Description
Pentoxifylline is a xanthine derivative that exhibits anti-inflammatory, cardioprotective, antithrombotic, analgesic, and anti-fibrotic activities. Pentoxifylline is clinically used to treat intermittent claudication, peripheral vascular disease, and neuropathies. Pentoxifylline is a non-selective inhibitor of phosphodiesterases (PDEs) that increases cAMP levels and activates PKA; it also inhibits adenosine A2 receptors. In vitro, pentoxifylline decreases phosphorylation of IκBα and suppresses activity of NFκB. This compound also inhibits inflammation-induced hyperalgesia and separately, suppresses fibrin-induced epithelial-to-mesenchymal transition (EMT) and the development of fibrosis in animal models.
References
Fang CC, Huang JW, Shyu RS, et al. Fibrin-Induced epithelial-to-mesenchymal transition of peritoneal mesothelial cells as a mechanism of peritoneal fibrosis: effects of pentoxifylline. PLoS One. 2012;7(9):e44765. PMID: 23028611
Nowak Ł, Zurowski D, Dobrogowski J, et al. Pentoxifylline modifies central and peripheral vagal mechanism in acute and chronic pain models. Folia Med Cracov. 2012;52(1-2):83-95. PMID: 23697217
Deree J, Martins JO, Melbostad H, et al. Insights into the regulation of TNF-alpha production in human mononuclear cells: the effects of non-specific phosphodiesterase inhibition. Clinics (Sao Paulo). 2008 Jun;63(3):321-8. PMID: 18568240.
Marques LJ, Zheng L, Poulakis N, et al. Pentoxifylline inhibits TNF-alpha production from human alveolar macrophages. Am J Respir Crit Care Med. 1999 Feb;159(2):508-11. PMID: 9927365.
Ward A, Clissold SP. Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy. Drugs. 1987 Jul;34(1):50-97. PMID: 3308412.
