Nowadays, 5-aminolevulinic acid (5-ALA) plays an influential role in the detection of malignant tumors as a photodynamic diagnosis tool. Nevertheless, an outlook regarding 5-ALA applicability in magnetic resonance imaging (MRI) has recently emerged. This review intends to provide an overview of the documents regarding the effect of 5-ALA on cellular iron metabolism and the application of 5-ALA in MRI. Many studies confirmed the impact of 5-ALA on promoting intracellular Heme synthesis and iron metabolism, which support the capability of 5-ALA in MRI owing to the susceptibility effect of iron. Therefore, concerning the high safety and high affinity of 5-ALA to tumor cells, 5-ALA-based MRI could be an intriguing method for malignant foci identification.