Search results for "Deoxycytidine"

showing 10 items of 98 documents

Low density lipoproteins and human serum albumin as the carriers of squalenoylated drugs: insights from molecular simulations

2018

We have studied the interaction of three clinically promising squalenoylated drugs (gemcitabine-squalene, adenine-squalene, and doxorubicin-squalene) with low-density lipoproteins (LDL) by means of atomistic molecular dynamics simulations. It is shown that all studied squalenoylated drugs accumulate inside the LDL particles. This effect is promoted by the squalene moiety, which acts as an anchor and drives the hydrophilic drugs into the hydrophobic core of the LDL lipid droplet. Our data suggest that LDL particles could be a universal carriers of squalenoylated drugs in the bloodstream. Interaction of gemcitabine-squalene with human serum albumin (HSA) was also studied by ensemble of dockin…

Squalene[PHYS.PHYS.PHYS-BIO-PH]Physics [physics]/Physics [physics]/Biological Physics [physics.bio-ph]Drug CompoundingPharmaceutical ScienceSerum Albumin Human02 engineering and technologyPlasma protein bindingMolecular Dynamics Simulation010402 general chemistry01 natural sciencesMolecular Docking SimulationDeoxycytidineSqualenechemistry.chemical_compound[ PHYS.PHYS.PHYS-BIO-PH ] Physics [physics]/Physics [physics]/Biological Physics [physics.bio-ph]Lipid dropletDrug DiscoverymedicineMoietyHumansComputingMilieux_MISCELLANEOUSDrug CarriersBinding SitesAdenine[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences021001 nanoscience & nanotechnologyHuman serum albuminGemcitabine3. Good health0104 chemical sciences[CHIM.THEO]Chemical Sciences/Theoretical and/or physical chemistryLipoproteins LDLMolecular Docking Simulation[ SDV.SP ] Life Sciences [q-bio]/Pharmaceutical scienceschemistryDocking (molecular)Doxorubicin[ CHIM.THEO ] Chemical Sciences/Theoretical and/or physical chemistryBiophysicsMolecular MedicineNanoparticles0210 nano-technologyDrug carrierHydrophobic and Hydrophilic Interactionsmedicine.drugProtein Binding
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Role of a 48-week pegylated interferon therapy in hepatitis B e antigen positive HIV-co-infected patients on cART including tenofovir: EMVIPEG study.

2014

In hepatitis B e antigen (HBeAg) positive-HIV co-infected patients treated with combined antiretroviral therapy (cART), including tenofovir disoproxil fumarate (TDF), the rate of HBe seroconversion remains low. Whether adding pegylated interferon alfa (PegIFN) could increase the likelihood of HBeAg loss and HBe seroconversion has not been assessed.A 48-week PegIFN therapy was added to HBeAg positive-HIV co-infected patients on TDF and emtricitabine, or lamivudine for at least 6 months. The primary endpoint was HBV sustained response: HBe seroconversion with undetectable HBV DNA levels 24 weeks after completing PegIFN therapy (W72).Fifty-one patients (49 men, median age 46 years, range: 32-6…

AdultMalemedicine.medical_specialtyHBsAgOrganophosphonatesHIV Infectionsmedicine.disease_causeEmtricitabineGastroenterologyAntiviral AgentsDeoxycytidinePolyethylene GlycolsHepatitis B ChronicPegylated interferonInternal medicineAntiretroviral Therapy Highly ActivemedicineEmtricitabineHumansHepatitis B e AntigensSeroconversionTenofovirHepatitis B virusDrug CarriersHepatologybusiness.industryCoinfectionAdeninevirus diseasesLamivudineHIVInterferon-alphaMiddle AgedViral Loaddigestive system diseasesRecombinant ProteinsCD4 Lymphocyte CountTreatment OutcomeHBeAgLamivudineImmunologyFemalebusinessViral loadmedicine.drugJournal of hepatology
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Bevacizumab efficacy in metastatic colorectal cancer is dependent on primary tumor resection.

