Drug Design, Development and Therapy (Jun 2025)
Clinical Use of Fospropofol Disodium: Evaluation of Pharmacology, Safety, and Efficacy
Abstract
Congcong Zou,1 Hongyang Chen,2 Yanhua Qiu1 1Anesthesia and Surgery Center of West China Xiamen Hospital, Sichuan University, Xiamen, People’s Republic of China; 2Department of Anesthesiology, West China Hospital, Sichuan University, Chengdu, People’s Republic of ChinaCorrespondence: Yanhua Qiu, Anesthesia and Surgery Center of West China Xiamen Hospital, Sichuan University, 699 Jinyuan West Road, Xingbin Street, Jimei District, Xiamen, 361000, People’s Republic of China, Email [email protected]: Fospropofol disodium (FD) is a safe and effective alternative to propofol, as it avoids injection pain, severe hypotension, significant respiratory depression, and allergic reactions during intravenous anesthesia induction. FD, the water-soluble prodrug of propofol, was initially developed by Eisai in Japan and was approved by the FDA for marketing in the United States in 2008. However, due to formaldehyde accumulation, safety concerns in outpatient settings, and the requirement for administration by anesthesiologists, the product had poor sales and was withdrawn in 2012. Subsequently, short-term FD use was found resulting in limited formaldehyde accumulation, which is then metabolized to formate at levels comparable to endogenous concentrations, posing no significant health risk. Most adverse events, including respiratory depression and hypotension, were found to be transient, self-limiting, and predominantly mild to moderate in severity. On May 25, 2021, the National Medical Products Administration (NMPA) approved the injection of FD, with the approval number H20210017. As a new type Class I drug applied for market registration in China, it is indicated for general anesthesia induction in adults. The review covers the known and emerging characteristics of pharmacokinetic and pharmacodynamic properties of FD approved by the FDA and the new type Class I FD approved by China, emphasizing their non-inferior sedative efficacy and relatively mild adverse reactions compared to propofol and provides insights into their safer application in a broader population. Additionally, it highlights the necessity of structured personnel management during sedation and anesthesia procedures. In short, FD can be safely and effectively used for endoscopic examinations, minor surgeries and continuous sedation in the ICU. While FD demonstrates safety and efficacy as a sedative in specific clinical scenarios, larger and more rigorous clinical trials are essential to validate its long-term use, application in high-risk populations, and administration by non-anesthesiologist healthcare providers.Keywords: fospropofol disodium, propofol, sedation, general anesthesia, induction, efficacy and safety
