Altered metabolism and perfusion are implicated in cancer’s underlying pathophysiology. Prior preclinical and clinical studies have shown that metabolic and perfusion imaging could provide a sensitive and specific evaluation of tumor grade and therapeutic response. We aim to develop a dual-agent hyperpolarized 13C MR technique for simultaneous metabolic and perfusion imaging in humans. Here, we report the technical developments towards its clinical translation: 1) formulation and co-polarization system of 13C pyruvate and urea, 2) imaging probe characterization, 3) safety-related studies, and 4) multi-probe imaging sequence. Upon FDA approval, this work would lead to the first-in-human dual-agent hyperpolarized MR study.