2014

Purpose Bevacizumab plus fluoropyrimidine-based chemotherapy is standard treatment for first-line and second-line metastatic colorectal cancer (mCRC). However, to date, there is no current biomarker predictive for the benefit of bevacizumab use for these patients. Preclinical data suggest that the presence of the primary tumor could be involved in less efficient antitumor activity of antiangiogenic agents, but no clinical data currently support this hypothesis. Methods We performed a retrospective analysis of factors associated with overall survival (OS) in a study cohort of 409 mCRC patients. Univariate and multivariate Cox proportional hazard regression models were used to assess the infl…

OncologyAdultMalemedicine.medical_specialtyBevacizumabOrganoplatinum CompoundsColorectal cancerAdenocarcinomaAntibodies Monoclonal HumanizedIrinotecanDeoxycytidineCapecitabineSurgical oncologyInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansProspective StudiesNeoplasm MetastasisSurvival rateCapecitabineAgedNeoplasm StagingRetrospective StudiesAged 80 and overColorectal Cancerbusiness.industryMiddle Agedmedicine.diseasePrognosisPrimary tumorCombined Modality TherapyBevacizumabOxaliplatinSurvival RateOncologyAdenocarcinomaBiomarker (medicine)SurgeryCamptothecinFemaleFluorouracilbusinessColorectal Neoplasmsmedicine.drugFollow-Up StudiesAnnals of surgical oncology
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PML as a potential predictive factor of oxaliplatin/fluoropyrimidine-based first line chemotherapy efficacy in colorectal cancer patients

2012

PML regulates a wide range of pathways involved in tumorigenesis, such as apoptosis, which is also one of the main mechanisms through which oxaliplatin and fluoropyrimidine exert their antineoplastic activity. The present study aims to investigate PML expression as a predictive factor of oxaliplatin/fluoropyrimidine therapy efficacy. Seventy-four metastatic colorectal cancer patients who received oxaliplatin/floropyrimidine-based first line therapy have been included in this retrospective study. PML expression was assessed by immunohistochemistry. PML down-regulation was detected in 39 (52.7%) patients (14 complete and 25 partial PML loss). RR was significantly lower (25.6%) in patients wit…

OncologyMaleOrganoplatinum CompoundsOxaloacetatesPhysiologyColorectal cancerSettore MED/06 - Oncologia MedicavirusesClinical BiochemistryCellLeucovorinPromyelocytic Leukemia Proteinmedicine.disease_causeDeoxycytidineAntineoplastic Combined Chemotherapy Protocolsbiologyvirus diseasesNuclear ProteinsMiddle AgedOxaliplatinSurvival Ratemedicine.anatomical_structureImmunohistochemistryoxaliplatin/fluoropyrimidineFemaleFluorouracilColorectal Neoplasmsmedicine.drugAdultmedicine.medical_specialtyAntimetabolites AntineoplasticPML; oxaliplatin/fluoropyrimidine; colorectal cancerAntineoplastic Agentscolorectal cancerPromyelocytic leukemia proteinPredictive Value of TestsInternal medicinemedicineHumansCapecitabineAgedRetrospective StudiesPMLbusiness.industryTumor Suppressor ProteinsRetrospective cohort studyCell Biologymedicine.diseaseOxaliplatinApoptosisDrug Resistance Neoplasmbiology.proteinCarcinogenesisbusinessTranscription Factors
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Differential Effects of Tenofovir/Emtricitabine and Abacavir/Lamivudine on Human Leukocyte Recruitment

2012

Background The association of abacavir (ABC) with cardiovascular disease has led to HIV treatment guidelines favouring the combination of tenofovir/emtricitabine (TDF/FTC) over that of ABC/lamivudine (ABC/3TC). We have analysed the effects of plasma-relevant concentrations of TDF, FTC, ABC and 3TC, individually and in clinically employed combinations, on human leukocyte accumulation. The effects of ABC, 3TC, TDF and FTC on the expression of adhesion molecules were also evaluated. Methods Interactions between human leukocytes – specifically peripheral blood polymorphonuclear or mono-nuclear cells – and human umbilical vein endothelial cells were evaluated in a flow chamber reproducing in viv…

OrganophosphonatesHIV InfectionsCD18Cell CommunicationPharmacologyEmtricitabineDeoxycytidinePeripheral blood mononuclear cellIn vivoAbacavirAntiretroviral Therapy Highly ActiveCell AdhesionLeukocytesmedicineEmtricitabineHumansPharmacology (medical)TenofovirPharmacologyCell adhesion moleculebusiness.industryAdenineEndothelial CellsLamivudineAbacavir/LamivudineDideoxynucleosidesDrug CombinationsInfectious DiseasesLamivudinebusinessCell Adhesion Moleculesmedicine.drugAntiviral Therapy
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Paclitaxel, carboplatin and gemcitabine combination as induction chemotherapy for stage IIIA N2 bulky non-small cell lung cancer

