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Bharucha, A.E. et al.

A.E. Bharucha, A. Kulkarni, K.M. Choi, M. Camilleri, M. Lempke, G.J. Brunn, S.J. Gibbons, A.R. Zinsmeister, G. Farrugia,

First-in-human study demonstrating pharmacological activation of heme oxygenase-1 in humans.

Heme oxygenase (HO)-1 degrades heme and protects against oxidative stress, but it has not been pharmacologically induced in humans. In this randomized study of 10 healthy volunteers, hemin (3 mg/kg intravenously in 25% albumin) was shown to increase plasma HO-1 protein concentration four- to fivefold and HO-1 activity ~15-fold relative to baseline at 24 and 48 h (placebo -56.41 +/- 6.31 (baseline), 69.79 +/- 13.00 (24 h), 77.44 +/- 10.62 (48 h) vs. hemin -71.70 +/- 9.20 (baseline), 1,126.20 +/- 293.30 (24 h), 1,192.20 +/- 333.30 (48 h)) in four of five subjects as compared with albumin alone (P </= 0.03). This represents the overcoming of a fundamental hurdle to HO-1 research in humans.[1]

References

First-in-human study demonstrating pharmacological activation of heme oxygenase-1 in humans. Bharucha, A.E., Kulkarni, A., Choi, K.M., Camilleri, M., Lempke, M., Brunn, G.J., Gibbons, S.J., Zinsmeister, A.R., Farrugia, G. Clin. Pharmacol. Ther. (2010) [Pubmed]

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