Phosphodiesterase Inhibitor

Ibudilast (1) is a non-selective phosphodiesterase (PDE) inhibitor with the inhibition profile shown in Table 1.^1,2) Especially, 1 strongly inhibits PDE4 isozymes (Table 2).³⁾ Ledeboer et al. referred to in their review⁴⁾ that preclinical studies indicated that 1 could cross the blood-brain barrier.

References

• 1) Possible role of cyclic AMP phosphodiesterases in the actions of ibudilast on eosinophil thromboxane generation and airways smooth muscle tone
  • J. E. Souness, M. E. Villamil, L. C. Scott, A. Tomkinson, M. A. Giembycz, D. Raeburn, Br. J. Pharmacol. 1994, 111, 1081.
• 2) Ibudilast: A Non-selective PDE Inhibitor with Multiple Actions on Blood Cells and the Vascular Wall
  • Y. Kishi, S. Ohta, N. Kasuya, S. Sakita, T. Ashikaga, M. Isobe, Cardiovasc. Drug Rev. 2001, 19, 215.
• 3) Preferential inhibition of human phosphodiesterase 4 by ibudilast
  • Z. Huang, S. Liu, L. Zhang, M. Salem, G. M. Greig, C. C. Chan, Y. Natsumeda, K. Noguchi, Life Sci. 2006, 78, 2663.
• 4) Ibudilast (AV-411): a new class therapeutic candidate for neuropathic pain and opioid withdrawal syndromes
  • A. Ledeboer, M. R. Hutchinson, L. R Watkins, K. W. Johnson, Expert Opin. Investig. Drugs 2007, 16, 935.

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