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Safety and Tolerability of Bismuthyl Ecabet Suspension, a Novel Anti-Ulcer Agent, following Single and Multiple Oral Dose Administration in Healthy Chinese Subjects

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Abstract

Background: Bismuthyl ecabet is a combination of sulfodehydroabietic acid and bismuth, which forms a new type of salt that is useful in treating peptic ulcers and gastritis.

Objective: This study was designed to assess the safety and tolerability of bismuthyl ecabet suspension in healthy Chinese subjects.

Methods: For the study 77 volunteers were randomized into single- or multiple-dose groups for oral administration of bismuthyl ecabet 200–1600 mg once daily or 1200 mg twice daily for 7 days. Safety and tolerability were assessed by adverse events, physical examination and serum biochemistry.

Results: In both the single- and multiple-dose studies, no severe adverse events were observed in any of the volunteers. The main adverse events caused by the drug in single-dose groups were an increase in serum alanine transaminase (ALT), γ-glutamyl transpeptidase, blood urea nitrogen, total bilirubin and skin rash. The numbers of adverse events judged to be possibly related to the drug were 2/18 in the 400 mg, 2/18 in the 800 mg, 1/8 in the 1200 mg, and none in the 200 or 1600 mg dose groups. In the multiple-dose studies, an increased serum ALT and aspartate transaminase (AST) was found in one subject after 7 days of administration of the drug. All serum biochemistry returned to normal levels and skin rash resolved after 7 days without any special treatment.

Conclusion: Bismuthyl ecabet was shown to be safe and well tolerated in healthy Chinese subjects. The oral dosing regimen selected for subsequent phase II/III clinical trials was 800 mg twice daily.

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Acknowledgements

Nana Tang and Yongqing Wang contributed equally to this work as co-first authors. This study was supported by Cinmed Pharmaceuticals Co. Ltd, Shanghai, China.

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Authors and Affiliations

  1. Research Division of Clinical Pharmacology, the First Affiliated Hospital, Nanjing Medical University, 300 Guangzhou Road, Nanjing, 210029, China

    Yongqing Wang,  Ling Meng, Peipei Zhang, Kun Xu, Ningling Jiang, Haibo Zhang, Ning Ou, Deqin Wu, Anjiu Chen & Xiyong Zhang

  2. Department of Gastroentrology, the First Affiliated Hospital, Nanjing Medical University, 300 Guangzhou Road, Nanjing, 210029, China

    Nana Tang &  Ruihua Shi

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  1. Yongqing Wang
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  2. Nana Tang
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  3. Ling Meng
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  9. Deqin Wu
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  11. Xiyong Zhang
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Correspondence to Ling Meng or Ruihua Shi.

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Wang, Y., Tang, N., Meng, L. et al. Safety and Tolerability of Bismuthyl Ecabet Suspension, a Novel Anti-Ulcer Agent, following Single and Multiple Oral Dose Administration in Healthy Chinese Subjects. Clin Drug Investig 32, 247–252 (2012). https://doi.org/10.2165/11599110-000000000-00000

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  • DOI: https://doi.org/10.2165/11599110-000000000-00000

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