武内 徹
Fuculty of Medicine
Department of Internal Medicine (Ⅳ)
R&D stage
The Challenge
“The Missing Piece in Macrophage-Targeted Therapy”
Intractable inflammatory diseases such as ulcerative colitis (inflammatory bowel disease: IBD) and interstitial lung disease (ILD) require effective treatments with minimal side effects.
Macrophages (MΦ), along with S100A8 and S100A9 proteins, play key roles in the pathogenesis of inflammatory diseases.
The Innovation
“A World-First Macrophage-Specific Delivery System Targeting CD68: DDS”
hMIKO-1 is a low-molecular-weight protein designed based on S100A8/A9.
It is internalized into human macrophages via the CD68 receptor, which is highly expressed on these cells, and significantly suppresses the expression of inflammatory cytokines, thereby regulating excessive macrophage activation.
Proof of Concept
“Demonstrated Remarkable Tissue Repair in IBD and ILD”
In multiple disease models, we have confirmed not only symptomatic relief but also clear histological improvement beyond conventional palliative treatment.
In particular, hMIKO-1 has shown exceptionally high potential in suppressing pulmonary fibrosis, a condition recognized as highly intractable. These findings provide strong evidence supporting its advancement toward clinical application.
IBD model rat
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Negative control
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Positive control (5% DSS administration)
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M0.6 (5% DSS+hMIKO-1 administration)
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Clinical and histological improvements were observed in 5% dextran sulfate sodium (DSS)-induced IBD model rats.
NC: negative control PC: positive control M0.2-0.6: hMIKO-1 0.2-0.6 mg/day. H&E staining
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The intestinal length was restored!
IBD model mouse
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Negative control
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Positive control (BLM administration)
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M (BLM+hMIKO-1 administration)
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Histological improvement was observed in bleomycin (BLM)-induced interstitial lung disease (ILD) model mice, with suppression of collagen and inflammatory cytokine production.
Masson's trichrome staining
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Future Vision
Potential as a therapeutic agent for inflammatory and fibrotic conditions beyond IBD and ILD
Development into a next-generation DDS targeting macrophages (MΦ) by conjugating desired nucleic acids or drugs
Related Publications and Intellectual Property
- Okada K, Ikemoto M. Inflammation, 2022
- Kotani T, Ikemoto M, Takeuchi T. Int J Mol Sci, 2022
- Patent：特許第6891157号, Related Patent Applications Pending