Clinical Safety of Gadoxetate Disodium: Insights From 20 Years of Use and More Than 12 Million Administrations

钆塞酸二钠的临床安全性:来自20年使用和超过1200万次给药的启示

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Abstract

OBJECTIVE: To comprehensively analyze worldwide safety data of gadoxetate disodium after 20 years of use and to review its reclassification from group III to group II on the American College of Radiology (ACR) nephrogenic systemic fibrosis (NSF)-risk classification scheme. MATERIALS AND METHODS: Two safety data sets were analyzed: 23 clinical phase I to IV studies and Bayer pharmacovigilance database (PV) from 2004 to 2024. In addition, a literature review on NSF reports with special focus on patients with different degrees of renal impairment was performed. Patients' exposure was based on the assumption that one vial or prefilled syringe was given to each patient for each procedure, with an estimated total of over 12 million administrations. The primary target variable was the number, frequency and characteristics of unrelated/related adverse events (AEs) in clinical studies and adverse drug reactions (ADRs) reported to PV. Incidence and reporting rates were analyzed by descriptive statistical methods. RESULTS: A total of 10,282 patients were included in clinical phase I to IV studies. Drug-related AEs were reported in 6% and 1.7% in phase III and IV studies, respectively. Nine (0.11%) related serious adverse events (SAEs) were recorded in phase IV, none in phase III. The most frequently recorded AEs (related or unrelated to drug) in phases I to III were nausea (1.4%) and headache (1.2%). All other AEs were reported ≤ 1.0%. In phase IV, dyspnea (0.34%) and nausea (0.28%) (related or unrelated) were most frequently reported. More than 12 million doses of gadoxetate were administered according to sales data. Most frequently reported ADRs from the PV were hypersensitivity reactions (reporting rate 0.0147%), nausea (0.0029%) and pain (0.0019%). Exposure increased steadily from 16,578 administrations in 2006 to 1,289,979 per year by December 31, 2024. Conversely, the ADR rate decreased from 0.21% in 2006 to ≤0.05% in 2011 through 2024. No report diagnostic of or consistent with NSF was documented, even in patients with renal impairment. CONCLUSION: Liver-specific gadoxetate disodium demonstrated a favorable safety profile in patients independent of their renal function. No report diagnostic of or consistent with NSF has been reported with over 20 years of use. The well-established benefit/risk profile of gadoxetate disodium prompted the ACR to reclassify it from group III to group II as of April 2024.

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