2009
A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765, a PI3K/TORC1/TORC2 inhibitor administered orally to patients (pts) with advanced solid tumors
LoRusso P, Markman B, Tabernero J, Shazer R, Nguyen L, Heath E, Patnaik A, Papadopoulos K. A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765, a PI3K/TORC1/TORC2 inhibitor administered orally to patients (pts) with advanced solid tumors. Journal Of Clinical Oncology 2009, 27: 3502-3502. DOI: 10.1200/jco.2009.27.15_suppl.3502.Peer-Reviewed Original ResearchAdverse eventsPhase I dose-escalation studyI dose-escalation studyDurable stable diseaseElevated hepatic transaminasesFood-induced increaseElevated liver enzymesNausea/vomitingSerious adverse eventsAdvanced solid tumorsDose-escalation studyPI3K pathway inhibitionClass I PI3K isoformsTumor growth inhibitionPI3K pathwayPharmacodynamic modulationQD regimenStable diseaseBID regimenHepatic transaminasesNeurological complaintsRepeat dosingPI3K isoformsPlasma insulinTolerable doses
2007
A phase I dose escalation trial of a daily oral CDK 4/6 inhibitor PD-0332991
O’Dwyer P, LoRusso P, DeMichele A, Gupta V, Barbi A, Dials H, Chen I, Courtney R, Wilner K, Schwartz G. A phase I dose escalation trial of a daily oral CDK 4/6 inhibitor PD-0332991. Journal Of Clinical Oncology 2007, 25: 3550-3550. DOI: 10.1200/jco.2007.25.18_suppl.3550.Peer-Reviewed Original ResearchMTD/RP2DSchedule 2/1Stable diseasePD-0332991Escalation trialPhase IPositive solid tumorsRb-positive tumorsCommon tumor typesDose-dependent increaseNovel oral inhibitorEffect of foodPhospho-Rb proteinsCommon AEsPharmacodynamic modulationMedian ageAdvanced cancerOral inhibitorPositive tumorsTumor specimensPatientsSingle agentSolid tumorsTumor typesSuccessive dose