Apelin is a recently discovered bioactive peptide, known to be an endogenous high-affinity ligand for the previously orphan G protein-coupled receptor APJ. Apelin/APJ as a novel signaling pathway has been shown to play many crucial roles in cardiovascular function, blood pressure regulation, fluid homeostasis, feeding behavior, obesity, type 2 diabetes mellitus, adipoinsular axis regulation, cell proliferation, angiogenesis, neuroprotection and thermoregulation. This ubiquitous peptide opens a new field of research in biology and medicine. In this regard, the aim of this short review is to compile the evidence for the apelin involvement in modulation of cardiovascular system and introduction of this new peptidic pathway as a useful drug target in the treatment of cardiovascular diseases in future.