•The discovery of buprenorphine in 1966 revolutionized care for opioid use disorder.•US government and private industry partnership led to buprenorphine-based medications.•Confronting barriers to use these medications is critical to address the opioid crisis. Buprenorphine-based medications were first approved by the United States Food and Drug Administration in 2002 for the treatment of opioid dependence, or opioid use disorder (OUD) as the condition is presently known. This regulatory milestone was the outcome of 36 years of research and development, which also led to the development and approval of several other new buprenorphine-based medications. In this short review, we first describe the discovery and early development stages of buprenorphine. Second, we review key steps that led to the development of buprenorphine as a drug product. Third, we explain the regulatory approval of several buprenorphine-based medications for the treatment of OUD. We also discuss these developments in the context of the evolution of regulations and policies that have progressively improved OUD treatment availability and efficacy, although challenges remain in removing system-level, provider-level, and local-level barriers to quality treatment, to integrating OUD treatment into routine care and other settings, to reducing disparities in access to treatment, and to optimizing person-centered outcomes.