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
Modulation of O6-alkylguanine-DNA alkyltransferase-mediated carmustine resistance using streptozotocin: a phase I trial.
Panella TJ, Smith DC, Schold SC, Rogers MP, Winer EP, Fine RL, Crawford J, Herndon JE, Trump DL. Modulation of O6-alkylguanine-DNA alkyltransferase-mediated carmustine resistance using streptozotocin: a phase I trial. Cancer Research 1992, 52: 2456-9. PMID: 1533174.Peer-Reviewed Original ResearchConceptsFmol/M2/dayDose-limiting toxicityPhase I trialDose of BCNUSerum alkaline phosphataseBCNU doseSTZ doseStarting dosePartial responseSerum creatinineThird doseDose escalationI trialMild elevationDay 3BCNU resistanceNitrosourea resistanceSTZBCNU cytotoxicityBCNUDoseAdditional studiesO6-alkylguanine-DNA alkyltransferaseAlkaline phosphatase