Grotta della Monaca is a karst cave located in Calabria, the southernmost region of the Italian peninsula. About half a kilometre deep, the cavern has drawn the attention of man since Paleolithic because of the abundance of metal ores in it (mainly iron hydroxides but also copper carbonates). These easily reachable minerals have been exploited during prehistory and especially between the late Neolithic and the early Copper Age. Research conducted within the site from 2000 to 2012 has allowed us to understand various aspects of the ancient mining activities and, at the same time, to reconstruct the basic steps of the operational chain connected to the procurement and to the first processing of such resources: from the choice of tools to the various extractive techniques adopted, from the disposal of mining debris to the early operations of ore processing. In this paper we focus on two categories of macrolithic tools: those used to extract minerals and those used for their first processing. The first group is composed by 51 artefacts divided into axes, hammers and pickaxes with central groove, found in the deeper areas of the cave corresponding to mining areas. Their morphological and dimensional variability indicates a significant functional diversification; furthermore, the choice of different very hard metamorphic rocks implies a high awareness in the selection of the raw materials used for making this implements. The second group includes 22 tools with different functions – mainly made of sandstone – classified as querns and grinder/crusher. They were found in an underground area adjacent to the entrance, characterized by large and comfortable spaces, with the widespread presence of natural light. A recent traceological study has clarified the function of such artefacts, used to grind mined blocks of iron hydroxides to obtain a powder. The multidisciplinary approach in studying mining tools from Grotta della Monaca (such as petrography, archaeological typology and traceology) has allowed us to gain important knowledge about their general characteristics.