.

2013

PURPOSE: The miRNA-regulating enzymes Dicer and Drosha exhibit aberrant expression in several cancer types. Dicer and Drosha play a crucial role during the angiogenetic process in vitro and, for Dicer, in vivo. We aimed to investigate the potential role of Dicer and Drosha in predicting response to Bevacizumab-based therapy in advanced colorectal cancer (CRC) patients. METHODS: Dicer and Drosha mRNA levels were analysed in formalin-fixed paraffin-embedded specimens from patients affected by advanced CRC treated with or without Bevacizumab-containing regimens (n=116 and n=50, respectively) and from patients with diverticulosis as control group (n=20). The experimental data were obtained usin…

MaleRibonuclease IIICancer ResearchSettore MED/06 - Oncologia Medicagenetic processesAngiogenesis InhibitorsKaplan-Meier EstimateDEAD-box RNA HelicasesangiogenesisIntestinal MucosaOligonucleotide Array Sequence AnalysisAged 80 and overReverse Transcriptase Polymerase Chain Reactionfood and beveragesMiddle AgedPrognosisImmunohistochemistryCRCBevacizumabGene Expression Regulation NeoplasticqPCRTreatment OutcomeOncologyMonoclonalImmunohistochemistryFemaleColorectal Neoplasmsmedicine.drugAdultBevacizumabBiologyAntibodies Monoclonal HumanizedDroshaYoung AdultSDG 3 - Good Health and Well-beingmicroRNAmedicineHumansDroshamiRNAAgedGene Expression ProfilingfungiCancermedicine.diseaseGene expression profilingenzymes and coenzymes (carbohydrates)miRNA; angiogenesisMultivariate AnalysisCancer researchbiology.proteinBevacizumab; CRC; Dicer; Drosha; miRNAs; qPCRDicerDicer
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How Have Intravitreal Anti-VEGF and Dexamethasone Implant Been Used in Italy? A Multiregional, Population-Based Study in the Years 2010–2016

2020

Purpose. To describe intravitreal anti-VEGF drug and dexamethasone use in four Italian regions. Methods. Four regional claims databases were used to measure drug prevalence, compare dosing intervals to those recommended in the summary of product characteristics (SPC), and identify switchers. Bilateral treatment and diabetic macular edema (DME) coding algorithms were validated, linking claims with a sample of prospectively collected ophthalmological data. Results. Overall, 41,836 patients received ≥1 study drug in 2010–2016 (4.8 per 10,000 persons). In 2016, anti-VEGF drug use ranged from 0.8 (Basilicata) to 5.7 (Lombardy) per 10,000 persons while intravitreal dexamethasone use ranged from 0…

MaleVascular Endothelial Growth Factor A0301 basic medicineintravitrealAngiogenesis Inhibitorsalgorithm.0302 clinical medicineMedicineSummary of Product Characteristicsmedia_commonAged 80 and overDrug ImplantsvalidationLaser CoagulationRGeneral MedicineMiddle AgedItalyanti-VEGF030220 oncology & carcinogenesisMedicineFemaleclinical dataoriginal articleResearch Articlemedicine.drugDrugmedicine.medical_specialtyArticle Subjectmedia_common.quotation_subjectMEDLINEdexamethasonePharmacyMacular EdemaGeneral Biochemistry Genetics and Molecular BiologyInsurance Claim Review03 medical and health sciencesRanibizumabInternal medicineHumansDosingDexamethasoneAgedDiabetic RetinopathyGeneral Immunology and MicrobiologySettore MED/30 - Malattie Apparato Visivobusiness.industryclaims database030104 developmental biologydrug utilisationMacular Edema; Ranibizumab; Laser CoagulationImplantRanibizumabbusinessBioMed Research International
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Association of neovascular age-related macular degeneration with month and season of birth in Italy

2016

In order to investigate the influence of season and month of birth on the risk of neovascular age-related macular degeneration (n-AMD) in Italy, we evaluated the month birth and sex of all patients, recorded in the anti-vascular endothelial growth factor (VEGF) monitoring registry of the Italian Medicines Agency, born between 1925-1944, who received intravitreal anti-VEGF injections for n-AMD between January 1, 2013 and July 29, 2015. The numbers of all births in Italy in the same years, extracted from the Italian National Institute of Statistics, were used to calculate the expected number of n-AMD cases. Overall, 45,845 patients (19,207 men, 26,638 women) received intravitreal anti-VEGF fo…

