Introduction: Orthodontic tooth movement is a biologically mediated process involving inflammatory signaling and coordinated bone remodeling in response to mechanical force. Increasing evidence suggests that systemic and locally administered pharmacological agents can modulate this process by influencing cellular and molecular pathways regulating osteoclastogenesis and osteogenesis. Objective: To analyze the role of various medications in orthodontic tooth movement by describing their mechanisms of action, clinical implications, and emerging therapeutic applications. Methods: A narrative literature review was conducted using PubMed/MEDLINE, Scopus, Web of Science, and the Cochrane Library databases. Publications in English from January 2010 to October 2025 were screened. Original studies in humans and animal models, in vitro investigations, clinical trials, and relevant systematic reviews addressing drug-related modulation of OTM were included. Non-peer-reviewed publications, incomplete reports, and unrelated studies were excluded. A total of 70 studies met the inclusion criteria and were analyzed through qualitative synthesis. Results: Pharmacological agents were categorized as inhibitors or accelerators of OTM. Nonsteroidal anti-inflammatory drugs (NSAIDs), bisphosphonates, corticosteroids, and certain hormonal therapies were consistently associated with reduced osteoclastic activity and slower tooth movement. Conversely, prostaglandins, vitamin D metabolites, thyroid hormones, and selected molecular modulators demonstrated acceleration effects, primarily in preclinical models. Emerging approaches, including selective estrogen receptor modulators, monoclonal antibodies, and localized drug delivery systems, show promising potential; however, most evidence remains experimental and heterogeneous. Conclusion: Pharmacological modulation represents a biologically relevant adjunct to orthodontic biomechanics. Nevertheless, current evidence is predominantly derived from animal and preclinical studies, limiting direct clinical extrapolation. Careful assessment of patients’ pharmacological profiles is essential for individualized treatment planning, and further controlled clinical trials are required before routine therapeutic implementation. Keywords: orthodontic tooth movement, pharmacological agents, bone remodeling, drug-tissue interaction, narrative review
Pacheco-Quito et al. (Wed,) studied this question.