2020
Masterkey-01: Phase I/II, open-label multicenter study to assess safety, tolerability, pharmacokinetics, and antitumor activity of BDTX-189, an inhibitor of allosteric ErbB mutations, in patients with advanced solid malignancies.
Hamilton E, Patel M, Rodon J, Hong D, Schram A, Janne P, LoRusso P, Sachdev J, Ou S, Buck E, O'Connor M, Waters N, Witt K, Cook C. Masterkey-01: Phase I/II, open-label multicenter study to assess safety, tolerability, pharmacokinetics, and antitumor activity of BDTX-189, an inhibitor of allosteric ErbB mutations, in patients with advanced solid malignancies. Journal Of Clinical Oncology 2020, 38: tps3665-tps3665. DOI: 10.1200/jco.2020.38.15_suppl.tps3665.Peer-Reviewed Original ResearchAntitumor activityStandard therapyPreliminary efficacyERBB mutationsOpen-label multicenter studySignificant unmet need existsPhase I/IIHER2 tyrosine kinase inhibitorPhase 2 doseAdvanced solid malignanciesAdequate drug exposureMetastatic solid tumorsPreliminary antitumor activityExon 20 insertionsOncogenic driver mutationsTyrosine kinase inhibitorsUnmet need existsAssessment of safetyCurrent eGFRExpansion cohortMulticenter studyPharmacodynamic effectsSolid malignanciesDrug exposureCohort 1
2016
ACTR-10. PHASE 0 TRIAL OF AZD1775 IN FIRST-RECURRENCE GLIOBLASTOMA PATIENTS
Sanai N, Li J, Boerner J, Dhruv H, Berens M, LoRusso P. ACTR-10. PHASE 0 TRIAL OF AZD1775 IN FIRST-RECURRENCE GLIOBLASTOMA PATIENTS. Neuro-Oncology 2016, 18: vi3-vi3. DOI: 10.1093/neuonc/now212.009.Peer-Reviewed Original ResearchPhase 0 trialsInterindividual variabilityGlioblastoma patientsPhase II studyApparent oral clearanceGlomerular filtration ratePhase I trialCL/F.CL/FSparse blood samplingElimination rate constantAbsorption rate constantPD endpointsAdult patientsII studyOral clearanceI trialSingle doseDrug exposureFiltration ratePreclinical modelsPreclinical studiesGlioma patientsPlasma ratioBlood sampling
2009
Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of PF-00337210, a highly selective VEGFR inhibitor
Liu G, LoRusso P, Goncalves P, Holen K, Traynor A, Zhang J, Hee B, Tortorici M, Shalinsky D, Ricart A. Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of PF-00337210, a highly selective VEGFR inhibitor. Journal Of Clinical Oncology 2009, 27: 3519-3519. DOI: 10.1200/jco.2009.27.15_suppl.3519.Peer-Reviewed Original ResearchAdverse eventsMyocardial ischemiaCommon treatment-related adverse eventsVEGFR inhibitorsTreatment-related adverse eventsVEGF/VEGFR inhibitorsAdvanced solid tumorsObserved accumulation ratioSelective VEGFR inhibitorsStable diseaseBID dosingChest painHypertensive effectSignificant hypertensionFirst doseObjective responseAntihypertensive agentsSafety profileDrug exposurePharmacodynamic studiesXenograft growthHypertensionVascular permeabilityPK dataVEGFR inhibition
2006
A phase I study of a novel spectrum selective kinase inhibitor (SSKI), XL880, administered orally in patients (pts) with advanced solid tumors (STs)
Eder J, Appleman L, Heath E, Malburg L, Zhu A, Pilat M, Shapiro G, Lorusso P. A phase I study of a novel spectrum selective kinase inhibitor (SSKI), XL880, administered orally in patients (pts) with advanced solid tumors (STs). Journal Of Clinical Oncology 2006, 24: 3041-3041. DOI: 10.1200/jco.2006.24.18_suppl.3041.Peer-Reviewed Original ResearchConsecutive daily dosesAdvanced solid tumorsDaily dosesSolid tumorsSingle doseReceptor tyrosine kinasesSmall-molecule MET inhibitorTerminal half-life valuesGrade 2 hypertensionPapillary renal cell carcinomaSystemic drug exposurePeak plasma levelsRenal cell carcinomaTumor-associated vasculatureHepatocyte growth factor receptorGrowth factor receptorPharmacokinetic samplingPK samplingPartial responseRepeat dosingCell carcinomaMinor responsePlasma levelsDrug exposureMET inhibitors