An AI-assisted design pipeline delivered a new gallium-68 PET tracer, [68Ga]Ga-DOTA-FZPF, targeting PARP-1, which has now completed first-in-human evaluation in breast and ovarian cancer patients. The work translates AI-enabled chemistry and targeting optimization into a clinical imaging candidate. The study adds to momentum in radiotheranostics and biomarker imaging, where PARP-1 status can support treatment selection and patient stratification for DNA damage response–directed regimens. By reaching the first human testing stage, the tracer program moves beyond preclinical validation into the phase where biodistribution, safety, and imaging feasibility become the gating criteria for further development.