2000
Pharmacokinetic and pharmacodynamic evaluation of the glycinamide ribonucleotide formyltransferase inhibitor AG2034.
McLeod HL, Cassidy J, Powrie RH, Priest DG, Zorbas MA, Synold TW, Shibata S, Spicer D, Bissett D, Pithavala YK, Collier MA, Paradiso LJ, Roberts JD. Pharmacokinetic and pharmacodynamic evaluation of the glycinamide ribonucleotide formyltransferase inhibitor AG2034. Clinical Cancer Research 2000, 6: 2677-84. PMID: 10914709.Peer-Reviewed Original ResearchConceptsGlycinamide ribonucleotide formyltransferaseCourse 1Systemic clearanceGrade III/IV toxicityGrade II toxicityMin/m2Rapid systemic clearanceVolume of distributionEvaluable patientsSystemic exposurePharmacodynamic evaluationClinical centersBolus injectionPharmacokinetic approachBlood samplesPatient toxicityPatientsElimination patternReproducible ELISAAG2034Course 3Phase IAnticancer agentsPurine synthesis pathwayDe novo purine synthesis pathway
1998
Phase Ib trial of bryostatin 1 in patients with refractory malignancies.
Grant S, Roberts J, Poplin E, Tombes MB, Kyle B, Welch D, Carr M, Bear HD. Phase Ib trial of bryostatin 1 in patients with refractory malignancies. Clinical Cancer Research 1998, 4: 611-8. PMID: 9533528.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedAntineoplastic AgentsBryostatinsCohort StudiesCytotoxicity, ImmunologicDrug Administration ScheduleFemaleHumansImmunophenotypingInfusions, IntravenousInterleukin-2LactonesLymphocyte ActivationLymphocytesLymphomaMacrolidesMaleMetabolic Clearance RateMiddle AgedNeoplasmsPatient SelectionPlatelet AggregationProtein Kinase CConceptsPhase Ib trialIb trialCohort 3Lymphokine-activated killer cell activityBryostatin 1Bryostatin-1 administrationObjective clinical responsesKiller cell activityLiver function testsSubset of patientsBryostatin 1 treatmentSignificant posttreatment increasePKC activitySplit courseClinical responseFirst doseLiver metastasesNonhematological malignanciesRefractory malignanciesFunction testsPatient cohortCohort 1Interleukin-2Immunophenotypic profileTransient elevation
1987
Phase I trial of tiazofurin administered by i.v. bolus daily for 5 days, with pharmacokinetic evaluation.
Roberts JD, Stewart JA, McCormack JJ, Krakoff IR, Culham CA, Hartshorn JN, Newman RA, Haugh LD, Young JA. Phase I trial of tiazofurin administered by i.v. bolus daily for 5 days, with pharmacokinetic evaluation. Journal Of The National Cancer Institute 1987, 71: 141-9. PMID: 3802111.Peer-Reviewed Original ResearchConceptsTreatment interruptionTransient toxic effectsM2/dayTreatment coursePhase I clinical trialToxic effectsAntitumor activityPhase II trialPhase I trialBolus IV infusionFrequent treatment interruptionsSerum biochemical abnormalitiesSystemic toxic effectsCoadministration of allopurinolMurine tumor modelsUric acid productionLow dose levelsSignificant antitumor activityBolus dailyInjury manifestTransient pericarditisII trialSerum hemoglobinI trialIV infusion