MaleVascular Endothelial Growth Factor AAginggenetic structuresMonth of birthVEGF receptorsneovascular AMDAngiogenesis InhibitorsAptamersMacular Degeneration0302 clinical medicineSeason of birthReceptors80 and overMedicineRegistriesAged 80 and overNeovascularization PathologicbiologyVascular Endothelial Growth FactorIncidenceIncidence (epidemiology)Aptamers NucleotideBevacizumabTreatment OutcomeItalyanti-VEGFFemaleSeasonsNucleotideNeovascular age-related macular degenerationResearch Papermedicine.drugAnti-VEGF; Month of birth; Neovascular age-related macular degeneration; Neovascular AMD; Season of birth; Aged; Aged 80 and over; Angiogenesis Inhibitors; Aptamers Nucleotide; Bevacizumab; Female; Humans; Incidence; Italy; Macular Degeneration; Male; Neovascularization Pathologic; Ranibizumab; Receptors Vascular Endothelial Growth Factor; Recombinant Fusion Proteins; Registries; Treatment Outcome; Vascular Endothelial Growth Factor A; Seasons; Aging; Cell BiologySeason of birthBevacizumabRecombinant Fusion ProteinsNeovascular AMDneovascular age-related macular degeneration03 medical and health sciencesRanibizumabAge relatedHumansNeovascularizationAgedPathologicseason of birthbusiness.industrymonth of birthAnti-VEGFCell BiologyMacular degenerationmedicine.diseaseeye diseasesanti-VEGF; month of birth; neovascular AMD; neovascular age-related macular degeneration; season of birthReceptors Vascular Endothelial Growth Factor030221 ophthalmology & optometrybiology.proteinsense organsRanibizumabbusinessMonth of birth030217 neurology & neurosurgeryDemographyAging
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Course of intraocular pressure after intravitreal injection of 0.05 mL ranibizumab (Lucentis).

2009

Purpose This prospective study examines the changes in short-term intraocular pressure (IOP) in patients with wet age-related macular degeneration (AMD) receiving intravitreal injections of 0.05 mL ranibizumab (Lucentis®) in a supine position. Methods A total of 45 eyes (45 patients, 16 M, 29 F, mean age: 78 y) received intravitreal ranibizumab injections for treatment of wet AMD (0.05 mL = 0.5 mg). The IOP was measured by Schiötz tonometry immediately preoperatively and postoperatively, and also after 3 and 10 minutes in a supine position. No history of glaucoma was present. Results The mean preoperative IOP was 22.4±5.5 mmHg in supine position. Immediately after the injection, IOP increas…

MaleVascular Endothelial Growth Factor AIntraocular pressuremedicine.medical_specialtySupine positiongenetic structuresAngiogenesis InhibitorsAntibodies Monoclonal HumanizedInjections03 medical and health sciencesTonometry Ocular0302 clinical medicineOphthalmologyRanibizumabWet age-related macular degenerationmedicineSupine PositionHumansIn patientProspective StudiesProspective cohort studyIntraocular PressureAgedAged 80 and overbusiness.industryAntibodies MonoclonalGeneral MedicineMacular degenerationMiddle Agedmedicine.diseaseeye diseasesVitreous BodyOphthalmology030221 ophthalmology & optometryWet Macular DegenerationFemalesense organsRanibizumabbusiness030217 neurology & neurosurgerymedicine.drugEuropean journal of ophthalmology
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Outcomes of cataract surgery in diabetic patients: results of the Pan American Collaborative Retina Study Group.

2014

Purpose: This study was designed to evaluate the visual and anatomical outcomes after cataract surgery in diabetic patients with different intraoperative therapeutic strategies. Methods: The research design comprised of a multicentric, retrospective, interventional study conducted at 6 centers in Argentina, Brazil, Costa Rica, Puerto Rico, Spain, and Venezuela. We included 138 diabetic patients with at least 6-month follow-up following phacoemulsification and intraocular lens implantation. Best-corrected visual acuity (BCVA) and central subfield thickness were collected at baseline and at 1-, 2-, 3-, and 6-month follow-up. Of these, 42 cases were not treated with any intraoperative coadjuva…

