Although considerable progress on enantioselective gold(I)-catalyzed transformations has been achieved, the asymmetric activation of non-prochiral alkyne-containing small molecules still represents a great challenge. Herein we summarize recent advances in intra- and intermolecular enantioselective gold(I)-catalyzed reactions involving alkynes, discussing new chiral ligand designs that lie at the basis of these developments. Square planar chiral gold(III) complexes, which offer an alternative to chiral gold(I) complexes, are also discussed.