2021
866 RBN-2397, a novel, potent, and selective PARP7 inhibitor, induces tumor-intrinsic type I interferon responses and adaptive immunity in preclinical models and patient tumors
Kuplast-Barr K, Kuplast-Barr K, Johnson M, Patel M, Yap T, Falchook G, LoRusso P, Abo R, Liu C, Manyak E, Cleary L, Bozon V, Parasuraman S, Keilhack H, McEachern K. 866 RBN-2397, a novel, potent, and selective PARP7 inhibitor, induces tumor-intrinsic type I interferon responses and adaptive immunity in preclinical models and patient tumors. Journal For ImmunoTherapy Of Cancer 2021, 9: a907-a907. DOI: 10.1136/jitc-2021-sitc2021.866.Peer-Reviewed Original ResearchPreclinical modelsPatient tumor biopsiesTumor biopsiesAdaptive immunityCancer cellsHuman phase 1 studyTumor-specific immune memoryCD8 T cell infiltrationTumor microenvironmentPhase I clinical studyType IAdvanced solid tumorsPhase 1 studyT cell infiltrationGranzyme B expressionDurable tumor regressionAdaptive immune responsesInterferon-stimulated gene expressionImmune stimulatory effectsType I interferon responseCytosolic nucleic acidsType I interferonActivated T cellsNon-tumor tissuesI interferon response
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
1994
Antitumour activity of N-[[1-[[2-(diethylamino)ethyl]amino]-9-oxo-9H-thioxanthen-4-yl]methyl]methanesulfonamide (WIN33377) and analogues
Corbett T, Lowichik N, Pugh S, Polin L, Panchapor C, White K, Knight J, Demchik L, Jones J, Jones L, Biernat L, Lorusso P, Foster B, Heilbrun L, Rake J, Mattes K, Perni R, Powles R, Hlavac A, Wentland M, Coughlin S, Baker L, Valeriote F. Antitumour activity of N-[[1-[[2-(diethylamino)ethyl]amino]-9-oxo-9H-thioxanthen-4-yl]methyl]methanesulfonamide (WIN33377) and analogues. Expert Opinion On Investigational Drugs 1994, 3: 1281-1292. DOI: 10.1517/13543784.3.12.1281.Peer-Reviewed Original ResearchLiver toxicityAntitumour activityClinical trialsPhase I clinical trialSevere liver toxicityEfficacious dose levelsPreclinical modelsDose levelsBetter efficacyWeekly scheduleAntischistosomal agentsDay scheduleHycanthoneM2 levelToxicityTrialsMost analoguesAgentsRecovery timeVariety of analoguesGroupActivityMiceDose