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Chemical Compound Review:

Tetomilast 6-[2-(3,4-diethoxyphenyl)- 1,3-thiazol-4...

Synonyms: CHEMBL332750, SureCN436663, OPC-6535, ACMC-1BW9F, AG-D-89770, ...

Bloomfield, G.L. et al., Hasegawa, T. et al., Schreiber, S. et al., Cheng, X.S. et al., Ejiri, S. et al.

Schreiber, Keshavarzian, Isaacs, Schollenberger, Guzman, Orlandi, Hanauer,

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Disease relevance of OPC-6535

CONCLUSIONS: This phase II trial of tetomilast in ulcerative colitis did not achieve statistical significance for the primary end point [1].
BACKGROUND: The objective of this study was to investigate the effects of OPC-6535 on Propionibacterium acnes-primed and lipopolysaccharide-induced liver injury in the rat [2].
OPC-6535, a superoxide anion production inhibitor, attenuates acute lung injury [3].
Treatment with OPC-6535 failed to prevent the development of pulmonary hypertension and systemic hypotension [3].
Treatment of animals with OPC-6535 prior to the onset of sepsis produced significant protection against acute lung injury but failed to attenuate hemodynamic derangements associated with sepsis [3].

High impact information on OPC-6535

BACKGROUND & AIMS: Tetomilast (OPC-6535), a novel thiazole compound, inhibits phosphodiesterase-4 and proinflammatory functions of leukocytes including superoxide production and cytokine release [1].
Superoxide production in the myocardium was significantly higher in the IL-1 beta group than in the control group at day 2 (p < 0.01), and OPC-6535 significantly suppressed the IL-1 beta-induced superoxide production (p < 0.01) [4].
OPC-6535 reduced TNF-alpha, AST, and ALT, but did not affect GRO/CINC-1 or myeloperoxidase [2].
Treatment with OPC-6535 suppressed superoxide and TNF-alpha but did not affect GRO/CINC-1 [2].
Treatment with OPC-6535 significantly reduced acute lung injury, as indicated by improved bronchoalveolar lavage protein and neutrophil content, resulting in a significant improvement in arterial oxygenation [3].

Anatomical context of OPC-6535

CONCLUSION: Attenuation of liver injury by OPC-6535 is believed to be due to its inhibitory effects on superoxide and TNF-alpha production by hepatic macrophages in P. acnes- and lipopolysaccharide-treated rats [2].

Analytical, diagnostic and therapeutic context of OPC-6535

Protective effect of OPC-6535, a superoxide anion production inhibitor, on liver grafts subjected to warm ischemia during porcine liver transplantation [5].

References

A randomized, placebo-controlled, phase II study of tetomilast in active ulcerative colitis. Schreiber, S., Keshavarzian, A., Isaacs, K.L., Schollenberger, J., Guzman, J.P., Orlandi, C., Hanauer, S.B. Gastroenterology (2007) [Pubmed]
Effects of OPC-6535 on lipopolysaccharide-induced acute liver injury in the rat: involvement of superoxide and tumor necrosis factor-alpha from hepatic macrophages. Hasegawa, T., Sakurai, K., Kambayashi, Y., Saniabadi, A.R., Nagamoto, H., Tsukada, K., Takahashi, A., Kuwano, H., Nakano, M. Surgery (2003) [Pubmed]
OPC-6535, a superoxide anion production inhibitor, attenuates acute lung injury. Bloomfield, G.L., Ridings, P.C., Blocher, C.R., Fisher, B.J., Sugerman, H.J., Nagamoto, H., Fowler, A.A. J. Surg. Res. (1997) [Pubmed]
Role of superoxide anion in the pathogenesis of cytokine-induced myocardial dysfunction in dogs in vivo. Cheng, X.S., Shimokawa, H., Momii, H., Oyama, J., Fukuyama, N., Egashira, K., Nakazawa, H., Takeshita, A. Cardiovasc. Res. (1999) [Pubmed]
Protective effect of OPC-6535, a superoxide anion production inhibitor, on liver grafts subjected to warm ischemia during porcine liver transplantation. Ejiri, S., Eguchi, Y., Kishida, A., Kurumi, Y., Tani, T., Kodama, M. Transplant. Proc. (2000) [Pubmed]

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