Development of GPER agonists as Cancer Therapeutics

Project summaryThis project is designed to evaluate a new class of anti cancer agents for treatment of invasive melanomapancreaslungand colon carcinomasThe study compounds are smallsynthetic molecules that have not previously been used in peopleand bind to a surface receptor on tumor cells that has not previously been targeted in cancerStrong preliminary results indicate that the study compounds potentiate the efficacy of the new immune checkpoint inhibitors that are now the standard of care for metastatic melanomaIn this proposalwe will determine dosing regimens that will maximize the anti cancer effectsdefine biomarkers that correlate with tumor responseand determine whether the anti melanoma synergy between GandPDextends to other immune checkpoint inhibitorsCompletion of the proposed work will contribute to the completion of IND enabling work necessary to translate these discoveries to first in human trials Project NarrativeWhile new immune checkpoint inhibitor pharmaceuticals have resulted in improved outcomes for some metastatic cancer patientsmost will still succumb to their tumorand new therapeutic options are urgently neededThis work will build on promising preliminary data to evaluate a new class of compounds that improve the efficacy of immune checkpoint inhibitors in melanomapancreaslungand colon carcinomasas well as identify optimal dosing regimens and biomarker assaysTogetherthis work will facilitate the completion of IND enabling work necessary to translate these discoveries to first in human trials