Disadvantages of conventional drug delivery systems (DDS), such as systemic circulation, interaction with physiochemical factors, reduced bioavailability, and insufficient drug concentration at bone defect site, have underlined the importance of developing efficacious local drug delivery systems. Octacalcium phosphate (OCP) is presumed to be the precursor of biologically formed apatite, owing to its similarity to hydroxyapatite (HAp) and readiness to convert to it. Specific crystal structure of OCP is constructed of compiled apatite layers and water layers, which make possible the incorporation of various ions in its structure, making it feasible to alter the overall effect OCP has in the system. Next to that intrinsic property, characteristics as high solubility, biodegradability and osteoconductivity have made it indispensable to tailor OCP as a carrier material. In this review, we present the main characteristics and progress done on utilizing OCP as an innovative vehicle and provide suggestions for possible research pathways and advantages for local drug delivery in bone tissue engineering. Statement of significance: Octacalcium phosphate (OCP), being a precursor to biologically formed apatite, has many assets when compared to other calcium phosphates. Owing to its highly pertinent structure, it is being used as a vehicle for biologically active substances or ions for bone regeneration. However, orchestrating drug delivery systems with OCP, in order to achieve the best possible outcome, is still a pioneering concept, and the all-encompassing data is still scarce. Although several articles have been published on this matter, to this date there is no systematic overview pointing out the benefits that OCP can bring in the field of drug delivery. Here we offer a comprehensive overview, starting from the OCP synthesis to its structure, morphology, and the biological significance OCP has.