2023
An oral androgen receptor RIPTAC for prostate cancer.
Raina K, Eastman K, Yu X, Forbes C, Jones K, Mousseau J, Li H, Kayser-Bricker K, Crews C. An oral androgen receptor RIPTAC for prostate cancer. Journal Of Clinical Oncology 2023, 41: 184-184. DOI: 10.1200/jco.2023.41.6_suppl.184.Peer-Reviewed Original ResearchPCa cell linesAR expressionProstate cancerAR-positive cellsCastration-resistant settingLow oral doseProstate cancer modelTumor growth inhibitionProstate cancer cellsCell linesEfficacious exposureVCaP xenograftsOral dosePreclinical dataOral dosingLow nM concentrationsTumor-specific inhibitionCancer modelPharmacokinetic propertiesNormal tissuesOral bioavailabilitySignaling InhibitorsToxicology studiesAR geneCancer cells
2019
A single‐center, open‐label positron emission tomography study to evaluate brivaracetam and levetiracetam synaptic vesicle glycoprotein 2A binding in healthy volunteers
Finnema SJ, Rossano S, Naganawa M, Henry S, Gao H, Pracitto R, Maguire RP, Mercier J, Kervyn S, Nicolas J, Klitgaard H, DeBruyn S, Otoul C, Martin P, Muglia P, Matuskey D, Nabulsi NB, Huang Y, Kaminski RM, Hannestad J, Stockis A, Carson RE. A single‐center, open‐label positron emission tomography study to evaluate brivaracetam and levetiracetam synaptic vesicle glycoprotein 2A binding in healthy volunteers. Epilepsia 2019, 60: 958-967. PMID: 30924924, PMCID: PMC6532410, DOI: 10.1111/epi.14701.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralAnticonvulsantsCarbon RadioisotopesFemaleHealthy VolunteersHumansInhibitory Concentration 50Injections, IntravenousLevetiracetamMagnetic Resonance ImagingMaleMembrane GlycoproteinsNerve Tissue ProteinsNeuroimagingPositron-Emission TomographyProtein BindingPyrrolidinonesConceptsSynaptic vesicle glycoprotein 2AIntravenous brivaracetamHours postdoseBrain penetrationHealthy volunteersDaily oral dosingPositron emission tomography studyFurther clinical studiesEmission tomography studiesPlasma concentration relationshipPositron emission tomography (PET) tracerEmission tomography tracerVivo animal studiesAcute seizuresAntiepileptic drugsTherapeutic dosesCohort 2Oral dosingCohort 1Clinical studiesCohort 3LevetiracetamAnimal studiesRelevant dosesBrivaracetam
2015
Brivaracetam, a selective high‐affinity synaptic vesicle protein 2A (SV2A) ligand with preclinical evidence of high brain permeability and fast onset of action
Nicolas JM, Hannestad J, Holden D, Kervyn S, Nabulsi N, Tytgat D, Huang Y, Chanteux H, Staelens L, Matagne A, Mathy FX, Mercier J, Stockis A, Carson RE, Klitgaard H. Brivaracetam, a selective high‐affinity synaptic vesicle protein 2A (SV2A) ligand with preclinical evidence of high brain permeability and fast onset of action. Epilepsia 2015, 57: 201-209. PMID: 26663401, DOI: 10.1111/epi.13267.Peer-Reviewed Original ResearchConceptsFaster onsetAcute seizuresHigh-affinity synaptic vesicle protein 2A ligandNonhuman primate PET studyAudiogenic seizure miceRapid brain entryOnset of actionSingle oral dosingHigh brain permeabilityBlood-brain barrier permeability (BBBP) valuesPrimate PET studyAudiogenic miceBrain entryCaco-2 cellsSeizure micePreclinical evidenceAntiepileptic drugsSusceptible miceBrain levelsBrain penetrationPreclinical dataBrain kineticsOral dosingSingle dosingClinical studiesPhase II study of tivantinib (ARQ 197) in patients with metastatic triple-negative breast cancer
Tolaney SM, Tan S, Guo H, Barry W, Van Allen E, Wagle N, Brock J, Larrabee K, Paweletz C, Ivanova E, Janne P, Overmoyer B, Wright JJ, Shapiro GI, Winer EP, Krop IE. Phase II study of tivantinib (ARQ 197) in patients with metastatic triple-negative breast cancer. Investigational New Drugs 2015, 33: 1108-1114. PMID: 26123926, PMCID: PMC4608248, DOI: 10.1007/s10637-015-0269-8.Peer-Reviewed Original ResearchConceptsMetastatic triple-negative breast cancerTriple-negative breast cancerPhase 2 studyProgression-free survivalBreast cancerPartial responseSingle-arm phase 2 studyResults 22 patientsPhase II studyDaily oral dosingOverall response rateRecent preclinical dataMechanism of actionTivantinib monotherapyMetastatic settingAdverse eventsII studyMethods PatientsPrior linesPreclinical dataOral dosingTivantinibPatientsMET expressionResponse rate
