The formylpeptide receptor (FPR) family, particularly FPR2, has emerged as a master regulator of inflammation and its resolution. Given that both cardiovascular diseases and metabolic disorders are characterised by pro-inflammatory scenarios, often with resultant impairment of the healing response to (i.e. resolution of) inflammation, therapeutic targeting of the FPR family with judicious agonist selection provides new promise for tackling cardiometabolic disease. Here, we consider the pharmacology of this intriguing receptor family, the potential for novel biased signalling at its receptor subtypes and the current status of both endogenous and synthetic agonists (including peptides/proteins, small molecules and lipids) reported to be active at FPRs. A detailed review of the therapeutic potential of published FPR ligands involved in regulating and resolving inflammation in cardiometabolic disease is also provided. We anticipate that a broader understanding of, and greater appreciation for, the translational potential of pro-resolution FPR-based therapies may offer new effective means of targeting a range of cardiometabolic disorders and their resultant complications.