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Clinical Trial
. 2023 Jul 11:17:2051-2061.
doi: 10.2147/DDDT.S416325. eCollection 2023.

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

Guolan Wu  1   2   3 , Huili Zhou  1   2 , Duo Lv  1   2 , Ruling Zheng  4 , Lihua Wu  1 , Songxia Yu  1   2 , Jiejing Kai  1   2 , Nana Xu  1   2 , Lie Gu  5 , Nanfang Hong  5 , Jianzhong Shentu  1   2
Affiliations
Clinical Trial

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

Guolan Wu et al. Drug Des Devel Ther. .

Abstract

Purpose: Suramin is a multifunctional molecule with a wide range of potential applications, including parasitic and viral diseases, as well as cancer.

Methods: 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.

Results: After a single dose, suramin maximum plasma concentration (Cmax) and area under the plasma concentration-time curve from time zero to the time of the last measurable concentration (AUClast) increased in a dose-proportional manner. The plasma half-life (t1/2) 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.

Conclusion: 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.

Keywords: antiviral; clinical pharmacokinetics; drug repurposing; safety; suramin.

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Conflict of interest statement

Lie Gu and Nanfang Hong are employed by Hainan Honz Pharmaceutical Co., Ltd. who funded the study. Jianzhong Shentu, as the principal investigator, received funding from Hainan Honz Pharmaceutical Co., Ltd. All other authors declare no competing interests.

Figures

Figure 1
Figure 1
Study design. Placebo-treated subjects were followed for at least 28 days until unblinding permits in each dose group. PK sampling time was up to 140 days for suramin treatment cohorts to better characterize the terminal phase, given the long elimination half-life based on emerging data.
Figure 2
Figure 2
Mean concentration–time curve with standard deviation for suramin in healthy human subjects after a single dose.
Figure 3
Figure 3
Dose linearity plots of Cmax and AUC parameters in a single ascending-dose study.
See this image and copyright information in PMC

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Grants and funding

This work was funded by Hainan Honz Pharmaceutical Co., Ltd. This work was also supported by Zhejiang Provincial Science and Technology Department Key R & D Plan Emergency Project (No. 2020c03123-8).

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