2012
Rapid Evaluation in Whole Blood Culture of Regimens for XDR-TB Containing PNU-100480 (Sutezolid), TMC207, PA-824, SQ109, and Pyrazinamide
Wallis RS, Jakubiec W, Mitton-Fry M, Ladutko L, Campbell S, Paige D, Silvia A, Miller PF. Rapid Evaluation in Whole Blood Culture of Regimens for XDR-TB Containing PNU-100480 (Sutezolid), TMC207, PA-824, SQ109, and Pyrazinamide. PLOS ONE 2012, 7: e30479. PMID: 22279595, PMCID: PMC3261206, DOI: 10.1371/journal.pone.0030479.Peer-Reviewed Original ResearchMeSH KeywordsAdamantaneAntitubercular AgentsDiarylquinolinesDrug MonitoringDrug Therapy, CombinationEthylenediaminesExtensively Drug-Resistant TuberculosisHumansMicrobial Sensitivity TestsMycobacterium tuberculosisNitroimidazolesOxazolidinonesPyrazinamideQuinolinesReproducibility of ResultsTime FactorsConceptsPNU-100480Whole blood culturesPA-824Blood culturesWhole-blood bactericidal activityBactericidal activityStandard TB therapyDihydroxy vitamin DIntracellular M. tuberculosisBlood bactericidal activityCumulative activityPZA-resistant strainsHigh therapeutic concentrationsActive regimensTB regimensNew regimensTB therapyVitamin DOral dosingTherapeutic concentrationsDrug combinationsPharmacokinetic dataRegimensIndividual drugsTMC207
2010
A phase I pharmacokinetic study of pulse-dose vorinostat with flavopiridol in solid tumors
Dickson MA, Rathkopf DE, Carvajal RD, Grant S, Roberts JD, Reid JM, Ames MM, McGovern RM, Lefkowitz RA, Gonen M, Cane LM, Dials HJ, Schwartz GK. A phase I pharmacokinetic study of pulse-dose vorinostat with flavopiridol in solid tumors. Investigational New Drugs 2010, 29: 1004-1012. PMID: 20461440, PMCID: PMC3545439, DOI: 10.1007/s10637-010-9447-x.Peer-Reviewed Original ResearchConceptsSerum levelsPhase I pharmacokinetic studyIntermittent high doseResults 34 patientsD1-3I pharmacokinetic studyCyclin-dependent kinase inhibitor flavopiridolKinase inhibitor flavopiridolStable diseaseOral doseOral dosingHigh doseCombination treatmentPatientsSolid tumorsCmaxOne weekDosePharmacokinetic studyVorinostatMTDFlavopiridolNeutropeniaChemotherapyLevels
2008
Intragastric pH With Oral vs Intravenous Bolus Plus Infusion Proton-Pump Inhibitor Therapy in Patients With Bleeding Ulcers
Laine L, Shah A, Bemanian S. Intragastric pH With Oral vs Intravenous Bolus Plus Infusion Proton-Pump Inhibitor Therapy in Patients With Bleeding Ulcers. Gastroenterology 2008, 134: 1836-1841. PMID: 18423628, DOI: 10.1053/j.gastro.2008.03.006.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralDrug Administration ScheduleDuodenal UlcerDuodenoscopyFemaleGastric AcidGastric Acidity DeterminationGastroscopyHumansHydrogen-Ion ConcentrationInfusions, IntravenousMaleMiddle AgedPeptic Ulcer HemorrhageProton Pump InhibitorsStomach UlcerTime FactorsTreatment OutcomeConceptsProton pump inhibitor therapyOral PPIIntravenous PPIInhibitor therapyConfidence intervalsStudy periodFrequent oral dosingHigh-risk stigmataSimilar antisecretory effectIntravenous lansoprazoleOral lansoprazolePPI therapyAntisecretory effectWide confidence intervalsIntragastric pHIntravenous bolusBleeding ulcersOral dosingPatientsBaseline pHUlcersAbstractTextTherapyAIMSBolus
2006
Effect of frequent dosing of an oral proton pump inhibitor on intragastric pH
PAIS SA, NATHWANI RA, DHAR V, NOWAIN A, LAINE L. Effect of frequent dosing of an oral proton pump inhibitor on intragastric pH. Alimentary Pharmacology & Therapeutics 2006, 23: 1607-1613. PMID: 16696810, DOI: 10.1111/j.1365-2036.2006.02933.x.Peer-Reviewed Original ResearchConceptsProton pump inhibitorsPump inhibitorsOral proton pump inhibitorsDoses of lansoprazoleFrequent oral dosingLansoprazole plasma concentrationHelicobacter pylori statusCYP2C19 statusOral lansoprazolePylori statusOvernight fastOral dosingPlasma concentrationsFrequent dosingHealthy volunteersClot formationTime pointsLansoprazoleMean proportionDosingInhibitorsSubjectsStatusPatientsPeriod
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