Cardiovascular disease is the foremost cause of mortality worldwide and a major contributor to healthcare expenditure, primarily due to the high incidence and progression to heart failure. Current treatments remain insufficient to halt or reverse disease progression, highlighting the urgent need for innovative approaches.1 Animal venoms, comprising a diverse array of highly selective bioactive peptides, represent a rich and underexplored resource for modulating human physiological systems, including cardiac function.2,3 This study enables the systematic exploration of venom-derived peptides with relevance to cardiovascular disease by leveraging integrated multidisciplinary strategies. These include venom bioactivity screening in human cardiac models, integrated venomics, peptide chemistry, and structure-activity relationship studies. Functional characterisation of selected candidates has revealed modulatory effects on cardiac contractility and rhythm, highlighting their value as pharmacological tools and prospective therapeutic leads. Our ongoing studies will continue to expand the repertoire of molecular tools available for cardiovascular research and may help address mechanisms not currently targeted by existing treatments.