2017
18F-Fluoroestradiol PET/CT Measurement of Estrogen Receptor Suppression during a Phase I Trial of the Novel Estrogen Receptor-Targeted Therapeutic GDC-0810: Using an Imaging Biomarker to Guide Drug Dosage in Subsequent Trials
Wang Y, Ayres KL, Goldman DA, Dickler MN, Bardia A, Mayer IA, Winer E, Fredrickson J, Arteaga CL, Baselga J, Manning HC, Mahmood U, Ulaner GA. 18F-Fluoroestradiol PET/CT Measurement of Estrogen Receptor Suppression during a Phase I Trial of the Novel Estrogen Receptor-Targeted Therapeutic GDC-0810: Using an Imaging Biomarker to Guide Drug Dosage in Subsequent Trials. Clinical Cancer Research 2017, 23: 3053-3060. PMID: 28011460, PMCID: PMC5474190, DOI: 10.1158/1078-0432.ccr-16-2197.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedBiomarkers, PharmacologicalBreast NeoplasmsCinnamatesDose-Response Relationship, DrugEstradiolEstrogen Receptor alphaFemaleFulvestrantHumansIndazolesMiddle AgedMolecular ImagingMolecular Targeted TherapyPositron Emission Tomography Computed TomographyReceptors, EstrogenTamoxifenConceptsFES-PET/CTPET/CTClinical trialsER-positive metastatic breast cancerPhase IPhase I clinical trialEstrogen receptor occupancyPhase II trialMetastatic breast cancerSubsequent clinical trialsClin Cancer ResER downregulationFulvestrant therapyAntagonist/Escalation trialII trialTarget lesionsBreast cancerER occupancyUseful biomarkerPatientsReceptor occupancyDay 3Uptake valueDrug dosage
1992
High-Dose Oral Tamoxifen, a Potential Multidrug-Resistance-Reversal Agent: Phase I Trial in Combination With Vinblastine
Trump DL, Smith DC, Ellis PG, Rogers MP, Schold SC, Winer EP, Panella TJ, Jordan VC, Fine RL. High-Dose Oral Tamoxifen, a Potential Multidrug-Resistance-Reversal Agent: Phase I Trial in Combination With Vinblastine. Journal Of The National Cancer Institute 1992, 84: 1811-1816. PMID: 1359155, DOI: 10.1093/jnci/84.23.1811.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralAdultAgedAntineoplastic Combined Chemotherapy ProtocolsATP Binding Cassette Transporter, Subfamily B, Member 1Drug Administration ScheduleDrug ResistanceFemaleHumansInfusions, IntravenousMaleMembrane GlycoproteinsMiddle AgedNeoplasm ProteinsNeoplasmsTamoxifenVinblastineConceptsLoading doseN-desmethyltamoxifenOral tamoxifenContinuous infusionPlasma concentrationsHigh-dose oral tamoxifenDose-limiting toxic effectPhase I clinical trialAdvanced epithelial tumorsHigh-dose tamoxifenTriphenylethylene antiestrogen tamoxifenPhase II trialDose-limiting toxicityPhase I trialDoses of tamoxifenStart of treatmentP-glycoprotein functionToxicity of vinblastineAnti-neoplastic agentsToxic effectsMetabolite N-desmethyltamoxifenIntracellular concentrationAsymptomatic prolongationStarting doseII trial