Personalized medicine, also known as precision medicine, is a broad medical paradigm for tailoring patients’ treatments based upon their individual biological makeup to produce the most effective, safest clinical outcomes. Personalized medicine has the potential for enhancing nearly all fields of human health but has gained particular traction in oncology, a disease characterized by heterogeneity within patient populations. The application of personalized medicine in oncology requires both bioanalytical methods capable of providing real-time, useful clinical information in individual patients and new precision drugs matched to individual patient’s clinical disease. My dissertation research encompasses two main projects centered on personalized medicine. The first project is the study of the molecular pharmacology of the antiviral and anticancer compound OSW-1. OSW-1 induces its antiviral activity through targeting oxysterol-binding protein (OSBP) and its anticancer activity through targeting OSBP-related protein 4 (ORP4). My research has established ORP4 as a potential personalized drug target in ovarian cancer, and OSW-1 as a potential lead target with potent anticancer activity in ovarian cell lines through targeting ORP4. The second major development is a single cell mass spectrometry method capable of quantifying chemotherapy drug levels in individual cancer cells, including single cancer cells isolated from patients. These discoveries have clear potential for developing clinically relevant, better personalized medicine through the development of optimal precision drug design and administration.