MaleVascular Endothelial Growth Factor ATriamcinolone acetonideVisual acuitygenetic structuresmedicine.medical_treatmentExtração de catarataVisual AcuityIntraocular lensCuidados intraoperatóriosAngiogenesis InhibitorsTriamcinolonelcsh:OphthalmologyLens Implantation IntraocularDiabetic retinopathyAntibodies monoclonalAged 80 and overGeneral MedicineDiabetic retinopathyMiddle AgedMulticenter studyBevacizumabTreatment OutcomeCataract extractionChemotherapy AdjuvantEstudo multicêntricoIntravitreal InjectionsFemalemedicine.symptommedicine.drugAdultmedicine.medical_specialtyBevacizumabAntibodies Monoclonal HumanizedCataractMacular EdemaIntraoperative careOphthalmologyEdema macularmedicineAnticorpos monoclonaisHumansMacular edemaGlucocorticoidsAgedRetrospective StudiesMacular edemaDiabetic RetinopathyIntraoperative CarePhacoemulsificationbusiness.industryRetinopatia diabéticaPhacoemulsificationCataract surgeryFacoemulsificaçãomedicine.diseaseSurgeryImplante de lente intraocularOphthalmologyLens implantation intraocularlcsh:RE1-994businessFollow-Up StudiesArquivos brasileiros de oftalmologia
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A randomized trial of intravitreal bevacizumab vs. ranibizumab for myopic CNV.

2014

AIMS: The aim was to compare the efficacy of intravitreal therapy with bevacizumab and ranibizumab for choroidal neovascularization (CNV) in pathologic myopia (PM). METHODS: This was a prospective multicenter randomized nonblinded trial. RESULTS: In seven centers, 78 eyes were randomized 1:1 to treatment with bevacizumab (group B, 40 eyes) or ranibizumab (group R, 38 eyes) given with an "on demand" regimen (PRN). The mean follow-up was 19 months (SD 2, range 12-24). The mean BCVA at baseline was 0.60 logMAR (20/80 Snellen equivalent, Seq) and 50 letter score (ls). Mean final BCVA was 0.51 LogMAR (20/63 Seq) and 57 ls (p = 0.0009 and p = 0.0002, respectively). In group B, mean basal BCVA was…

MaleVascular Endothelial Growth Factor AVisual Acuity/drug effectsVisual acuitygenetic structuresVisual AcuityAngiogenesis Inhibitorslaw.inventionBevacizumab/therapeutic use0302 clinical medicineRandomized controlled triallawMyopiaMedicineProspective StudiesProspective cohort studyPathological myopiaAged 80 and overMiddle AgedSensory SystemsBevacizumabVascular endothelial growth factor AChoroidal neovascularizationIntravitreal InjectionsMyopia DegenerativeFemalemedicine.symptommedicine.drugAdultmedicine.medical_specialtyBevacizumabNeuroscience(all)CNVBevacizumab; CNV; Pathological myopia; Ranibizumab.Antibodies Monoclonal HumanizedRanibizumab/therapeutic use03 medical and health sciencesCellular and Molecular NeuroscienceOphthalmologyRanibizumabVascular Endothelial Growth Factor A/antagonists & inhibitorsHumansAngiogenesis Inhibitors/therapeutic useIntravitreal bevacizumabAgedpathological myopia CNV bevacizumab ranibizumabSettore MED/30 - Malattie Apparato Visivobusiness.industryTherapeutic effectChoroidal Neovascularization/drug therapyeye diseasesChoroidal NeovascularizationOphthalmologyRegimen030221 ophthalmology & optometryMyopia Degenerative/drug therapysense organsRanibizumabbusiness030217 neurology & neurosurgeryFollow-Up StudiesGraefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie
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Assessment of intravitreal anti-VEGF drugs and dexamethasone for retinal diseases in real world setting: A multi-centre prospective study from Southe…

2022

Describe drug utilisation and clinical outcomes of intravitreal anti-VEGF drug and dexamethasone use in the real-world setting in Southern Italy using data from multi-centre study of retinal disease. Clinical data of retinal disease patients treated with anti-VEGF drugs and dexamethasone implant in 6 out-patient ophthalmology centres from Southern Italy were collected by means of an electronic case report form. Patients receiving at least one intravitreal injection/implant of the study drugs were followed for up to two years and described in terms of demographics and clinical characteristics. Drug utilisation patterns were described. A sign-rank test was used to compare clinical data on vi…

MaleVascular Endothelial Growth Factor Agenetic structuresPharmacology &ltPHARMACOLOGY diabetic macular edema &ltbiostatisticsAngiogenesis InhibitorsDexamethasoneMacular DegenerationCATARACTRetinal DiseasesRanibizumabRetinal Vein OcclusionHumansProspective StudiesRETINAAgedAged 80 and overPharmacologySettore MED/30 - Malattie Apparato Visivopathologic myopiaGeneral MedicineMiddle AgedBevacizumabOphthalmologyLENSRETINA epidemiology / biostatistics pathologic myopia retina - medical therapies &ltIntravitreal InjectionsPharmacology diabetic macular edema RETINA epidemiology biostatisticsLENSCATARACTpathologic myopiaFemaleepidemiologydiabetic macular edemaEuropean Journal of Ophthalmology
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