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

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

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Abstract

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 (3mg/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 48h (placebo 56.41±6.31 (baseline), 69.79±13.00 (24h), 77.44±10.62 (48h) vs. hemin 71.70±9.20 (baseline), 1,126.20 293.30 (24h), 1,192.20 333.30 (48h)) 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.

Original languageEnglish (US)
Pages (from-to)187-190
Number of pages4
JournalClinical pharmacology and therapeutics
Volume87
Issue number2
DOIs
StatePublished - Feb 1 2010

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Bharucha, A. E., Kulkarni, A. A., Choi, K. M., Camilleri, M., Lempke, M., Brunn, G. J., Gibbons, S. J., Zinsmeister, A. R., & Farrugia, G. (2010). First-in-human study demonstrating pharmacological activation of heme oxygenase-1 in humans. Clinical pharmacology and therapeutics, 87(2), 187-190. https://doi.org/10.1038/clpt.2009.221