2005

<i>Background:</i> Induction chemotherapy followed by surgical resection or definitive radiotherapy for patients affected by stage IIIA N2 bulky non-small cell lung cancer (NSCLC) has been investigated in several trials. <i>Patients and Methods:</i> In this present study, 52 patients with stage IIIA N2 bulky NSCLC with cytologically or histologically confirmed mediastinal lymph node involvement received paclitaxel 175 mg/mq on day 1, carboplatin AUC 5 on day 1 and gemcitabine 1,000 mg/mq on day 1 and 8 every 3 weeks for three cycles as induction chemotherapy. <i>Results:</i> Objective response (4 complete remission and 36 partial remission) was achieved i…

AdultMaleOncologyCancer Researchmedicine.medical_specialtyLung NeoplasmsPaclitaxelmedicine.drug_classmedicine.medical_treatmentDeoxycytidineAntimetaboliteDisease-Free SurvivalDrug Administration ScheduleCarboplatinchemistry.chemical_compoundCarcinoma Non-Small-Cell LungInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansLung cancerAgedNeoplasm StagingChemotherapybusiness.industryRemission InductionInduction chemotherapyLung cancer Paclitaxel Carboplatin stage III ChemotherapyGeneral MedicineMiddle Agedmedicine.diseaseSurvival AnalysisGemcitabineGemcitabineCarboplatinrespiratory tract diseasesSurgeryRadiation therapyTreatment OutcomeOncologychemistryPaclitaxelChemotherapy AdjuvantFemaleRadiotherapy Adjuvantbusinessmedicine.drug
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Oxaliplatin and Capecitabine-Based Chemoradiotherapy for Gastric Cancer—An Extended Phase I MARGIT and AIO Trial

2008

Purpose Adjuvant 5-fluorouracil–based chemoradiotherapy has been shown to improve the prognosis of gastric cancer. To optimize these results, in the present study oxaliplatin and capecitabine were used instead of 5-fluorouracil. We sought to determine the maximum tolerated dose and the dose-limiting toxicities (DLT) of these drugs in combination with intensity-modulated radiotherapy. Methods and Materials Patients with resected adenocarcinoma of the stomach or the gastroesophageal junction were included. They received two cycles of induction chemotherapy (oxaliplatin and capecitabine [XelOx] regimen). Using standard Phase I methodology, patients received 45 Gy in 1.8-Gy fractions either in …

MaleOncologyCancer Researchmedicine.medical_specialtyOrganoplatinum CompoundsNauseamedicine.medical_treatmentDeoxycytidineGastroenterologyCapecitabineLeukocytopeniaStomach NeoplasmsInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansRadiology Nuclear Medicine and imagingCapecitabineAgedChemotherapyRadiationbusiness.industryInduction chemotherapyMiddle AgedCombined Modality TherapyOxaliplatinOxaliplatinRegimenOncologyFemaleRadiotherapy AdjuvantFluorouracilmedicine.symptombusinessChemoradiotherapymedicine.drugInternational Journal of Radiation Oncology*Biology*Physics
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Phase I-II trial of gemcitabine-based first-line chemotherapies for small cell lung cancer in elderly patients with performance status 0-2: the G-STE…

2011

Introduction: Treatment of elderly patients with small cell lung cancer (SCLC) is based on scanty evidence. Methods: Patients with extensive SCLC, age >70 years, and performance status 0-2 were eligible for a study looking for optimal two-drug combination of gemcitabine (Gem) with vinorelbine (Vin), etoposide (Eto), cisplatin (Cis), or carboplatin (Car). Gemcitabine dose was the same (1000 mg/m2, days 1-8) in all combinations. A two-stage minimax flexible design for response was applied to GemVin combination (Vin 25 mg/m2, days 1-8). For GemCar, GemCis, GemEto, a phase I-II Bayesian design was applied, looking for the optimal dose of the partner drugs. Objective response rate ≥60% and un…

