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Safety and Pharmacokinetics of PSD502 in Healthy Chinese Male and Female Volunteers: Two Randomized, Double-Blind, Placebo-Controlled, Phase I Trials

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Abstract

Background and Objective

PSD502 is a metered-dose spray for premature ejaculation. The two trials aimed to evaluate the safety and pharmacokinetics of PSD502 in healthy Chinese male and female individuals.

Methods

Two phase I, randomized, double-blind, placebo-controlled trials were conducted in men (Trial 1) and women (Trial 2). The participants were randomized 3:1 to receive PSD502 (7.5 mg of lidocaine and 2.5 mg of prilocaine per spray) or a placebo. For male individuals, a single dose (three sprays) once daily was applied to the glans penis for 21 days except for nine sprays (three doses) on days 7 and 14, 4 h apart for each dose. For female individuals, two sprays were applied to the vagina and one to the cervix once daily for 7 days. The primary endpoint was safety. Pharmacokinetics analysis was also performed.

Results

Twenty-four male and 24 female individuals were recruited. Treatment-emergent adverse events occurred in 38.9% (7/18) of male individuals and 66.7% (12/18) of female individuals in the PSD502 group, respectively. Both trials reported 50.0% (3/6) treatment-emergent adverse events for the placebo. No grade ≥ 3 treatment-emergent adverse events, serious adverse events, or treatment-emergent adverse events leading to early withdrawal or discontinuation occurred. After consecutive applications, lidocaine and prilocaine cleared rapidly in both trials. Plasma concentrations exhibited high inter-individual variability. The maximum plasma concentrations of active ingredients were far below the anticipated minimum toxic concentrations. The area under the plasma concentration–time curve of metabolites were ≤ 20% of the parent drugs. No clinically significant accumulations were observed in the two trials.

Conclusions

PSD502 was well tolerated and showed low plasma concentrations in healthy Chinese male and female individuals.

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Acknowledgments

The authors acknowledge all the participants in these two trials and thank Xin Wang from Fosun Pharma for her contribution to the study design. Medical writing assistance was provided by MedSci and funded by Fosun Pharma.

Author information

Authors and Affiliations

  1. Department of Drug Clinical Trial Center, Peking University Third Hospital, Huayuan North Road No. 49, Haidian, Beijing, China

    Fangfang Wang, Zhiping Liu, Xiaoye Niu, Lin Zhao, Jixiang Zhu & Haiyan Li

  2. Department of Cardiology and Institute of Vascular Medicine, NHC Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides, Key Laboratory of Molecular Cardiovascular Science, Ministry of Education, Beijing Key Laboratory of Cardiovascular Receptors Research, Peking University Third Hospital, Beijing, China

    Fangfang Wang & Haiyan Li

  3. National Clinical Research Center for Obstetrics and Gynecology, Peking University Third Hospital, Huayuan North Road No. 49, Haidian, Beijing, China

    Linjing Qi & Xiaoye Wang

  4. Shanghai Fosun Pharmaceutical (Group) Co., Ltd, Shanghai, China

    Lu Liu, Ziyang Liu, Yunan Sun, Lei Diao & Jun Lu

  5. Jiangsu Wanbang Biopharmaceuticals Co., Ltd, Xuzhou, China

    Yongchun Zhou

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  1. Fangfang Wang
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Corresponding authors

Correspondence to Xiaoye Wang or Haiyan Li.

Ethics declarations

Funding

These studies were funded by Wanbang Biopharmaceuticals.

Conflict of interest

Lu Liu, Ziyang Liu, Yunan Sun, Lei Diao, and Jun Lu are full-time employees of Fosun Pharma. Yongchun Zhou is a full-time employee of Wanbang Biopharmaceuticals. Fangfang Wang, Zhiping Liu, Xiaoye Niu, Lin Zhao, Jixiang Zhu, Linjing Qi, Xiaoye Wang, and Haiyan Li have no conflicts of interest that are directly relevant to the content of this article.

Ethics approval

The protocols of two trials (CTR20213292 and CTR20213291) were approved by the Institutional Review Board of Peking University Third Hospital (Beijing, China). The studies were conducted in accordance with the 1964 Declaration of Helsinki and its later amendments and all Chinese regulatory requirements.

Consent to participate

Written informed consent was obtained from all subjects for these two studies before the screening.

Consent for publication

Not applicable.

Availability of data and material

All data generated or analyzed during this study are included in this published article and its supplementary information files.

Code availability

Not applicable.

Author contributions

Conceptualization: LD, JL, YZ, XW, and HL; methodology: LL and ZL; investigation: FW, ZL, XN, LZ, JZ, and LQ; formal analysis: YS; and writing (review and editing): FW, ZL, XN, LZ, JZ, LQ, LL, ZL, YS, LD, JL, YZ, XW, and HL.

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Wang, F., Liu, Z., Niu, X. et al. Safety and Pharmacokinetics of PSD502 in Healthy Chinese Male and Female Volunteers: Two Randomized, Double-Blind, Placebo-Controlled, Phase I Trials. Clin Drug Investig 43, 503–515 (2023). https://doi.org/10.1007/s40261-023-01277-4

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  • DOI: https://doi.org/10.1007/s40261-023-01277-4

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