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Purpose <p>Ustekinumab, targeting interleukin (IL)-12 and IL-23, is effective in treating chronic immune-mediated inflammatory diseases, but needs to be dosed via subcutaneous (SC) injection, which impacts patient comfort and treatment adherence. To enable oral dosing of ustekinumab, the utility of a robotic pill (RP) was evaluated in humans.</p> Methods <p>A Phase 1 study was conducted to evaluate the safety, tolerability, and pharmacokinetics (PK) of single doses (0.5 and 0.75&#xa0;mg) of an ustekinumab biosimilar (CT-P43) delivered via RP (RT-111) in healthy participants compared to ustekinumab (0.5&#xa0;mg) administered via SC injection.</p> Results <p>RT-111 was well-tolerated with no reported SAEs. Ustekinumab was detected in 35/40 participants dosed with RT-111. At the 0.5&#xa0;mg dose, RT-111 and SC administration yielded similar C<sub>max</sub> (RT-111: 67 ± 7 ng/mL, SC: 56 ± 4 ng/mL), while a dose-proportional increase in C<sub>max</sub> was observed at the 0.75&#xa0;mg dose (92 ± 8 ng/mL). Uptake via oral delivery was faster, with a T<sub>max</sub> of 3 vs. 10 days for the SC group. Bioavailability of RT-111 was comparable (81%) to that of SC injection.</p> Conclusion <p>This is the first report of successful oral delivery of a therapeutic antibody via an orally ingestible RP in humans, with bioavailability comparable to SC injection.</p> Clinical trial number <p>Study was registered at Clinicaltrials.gov as NCT05890118 in May 2023.</p>

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Oral delivery of an ustekinumab biosimilar with bioavailability comparable to subcutaneous administration in healthy human participants

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年1月19日

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  • Joshua T. Myers,
  • Alyson Yamaguchi,
  • Kyle Horlen,
  • Leonard C. Fung,
  • April Toledo Vo,
  • Deepa Mohan,
  • Mary Hoopes,
  • Mir Imran,
  • Jacques Van Dam,
  • Ofer M. Gonen,
  • Mir A. Hashim,
  • Arvinder K. Dhalla,
  • Andrew Blauvelt

摘要

Purpose

Ustekinumab, targeting interleukin (IL)-12 and IL-23, is effective in treating chronic immune-mediated inflammatory diseases, but needs to be dosed via subcutaneous (SC) injection, which impacts patient comfort and treatment adherence. To enable oral dosing of ustekinumab, the utility of a robotic pill (RP) was evaluated in humans.

Methods

A Phase 1 study was conducted to evaluate the safety, tolerability, and pharmacokinetics (PK) of single doses (0.5 and 0.75 mg) of an ustekinumab biosimilar (CT-P43) delivered via RP (RT-111) in healthy participants compared to ustekinumab (0.5 mg) administered via SC injection.

Results

RT-111 was well-tolerated with no reported SAEs. Ustekinumab was detected in 35/40 participants dosed with RT-111. At the 0.5 mg dose, RT-111 and SC administration yielded similar Cmax (RT-111: 67 ± 7 ng/mL, SC: 56 ± 4 ng/mL), while a dose-proportional increase in Cmax was observed at the 0.75 mg dose (92 ± 8 ng/mL). Uptake via oral delivery was faster, with a Tmax of 3 vs. 10 days for the SC group. Bioavailability of RT-111 was comparable (81%) to that of SC injection.

Conclusion

This is the first report of successful oral delivery of a therapeutic antibody via an orally ingestible RP in humans, with bioavailability comparable to SC injection.

Clinical trial number

Study was registered at Clinicaltrials.gov as NCT05890118 in May 2023.