Small molecule therapy for metastatic prostate cancer

Enzalutamide resistance is a major obstacle in the treatment of metastatic castration resistant prostate cancer mCRPC Recently we developed a small molecule lead compound GH and demonstrated its potent activity against bone metastatic prostate cancer cells In this Phase I STTR application we hypothesize that GH is a novel lead compound with nanomolar potency against enzalutamide resistant and bone metastatic prostate cancer Two Aims are proposed In Aim we will synthesize high purity GH and determine the acute toxicity pharmacokinetics and in vivo bioavailability distribution of GH in rodent models in Aim we will validate the in vivo efficacy of GH against mCRPC in clinically relevant animal models These studies will provide convincing rationale for us to continue the GH project at MetCure for further pre clinical and clinical development The project has important impact and translational potential in treating a lethal disease In this Phase I STTR application we will develop a potent small molecule drug GH to overcome enzalutamide resistance and treat bone metastatic prostate cancer a major cause of cancer death in American men This project has important impact in treating a lethal disease reducing cancer morbidity and improving healthcare in the United States and globally