2024
Safety, pharmacokinetics (PK), pharmacodynamics (PD) and efficacy of KT-253, a targeted protein degrader of MDM2, in patients with relapsed/refractory (R/R) solid tumors, lymphoma, high grade myeloid malignancies and acute lymphoblastic leukemia (ALL).
Khawaja M, Naqash A, Schneider R, Shastri A, Stahl M, Moser J, Abdel Karim N, Madanat Y, Jonas B, Stein E, Gadgeel S, McCloskey J, Gollerkeri A, Perea R, Chutake Y, Agarwal S, Henrick P, Shi K, Daver N. Safety, pharmacokinetics (PK), pharmacodynamics (PD) and efficacy of KT-253, a targeted protein degrader of MDM2, in patients with relapsed/refractory (R/R) solid tumors, lymphoma, high grade myeloid malignancies and acute lymphoblastic leukemia (ALL). Journal Of Clinical Oncology 2024, 42: 3084-3084. DOI: 10.1200/jco.2024.42.16_suppl.3084.Peer-Reviewed Original ResearchAcute lymphoblastic leukemiaMouse double minute 2Arm BArm AAdverse eventsSolid tumorsOpen-label phase 1 studyMouse double minute 2 inhibitorUpregulated p53 activityDecreased oral intakeMerkel cell carcinomaAdenoid cystic carcinomaPhase 1 studySolid tumor typesAcute apoptotic responseDose-dependent increaseGDF-15 proteinPreclinical PDX modelsWild-type p53Anti-tumor activityDouble minute 2Upregulation of CDKN1AR/R AMLDose escalationTumor regression
2022
A first-in-human, phase 1 study of ASTX029, a dual-mechanism inhibitor of ERK1/2, in relapsed/refractory solid tumors.
LoRusso P, Rasco D, Shapiro G, Mita A, Azad N, Swiecicki P, El-Khoueiry A, Gandara D, Kummar S, Tanajian H, Taylor J, Bottone F, Toguchi M, Hindley C, Chan D, Oganesian A, Keer H, Dao K, Sullivan R, Spira A. A first-in-human, phase 1 study of ASTX029, a dual-mechanism inhibitor of ERK1/2, in relapsed/refractory solid tumors. Journal Of Clinical Oncology 2022, 40: 9085-9085. DOI: 10.1200/jco.2022.40.16_suppl.9085.Peer-Reviewed Original ResearchRefractory solid tumorsPhase 1 studyCentral serous retinopathyDose levelsSolid tumorsPartial responseOpen-label phase 1 studyPhase 1bNon-small cell lung cancerTarget exposurePD effectsDose-limiting toxicity eventsPhase 2 dosePhase 2 studyPreliminary clinical activityCell lung cancerDaily dose levelsDose-escalation designDays of dosingFresh tumor biopsiesClass of drugsPhase 1aExtracellular signal-regulated kinase 1/2 (ERK1/2) inhibitorNSCLC subjectsOcular AEs
2019
Clinical Activity of CC-90009, a Cereblon E3 Ligase Modulator and First-in-Class GSPT1 Degrader, As a Single Agent in Patients with Relapsed or Refractory Acute Myeloid Leukemia (R/R AML): First Results from a Phase I Dose-Finding Study
Uy G, Minden M, Montesinos P, DeAngelo D, Altman J, Koprivnikar J, Vyas P, Fløisand Y, Vidriales M, Gjertsen B, Esteve J, Buchholz T, Couto S, Fan J, Hanna B, Li L, Pierce D, Hege K, Pourdehnad M, Zeidan A. Clinical Activity of CC-90009, a Cereblon E3 Ligase Modulator and First-in-Class GSPT1 Degrader, As a Single Agent in Patients with Relapsed or Refractory Acute Myeloid Leukemia (R/R AML): First Results from a Phase I Dose-Finding Study. Blood 2019, 134: 232. DOI: 10.1182/blood-2019-123966.Peer-Reviewed Original ResearchTreatment-emergent adverse eventsCereblon E3 ligase modulatorSystemic inflammatory response syndromeCC-90009Phase 1 studyR AMLHighest dose levelDose levelsCelgene CorporationDaiichi SankyoSpeakers bureauGrade 3/4 treatment-emergent adverse eventsDay 1Jazz PharmaceuticalsObserved treatment-emergent adverse eventOpen-label phase 1 studySerious treatment-emergent adverse eventsHyperglycemic hyperosmolar nonketotic syndromeIncomplete blood count recoveryMorphologic leukemia-free stateRefractory acute myeloid leukemiaHigh-risk myelodysplastic syndromeAdvisory CommitteeAntileukemic activityI Dose-Finding Study
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