OncologyMaleLung NeoplasmsDeoxycytidineCarboplatinchemistry.chemical_compoundElderlyAntineoplastic Combined Chemotherapy Protocols80 and overCarcinoma Small CellMultivariate AnalysiEtoposideEtoposidePlatinum compoundsAged 80 and overArea under the curveSCLCVinorelbinePrognosisElderly; Etoposide; Gemcitabine; Platinum compounds; SCLC; Vinorelbine; Aged; Aged 80 and over; Antineoplastic Combined Chemotherapy Protocols; Carboplatin; Carcinoma Small Cell; Cisplatin; Deoxycytidine; Disease-Free Survival; Etoposide; Female; Humans; Lung Neoplasms; Male; Multivariate Analysis; Prognosis; Proportional Hazards Models; Quality of Life; Treatment Outcome; Vinblastine; VinorelbineTreatment OutcomeOncologyPlatinum compoundToxicityFemalemedicine.drugHumanPulmonary and Respiratory Medicinemedicine.medical_specialtyPrognosiVinorelbineVinblastineDisease-Free SurvivalInternal medicinemedicineHumansAgedProportional Hazards ModelsCisplatinAntineoplastic Combined Chemotherapy ProtocolPerformance statusbusiness.industryCarcinomaSmall CellGemcitabineGemcitabineCarboplatinSurgeryLung NeoplasmchemistryMultivariate AnalysisProportional Hazards ModelQuality of LifeCisplatinbusiness
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Gemcitabine, oxaliplatin, levofolinate, 5-fluorouracil, granulocyte-macrophage colony-stimulating factor, and interleukin-2 (GOLFIG) versus FOLFOX ch…

2013

The GOLFIG-2 phase III trial was designed to compare the immunobiological activity and antitumor efficacy of GOLFIG chemoimmunotherapy regimen with standard FOLFOX-4 chemotherapy in frontline treatment of metastatic colorectal cancer (mCRC) patients. This trial was conceived on the basis of previous evidence of antitumor and immunomodulating activity of the GOLFIG regimen in mCRC. GOLFIG-2 is a multicentric open/ label phase III trial (EUDRACT: 2005-003458-81). Chemo-naive mCRC patients were randomized in a 1:1 ratio to receive biweekly standard FOLFOX-4 or GOLFIG [gemcitabine (1000 mg/m 2, day 1); oxaliplatin (85 mg/m2, day 2); levofolinate (100 mg/m2, days 1-2), 5-fluorouracil (5-FU) (400…

OncologyMaleCancer ResearchGranulocyte-macrophage-colonystimulating- factorOrganoplatinum Compoundsmedicine.medical_treatmentLeucovorinColorectal NeoplasmGastroenterologyDeoxycytidineFOLFOXAldesleukinPhase iii trialAntineoplastic Combined Chemotherapy ProtocolsImmunology and AllergyMedicineChemoimmunotherapyNeoplasm MetastasisAged 80 and overAldesleukinMiddle AgedNeoplasm MetastasiOxaliplatinColorectal carcinomaTreatment OutcomeFluorouracilFemaleFluorouracilColorectal NeoplasmsHumanmedicine.drugAdultmedicine.medical_specialtyImmunologyLymphocytes Tumor-InfiltratingChemoimmunotherapyInternal medicineHumansAgedPharmacologyChemotherapyAntineoplastic Combined Chemotherapy Protocolbusiness.industryOrganoplatinum CompoundGranulocyte-Macrophage Colony-Stimulating FactorGemcitabineGemcitabineOxaliplatinRegimenInterleukin-2Neoplasm GradingbusinessJournal of immunotherapy (Hagerstown, Md. : 1997)
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Curvature increases permeability of the plasma membrane for ions, water and the anti-cancer drugs cisplatin and gemcitabine

2019

ABSTRACTIn this work the permeability of a model asymmetric plasma membrane, for ions, water and the anti-cancer drugs cisplatin and gemcitabine is studied by means of all-atom molecular dynamics simulations. It is shown that permeability of the membranes increases from one to three orders of magnitude upon membrane bending depending on the compound and the sign of curvature. Our results show that the membrane curvature is an important factor which should be considered during evaluation of drug translocation.TOC GRAPHICS

Cell Membrane PermeabilityLipid Bilayerslcsh:MedicineAntineoplastic AgentsMolecular Dynamics SimulationCurvature01 natural sciencesDeoxycytidineArticleSupramolecular assemblyIonMembrane bending03 medical and health sciencesComputational biophysics0103 physical sciencesmedicineAnimalsHumanslcsh:Science030304 developmental biologyCisplatinIons0303 health sciences010304 chemical physicsChemistryCell Membranelcsh:RWaterMembrane structure and assemblyGemcitabineOrders of magnitude (mass)MembraneMembrane curvaturePermeability (electromagnetism)Drug deliveryBiophysicslcsh:QCisplatinmedicine.drugScientific Reports
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