Phase 1 trial of a novel, first-in-class G protein-coupled estrogen receptor (GPER) agonist, LNS8801, in patients with advanced or recurrent treatment-refractory solid malignancies.
Muller C, Brown-Glaberman U, Chaney M, Garyantes T, LoRusso P, McQuade J, Mita A, Mita M, Natale C, Orloff M, Papadopoulos K, Sato T, Yilmaz E, Rodon J. Phase 1 trial of a novel, first-in-class G protein-coupled estrogen receptor (GPER) agonist, LNS8801, in patients with advanced or recurrent treatment-refractory solid malignancies. Journal Of Clinical Oncology 2021, 39: 3084-3084. DOI: 10.1200/jco.2021.39.15_suppl.3084.Peer-Reviewed Original ResearchG protein-coupled estrogen receptorC-Myc depletionStable diseaseDose levelsMetastatic solid tumor malignanciesAnti-PD-1 antibodyProtein-coupled estrogen receptorHr of dosingPhase 2 doseRECIST partial responseTreatment-related SAEsImmune checkpoint inhibitorsPhase 1 trialSolid tumor malignanciesPK/PD dataSelective small molecule agonistHigh unmet needDays of treatmentAnti-tumor activityEstrogen receptor agonistsSmall molecule agonistsTumor immune recognitionG protein-coupled receptorsAnti-cancer therapyCombination cohort