Phase I, Single-Dose Study to Assess the Pharmacokinetics and Safety of Suramin in Healthy Chinese Volunteers

• Published in: Drug design, development and therapy development and therapy, 2023-01, Vol.17, p.2051-2061
• Main Authors: Wu, Guolan, Zhou, Huili, Lv, Duo, Zheng, Ruling, Wu, Lihua, Yu, Songxia, Kai, Jiejing, Xu, Nana, Gu, Lie, Hong, Nanfang, Shentu, Jianzhong
• Format: Article
• Language: English
• Subjects: antiviral; Antiviral agents; Area Under Curve; clinical pharmacokinetics; Dosage and administration; Dose-Response Relationship, Drug; Double-Blind Method; drug repurposing; East Asian People; Half-Life; Healthy Volunteers; Humans; Original Research; safety; suramin; Suramin - adverse effects; Suramin sodium; Virus diseases
• ISSN: 1177-8881; 1177-8881
• DOI: 10.2147/DDDT.S416325

Suramin is a multifunctional molecule with a wide range of potential applications, including parasitic and viral diseases, as well as cancer. A double-blinded, randomized, placebo-controlled single ascending dose study was conducted to investigate the safety, tolerability, and pharmacokinetics of suramin in healthy Chinese volunteers. A total of 36 healthy subjects were enrolled. All doses of suramin sodium and placebo were administered as a 30-minute infusion. Blood and urine samples were collected at the designated time points for pharmacokinetic analysis. Safety was assessed by clinical examinations and adverse events. After a single dose, suramin maximum plasma concentration (C ) and area under the plasma concentration-time curve from time zero to the time of the last measurable concentration (AUC ) increased in a dose-proportional manner. The plasma half-life (t ) was dose-independent, average 48 days (range 28-105 days). The cumulative percentages of the dose excreted in urine over 7 days were less than 4%. Suramin can be detected in urine samples for longer periods (more than 140 days following infusion). Suramin was generally well tolerated. Treatment-emergent adverse events (TEAEs) were generally mild in severity. The PK and safety profiles of suramin in Chinese subjects indicated that 10 mg/kg or 15 mg/kg could be an appropriate dose in a future multiple-dose study.