The Caatinga biome, which is situated in the interior regions of northeastern Brazil, is a well-defined and recognized ecological zone of semiarid tropical vegetation. It is the largest continuous expanse of seasonally dry tropical forests in South America. Despite its status as a center of endemism and biodiversity, the Caatinga remains among the least studied biogeographical regions. Unfortunately, anthropogenic disturbances contribute to the ongoing process of desertification, leading to significant losses in biodiversity that are yet to be fully understood. We have compiled scientific studies published in the last decade, specifically those addressing biodiversity and the utilization of phytochemicals from this unique biome. The analysis herein highlights major plant species and their most studied secondary metabolites and explores the technological and biotechnological aspects of the flora, with an emphasis on the development of new bioactive products. Additionally, we provide an overview of patents and insights into the production of biotechnological inputs. Despite its recognition as a biodiversity hotspot, the Caatinga biome is under threat, endangering the loss of exclusive treasures even before they were comprehensively studied. Hence, further efforts are needed to know and value the Caatinga flora and its chemical constituents to preserve them for the future development of products in a sustainable and rational way.