We summarize the latest results of C(sp ³)-C(sp ³) coupling by visible-light photoredox catalysis in recent years and focus on the catalytic systems, reaction mechanisms and practical applications in synthesizing bioactivity molecules or drug molecules. Indeed, introducing transition metals or chiral catalysts in the visible light-catalyzed reaction system and the constructing of a novel synergistic catalysis system can make the precise formation of the C(sp ³)-C(sp ³) bond under mild conditions become a reality, which will have important implications for the design and development of chiral drugs. Finally, the future development of visible-light photoredox catalysis is prospected.