A dialogue on innovation in anticancer drug discovery

Medicinal chemistry has driven the evolution of oncology drug discovery, transitioning from early cytotoxic agents to modern precision-guided therapies. This opinion article traces the historical trajectory of medicinal chemistry practices, beginning with the era of conventional chemotherapy and moving through the development of targeted therapies utilizing various precision oncology strategies. It then explores the recent wave of innovations-such as proximity inducers and drug conjugates-that have significantly redefined the druggable proteome. While these emerging modalities promise transformative benefits for patients, they also introduce unique challenges related to delivery, selectivity, and acquired resistance. We conclude with a perspective on the future of oncology that the integration of these novel strategies with computational design, advanced proteomics, and biomarker-driven approaches will be essential to accelerate the development of next-generation personalized cancer therapies.