Search results for "Indazoles"

showing 4 items of 44 documents

Cisplatin and epirubicin plus oral lonidamine as first-line treatment for metastatic breast cancer: A phase II study of the Southern Italy Oncology G…

1998

Lonidamine (LND) is a unique antineoplastic drug derived from indazole-3-carboxylic acid which inhibits oxygen consumption and aerobic glycolysis, interfering with energy metabolism of neoplastic cells. LND has been experimentally shown to potentiate the cytotoxic effects of epirubicin (EPI) in human breast cancer cell lines, cisplatin activity in both platinum-sensitive and -resistant human ovarian carcinoma cell lines, and EPI antineoplastic activity in some recent phase III trials carried out in advanced breast cancer. A multicenter phase II trial was carried out with the combination of cisplatin 60 mg/m2, EPI 100 mg/m2 and LND 450 mg/day p.o. in three refracted doses/day starting 2 days…

OncologyAdultCancer Researchmedicine.medical_specialtyIndazolesmedicine.medical_treatmentPhases of clinical researchAdministration OralBreast NeoplasmsDrug Administration Schedulechemistry.chemical_compoundBreast cancerInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansPharmacology (medical)Neoplasm MetastasisAgedEpirubicinPharmacologyChemotherapybusiness.industryLonidamineCancerMiddle Agedmedicine.diseaseMetastatic breast cancerOncologychemistryFemaleCisplatinbusinessProgressive diseaseEpirubicinmedicine.drug
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Selective electrochemical discrimination between dopamine and phenethylamine-derived psychotropic drugs using electrodes modified with an acyclic rec…

2010

Electrochemical discrimination between dopamine and psychotropic drugs which have in common a skeletal structure of phenethylamine, can be obtained using acyclic receptors L(1) and L(2), containing two terminal 3-alkoxy-5-nitroindazole rings. Upon attachment to graphite electrodes, L(1) and L(2) exhibit a well-defined, essentially reversible solid state electrochemistry in contact with aqueous media, based on electrolyte-assisted reduction processes involving successive cation and anion insertion/binding. As a result, a distinctive, essentially Nernstian electrochemical response is obtained for phenethylammonium ions of methamphetamine (METH), p-methoxyamphetamine (PMA), amphetamine (AMPH),…

PhenethylamineIndazolesStereochemistryDopamineMescalineElectrochemistryBiochemistryMedicinal chemistryAnalytical ChemistryMethamphetaminechemistry.chemical_compoundDopaminePhenethylaminesElectrochemistrymedicineEnvironmental ChemistryAmphetamineElectrodesSpectroscopyMescalinePsychotropic DrugsAmphetaminesMeth-Electrochemical TechniquesMethamphetamineCarbonAmphetaminechemistryAlkoxy groupmedicine.drugThe Analyst
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Entrectinib: a potent new TRK, ROS1, and ALK inhibitor

2015

Abstract: Introduction: Receptor tyrosine kinases (RTKs) and their signaling pathways, control normal cellular processes; however, their deregulation play important roles in malignant transformation. In advanced non-small cell lung cancer (NSCLC), the recognition of oncogenic activation of specific RTKs, has led to the development of molecularly targeted agents that only benefit roughly 20% of patients. Entrectinib is a pan-TRK, ROS1 and ALK inhibitor that has shown potent anti-neoplastic activity and tolerability in various neoplastic conditions, particularly NSCLC. Areas covered: This review outlines the pharmacokinetics, pharmacodynamics, mechanism of action, safety, tolerability, pre-cl…

Receptor Protein-Tyrosine KinasesEntrectinibNTRK1NTRK2NTRK3Receptor tyrosine kinaseEntrectinibMalignant transformationAntineoplastic AgentNeoplasmsProtein-Tyrosine KinaseALK; colorectal cancer; Entrectinib; non-small cell lung cancer; NTRK1; NTRK2; NTRK3; precision medicine; ROS1; salivary gland cancer; TrkA; TrkB; TrkC; Animals; Antineoplastic Agents; Benzamides; Humans; Indazoles; Neoplasms; Protein-Tyrosine Kinases; Proto-Oncogene Proteins; Receptor Protein-Tyrosine Kinases; Receptor; trkA; Receptor; trkB; Receptor; trkC; Pharmacology; Pharmacology (medical)Anaplastic Lymphoma KinasePharmacology (medical)salivary gland cancerProto-Oncogene ProteinbiologyTrkAPharmacology. TherapyTrkCTrkBGeneral MedicineProtein-Tyrosine KinasesReceptor Protein-Tyrosine KinaseBenzamidesmedicine.symptomROS1ReceptorHumanIndazolesmedicine.drug_classprecision medicineAntineoplastic Agentscolorectal cancerBenzamideProto-Oncogene ProteinsmedicineROS1AnimalsHumansReceptor trkBReceptor trkCReceptor trkAnon-small cell lung cancerPharmacologyAnimalReceptor Protein-Tyrosine KinasesALK inhibitorIndazoleMechanism of actionALKTrk receptorbiology.proteinCancer researchNeoplasmALK; colorectal cancer; Entrectinib; non-small cell lung cancer; NTRK1; NTRK2; NTRK3; precision medicine; ROS1; salivary gland cancer; TrkA; TrkB; TrkC; Animals; Antineoplastic Agents; Benzamides; Humans; Indazoles; Neoplasms; Protein-Tyrosine Kinases; Proto-Oncogene Proteins; Receptor Protein-Tyrosine Kinases; Receptor trkA; Receptor trkB; Receptor trkC; Pharmacology; Pharmacology (medical)Expert Opinion on Investigational Drugs
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Psychophysical and electrofunctional contrast sensitivity in cataractous patients treated with bendazac-lysine salt

1990

The clinical progression of the cataract may be influenced by drugs which reduce the denaturation of lens proteins. One of the most promising drugs is the bendazac-lysine salt. The drug was used in a double-blind study of a group of patients with initial cortical cataract in order to evaluate the changes in visual acuity and contrast sensitivity by means of a psychophysical and an electrophysiological method. After 6 months of treatment with bendazac the mean values of visual acuity showed a statistically significant increase in respect to baseline values, as well as an improvement of the threshold of contrast for most spatial frequencies. In the eyes treated with placebo there was no stati…

medicine.medical_specialtyIndazolesVisual acuitygenetic structuresEye diseasemedia_common.quotation_subjectVisual AcuityPlaceboCataractContrast SensitivityLens proteinDouble-Blind MethodOral administrationPhysiology (medical)OphthalmologyBendazacPsychophysicsmedicineHumansContrast (vision)media_commonbusiness.industryAnti-Inflammatory Agents Non-Steroidalmedicine.diseaseeye diseasesSensory SystemsSurgeryElectrophysiologyOphthalmologyElectrophysiologyEvoked Potentials Visualmedicine.symptombusinessPhotic Stimulationmedicine.drugDocumenta Ophthalmologica
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