Urban overheating is the most documented phenomenon of climate change impacting humans. This article presents the most recent developments on the magnitude and characteristics of urban overheating and the potential synergies with global climatic change. It analyses the latest qualitative and quantitative data on the impact of higher urban temperatures on buildings’ energy supply and demand, heat-related mortality, morbidity and wellbeing, human productivity, survivability of low-income populations, and environmental quality of cities. It describes the state of the art on the development of innovative mitigation materials, advanced urban greenery, heat dissipation, and evaporative techniques as the main mitigation and adaptation technologies to offset the impact of urban overheating. It also analyses the current knowledge on the impact of each mitigation technology on energy, health, environmental quality, urban economy, and survivability. Finally, this article presents the main future challenges related to urban overheating and proposes a specific research agenda to alleviate and counterbalance its impact on human life.