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Kidney Week

Abstract: FR-OR022

Lubiprostone in CKD: Insights into Mitochondrial Function and Polyamines from a Randomized Phase 2 Clinical Trial

Session Information

Category: CKD (Non-Dialysis)

  • 2302 CKD (Non-Dialysis): Clinical, Outcomes, and Trials

Authors

  • Watanabe, Shun, Tohoku Daigaku, Sendai, Miyagi Prefecture, Japan
  • Nakayama, Masaaki, St. Luke's International Hospital, Chuo-ku, Tokyo, Japan
  • Yokoo, Takashi, Tokyo Jikeikai Ika Daigaku, Minato, Tokyo, Japan
  • Sanada, Satoru, Sendai Byoin, Sendai, Miyagi Prefecture, Japan
  • Ubara, Yoshifumi, Toranomon Byoin, Minato, Tokyo, Japan
  • Komatsuda, Atsushi, Akita Daigaku, Akita, Akita Prefecture, Japan
  • Asanuma, Katsuhiko, Chiba Daigaku, Chiba, Chiba Prefecture, Japan
  • Suzuki, Yusuke, Juntendo Daigaku, Bunkyo, Tokyo, Japan
  • Konta, Tsuneo, Yamagata Daigaku, Yamagata, Yamagata Prefecture, Japan
  • Kazama, Junichiro James, Fukushima Kenritsu Ika Daigaku, Fukushima, Fukushima Prefecture, Japan
  • Suzuki, Takehiro, Tohoku Daigaku, Sendai, Miyagi Prefecture, Japan
  • Taguchi, Kensei, Kurume Daigaku, Kurume, Fukuoka Prefecture, Japan
  • Fukami, Kei, Kurume Daigaku, Kurume, Fukuoka Prefecture, Japan
  • Toyohara, Takafumi, Tohoku Daigaku, Sendai, Miyagi Prefecture, Japan
  • Tanaka, Tetsuhiro, Tohoku Daigaku, Sendai, Miyagi Prefecture, Japan
  • Abe, Takaaki, Tohoku Daigaku, Sendai, Miyagi Prefecture, Japan

Group or Team Name

  • LUBI-CKD TRIAL Investigators.
Background

Chronic kidney disease (CKD) often progresses to end-stage renal disease, with constipation being a risk factor. While lubiprostone, a chloride channel activator, improved eGFR in our primary analysis (Kidney Week 2023, FR-PO971), its efficacy across CKD severity and underlying mechanisms are unclear. This presentation further investigates lubiprostone's effects based on renal dysfunction severity and explores its renoprotective mechanisms.

Methods

This Phase II, randomized, double-blind, placebo-controlled study enrolled 150 patients with stage IIIb-IV CKD in Japan, receiving placebo, 8 µg, or 16 µg lubiprostone for 24 weeks. Primary endpoint was indoxyl sulfate. Secondary endpoints included other uremic toxins and renal function markers. Subgroup analyses evaluated treatment effects based on baseline renal function severity (moderate: eGFR 36–45 mL/min/1.73 m2, severe: eGFR 25–35 mL/min/1.73 m2). Multiomics analyses (metabolomics, metagenomics) on blood, urine, and stool samples (n=46) explored mechanisms.

Results

Lubiprostone didn't significantly alter uremic toxin levels. However, eGFR was improved in the 16 µg group by trial end, a key finding of our primary analysis. Importantly, subgroup analysis showed both 8 and 16 µg lubiprostone were effective in moderate CKD patients, but no significant differences were observed in the severe group. Multiomics analyses indicated lubiprostone modulated the gut microbiome, increasing circulating polyamine levels confirmed by targeted measurements. We further showed, in vivo and in vitro, that polyamine exposure improved mitochondrial function and renal function, supporting that increased polyamines contribute to renoprotection.

Conclusion

Lubiprostone is a novel and safe therapeutic agent that mitigates renal function decline in patients with CKD. Its renoprotective effects are particularly evident in patients with moderate renal dysfunction and appear to be mediated, at least in part, by the modulation of the gut microbiota-polyamine axis, leading to influences mitochondrial function. Key findings of this work are under revision for publication.
Clinical Trials Registry Number: UMIN000023850

Funding

  • Commercial Support – Sucampo Pharma, LLC.

Digital Object Identifier (DOI)