A systematic highlight on the syntheses of 1,2,3-triazole fused macrocycles possessing biological activities like anticancer, antibacterial, antiviral, anti-inflammatory, antilarval and more has been presented in this review since 2006. The well-renowned Cu-catalyzed azide-alkyne cycloaddition reaction was noted to be one of the highly efficient and most common methods utilized by several scientists for the synthesis of 1,4-disubstituted triazole fused macrocycles while the Ru-catalyzed cycloaddition led to the 1,5-disubstituted bioactive triazoles. This review would thus be extremely beneficial for both synthetic organic and medicinal chemists.